Bond Conjugation Research Articles

Forging 1,1'-Bicyclopropenyls by Synergistic Au/Ag Dual-Catalyzed Cyclopropenyl Cross-Coupling.

1,1'-Bicyclopropenyl is a constitutional isomer of benzene comprising two coupled cyclopropene units with the endocyclic double bonds in conjugation. Due to the intrinsic high strain energy, it remains a long-standing challenge to prepare 1,1'-bicyclopropenyl derivatives, particularly multisubstituted, nonsymmetrical ones, in an efficient and modular manner. Herein a straightforward Au/Ag bimetallic-catalyzed cyclopropenyl cross-coupling has been developed, providing a robust and versatile strategy for the rapid assembly of symmetrical and unsymmetrical 1,1'-bicyclopropenyl derivatives from cyclopropenyl benziodoxoles (CpBXs) and terminal cyclopropenes. Advantages of this strategy include tolerance to a wide range of synthetically useful functional groups, mild reaction conditions, and a simple catalytic system. The obtained 1,1'-bicyclopropenyl derivatives were shown to be valuable synthetic intermediates through selective downstream manipulations.

Humidity-sensitive luminescent dye-doped polyelectrolyte films: Fabrication, characterization, and potential application as colorimetric moisture sensor

A novel type of luminescent dye-doped polyelectrolyte films, which change their light absorption and photoluminescent properties upon changing relative humidity (RH) is reported. A polyelectrolyte – poly(4-styrene sulfonic acid) (PSSA) was chosen as a matrix, while Coumarin 6 (C6) was used as a luminescent dye. The films were prepared using a dip-coating technique. Coatings with a refractive index (RI) of around 1.49 and various thicknesses in a submicrometric range were obtained by changing the withdrawal speed or concentration of the polyelectrolyte. It was found that depending on the RH, C6 in the polyelectrolyte films may exist in two equilibrium forms – monocationic and dicationic. Significant differences between these two forms upon RH level variations were observed and investigated using FT-IR and UV–Vis spectroscopic techniques. FT-IR spectroscopy confirmed the distortion of the double bond conjugation in the benzothiazole unit of the dicationic form of the dye in the dry state. The dependences of the UV–Vis absorption and luminescent properties on RH were determined. The distinct color changes of the films, ranging from faint yellow to intense pink-red, enabled the estimation of the RH level through visual inspection. Taking advantage of a straightforward preparation protocol for this newly developed material, we believe that it may be used as a humidity-sensitive coating.

Synthesis and Biological Evaluations of Granulatamide B and its Structural Analogues.

While granulatamides A and B have been previously isolated, their biological activities have been only partially examined. The aim of this study was to synthesize granulatamide B (4b), a tryptamine-derivative naturally occurring in Eunicella coral species, using the well-known procedure of Sun and Fürstner and its 12 structural analogues by modifying the side chain, which differs in length, degree of saturation as well as number and conjugation of double bonds. The prepared library of compounds underwent comprehensive assessment for their biological activities, encompassing antioxidative, antiproliferative, and antibacterial properties, in addition to in vivo toxicity evaluation using a Zebrafish model. Compound 4i, which consists of a retinoic acid moiety, exhibited the strongest scavenging activity against ABTS radicals (IC50 = 36 ± 2 μM). In addition, 4b and some of the analogues (4a, 4c and 4i), mostly containing an unsaturated chain and conjugated double bonds, showed moderate but non-selective activity with certain IC50 values in the range of 20-40 μM. In contrast, the analogue 4l, a derivative of alpha-linolenic acid, was the least toxic towards normal cell lines. Moreover, 4b was also highly active against Gram-positive Bacillus subtilis with an MIC of 125 μM. Nevertheless, both 4b and 4i, known for the best-observed effects, caused remarkable developmental abnormalities in the zebrafish model Danio rerio. Since modification of the side chain did not significantly alter the change in biological activities compared to the parent compound, granulatamide B (4b), the substitution of the indole ring needs to be considered. Our group is currently carrying out new syntheses focusing on the functionalization of the indole core.

Electrocatalytic Reduction of Disulfide Bonds across Chemical Modalities.

The chemical properties of disulfides are leveraged in a wide array of applications, ranging from protein-drug conjugates for cancer treatment to self-healing materials. However, disulfide reduction strategies remain severely underdeveloped despite being the key to efficiently accessing the desired targets. Specifically, no homogeneous catalyst has been reported for this reaction, and conditions that allow the use of mild and green reductants (e.g., via electrochemical reduction) are not known. Herein, we unveil a vitamin B12-catalyzed, electrochemically driven protocol for efficiently reducing disulfide bonds in various aqueous buffers over a broad pH range. This robust and simple method is suitable for disulfide reductions of substrates ranging from small molecules to large proteins. Finally, one-pot reduction and conjugation of disulfide bonds in a monoclonal antibody were demonstrated to produce antibody conjugates.

Ca2+-nano starch-lutein endowed 3D printed surimi with antioxidation and mutual reinforcing transmembrane transport mechanisms via hepg2 and caco-2 cells model

To better enhance printing effects meanwhile casting functionality, antioxidation and absorption of bioactive component in printed Ca2+-nano starch (NS)-lutein (L)-surimi were investigated. Results shown that Ca2+-NS-L promoted surimi printability due to enhanced gel strength and denser structure. Mixing Ca2+-NS-L endowed printed surimi with antioxidation (DPPH, ABTS, hydroxyl radical, Fe2+ reduction were 42 %, 79 %, 65 %, 0.104 mg·mL−1, respectively) due to the ability of lutein with more –OH groups and conjugate bonds to capture free radicals. It also manifested in cellular antioxidation that Ca2+-NS-L-surimi regulated the level of Nrf2 to protect gene expression of antioxidases (SOD, CAT, GSH-Px increased by 30–180 %, compared to damaged cells) through keap1-Nrf2-ARE pathway. Additionally, lutein absorption and transportation of Ca2+-NS-L-surimi increased by 20 %, compared to NS-L. Possibly, combination of samples and membrane was facilitated by surface hydrophobic, promoting endocytosis. Meanwhile, digestive surimi (peptides) with acidic-alkaline amino acids and negative charges made samples be attracted and moved in bypass parts under electrostatic traction and repulsion (electrostatic domain) to promote transport process. Also, Ca2+ facilitated CaM expression in membrane and formed Ca2+ channel by combining with CaM to accelerate entry of samples into cells. Conclusively, Ca2+-NS-L both strengthened printability of surimi and antioxidation, promoting application of printed functional surimi.

Antioxidant Mechanism, Spectroscopic and Pharmacological Properties of Four Flavonoids: DFT, Docking and Molecular Dynamics.

Myricetin (1), Quercetin (2), Kaempferol (3) and Kaempferide (4) were flavonoids with phenolic hydroxyl groups. The antioxidant and pharmacological mechanisms of them were investigated in detail. The lowest hydroxyl dissociation enthalpies of 1, 2, 3 and 4 were calculated by DFT, respectively. The hydroxyl dissociation enthalpies of the four flavonoids at the O2 site are the highest. By analyzing the intramolecular hydrogen bonds and HOMO-LUMO orbitals of the four flavonoids, the reasons for their divergence of hydroxyl dissociation enthalpies and antioxidant mechanisms were further investigated. The UV-vis and IR spectra of four flavonoids were compared. The interactions about electrostatic attraction, p-π conjugation and hydrogen bond combined the flavonoid with the target protein closely. The root mean square deviation of peroxisome proliferator-activated receptor γ combined with 1, 2 and 3 increased, while that of PPARγ combined with 4 decreased.

Design, Synthesis, and Antifungal Activities of Novel Potent Fluoroalkenyl Succinate Dehydrogenase Inhibitors.

The development of new fungicide molecules is a crucial task for agricultural chemists to enhance the effectiveness of fungicides in agricultural production. In this study, a series of novel fluoroalkenyl modified succinate dehydrogenase inhibitors were synthesized and evaluated for their antifungal activities against eight fungi. The results from the in vitro antifungal assay demonstrated that compound 34 exhibited superior activity against Rhizoctonia solani with an EC50 value of 0.04 μM, outperforming commercial fluxapyroxad (EC50 = 0.18 μM) and boscalid (EC50 = 3.07 μM). Furthermore, compound 34 showed similar effects to fluxapyroxad on other pathogenic fungi such as Sclerotinia sclerotiorum (EC50 = 1.13 μM), Monilinia fructicola (EC50 = 1.61 μM), Botrytis cinerea (EC50 = 1.21 μM), and also demonstrated protective and curative efficacies in vivo on rapeseed leaves and tomato fruits. Enzyme activity experiments and protein-ligand interaction analysis by surface plasmon resonance revealed that compound 34 had a stronger inhibitory effect on succinate dehydrogenase compared to fluxapyroxad. Additionally, molecular docking and DFT calculation confirmed that the fluoroalkenyl unit in compound 34 could enhance its binding capacity with the target protein through p-π conjugation and hydrogen bond interactions.

Approaching Saint Bernard’s Sermons on the “Song of Songs” through the Book of Odes (Shijing): A Confluence of Medieval Theology and Chinese Culture

This paper aims to decode medieval theology from the vantage point of ancient Chinese poetry, employing a cross-textual methodology that encourages a fusion of horizons. It highlights Saint Bernard’s profound and influential theological exegesis of the “Song of Songs”, particularly his comparison of the divine–human relationship to the conjugal bond. The present study posits that readers from Chinese culture can gain access to Saint Bernard’s mystical theology through the sentiment of love, as portrayed in the Book of Odes (Shijing). Initially addressing love as a core human sentiment, this study progresses by juxtaposing the representations of love in the Book of Odes with those in the “Song of Songs”. This comparative analysis culminates in an exploration of Saint Bernard’s theological perspectives, illuminated through these analogous depictions of love. The results affirm that engaging with Saint Bernard’s discourse on love via the Book of Odes is not only feasible but also instrumental in dispelling widespread misconceptions.

Relationship between Flavonoid Chemical Structures and Their Antioxidant Capacity in Preventing Polycyclic Aromatic Hydrocarbons Formation in Heated Meat Model System.

The relationship between the chemical structures of six flavonoids and their abilities to inhibit the formation of polycyclic aromatic hydrocarbons (PAHs) in a heated meat model system was investigated. The PAH8 forming in samples was analyzed by using QuEChERS coupled GC-MS. Inhibitory effects of PAHs were myricetin (72.1%) > morin (55.7%) > quercetin (57.3%) > kaempferol (49.9%) > rutin (32.7%) > taxifolin (30.2%). The antioxidant activities of these flavonoids, assessed through (1, 1-diphenyl-2-picrylhydrazyl) free radical scavenging activity assay (DPPH), [2,2'-azinobis (3-ethylbenzothiazoline-6-sulphonic acid)] free radical scavenging activity assay (ABTS) and ferric ion reducing antioxidant power assay (FRAP) assays, exhibited a significant negative correlation with PAH reduction. Notably, myricetin that contained three hydroxyl groups on the B-ring, along with a 2,3-double bond in conjugation with a 4-keto moiety on the C-ring, demonstrated strong antioxidant properties and free radical scavenging abilities, which significantly contributed to their ability to inhibit PAH formation. However, rutin and taxifolin, substituted at the C-3 position of the C-ring, decreased the PAH inhibitory activity. The ABTS assay proved the most effective in demonstrating the correlation between flavonoid antioxidant properties and their capacity to inhibit PAH formation in heated meat model systems. Thus, the inhibition of PAHs can be achieved by dietary flavonoids according to their chemical structures.

New Cyanostyrylcopillar[5]arene Derivative: Synthesis, Photophysical Study, Chromogenic Detection of Aliphatic Amines, and Biofilm-Antibiofilm Activity.

The synthesis, characterization, and application of a new cyanostyrylcopillar[5]arene 1 is reported. Single-crystal X-ray diffraction and other spectroscopic techniques confirm the identity of the new copillar 1. The X-ray diffraction study reveals that the copillar 1 exhibits a 1D supramolecular chain in the solid state involving π···π interactions along the crystallographic c-axis and 1D chains are further connected by interchain C-H···π interactions to establish 2D supramolecular layers within the crystallographic bc-plane. 2D supramolecular chains on further packing introduce a 3D structure with void spaces filled with hexane molecules. Through minimal deviation in the dihedral angle, the cyano-substituted ethylenic group in 1 shows a conjugation with the phenolic -OH, favoring intramolecular bond conjugation (ITBC) and colorimetrically detects the aliphatic amines over aromatic amines in CH3CN. Among the aliphatic amines, tertiary amines are differentiated from primary and secondary amines by the naked eye through color change. Both in solution and solid states, 1 displays vapor phase detection of volatile aliphatic amines. Antibacterial activity analysis shows that while 1 exhibits the antibiofilm action against Gram-positive pathogenic bacteria, Staphylococcus aureus, it promotes biofilm formation by Gram-negative pathogenic bacteria, Pseudomonas aeruginosa.

Synthesis of multicolour luminescent graphitic carbon nitride quantum dots through controlled graphitization and surface states

Carbon nitride quantum dots are important metal free semiconductors due to their controlled optoelectronics and low toxicity. Here the sulphur heteroatom doping of these nanomaterials is achieved by the low cost hydrothermal process leading to a multicolour photoluminescence. A simple change in water/dimethyl sulfoxide ratio as a solvent helps to achieve a wide tunability in photoluminescence, almost from blue, green, yellow to red with a high quantum yield. This change has been accounted for the particle size, bond conjugation, and heteroatom doping of carbon nitride nanoparticles. Due to multicolour emission, benignity and low cost these materials can be the promising candidates for various optoelectronic applications.

Assignment of product ions produced from ciguatoxin-3C provides a deep insight into the fragmentation mechanism of polycyclic ether compounds.

Marine polycyclic ethers have drawn attention owing to their unique chemical structures and involvement in food poisoning and fish killing. To study structural diversity, we performed a structural assignment of product ions produced from a representative ladder-shaped polycyclic ether, ciguatoxin-3C, and elucidated the mechanism of generation. The product ions used for the structural assignment were produced from a precursor ion [M + H]+ using liquid chromatography/quadrupole time-of-flight mass spectrometry, by employing an atmospheric pressure chemical ionization source. Three charged sites were considered at both terminals of a molecule. Typical charge-remote fragmentation was produced at the respective charge sites, yielding a hybrid spectrum. C-C bonds bordering two ethers could cleave and trigger the fission of two other bonds. Prominent ions indicating the serial loss of water molecules resulted from the simultaneous deprivation of ethereal oxygen and hydrogen atoms. The resultant double bonds formed long chains of conjugated polyenes, which stabilized charge via resonance. Three alternative charge sites produce a hybrid spectrum. The simultaneous fission of three bonds was explained. For the first time, intense ions due to serial dehydration were explained by the elimination of ether oxygen atoms and the subsequent conjugation of double bonds. All product ions were considered by the structural features of polycyclic ether that facilitates the formation of conjugated polyenes.

Enrichment and structural assignment of geometric isomers of unsaturated furan fatty acids.

Furan fatty acids (FuFAs) are valuable minor fatty acids, which are known for their excellent radical scavenging properties. Typically, the furan moiety is embedded in an otherwise saturated carboxyalkyl chain. Occasionally, these classic FuFAs are accompanied by low amounts of unsaturated furan fatty acids (uFuFAs), which additionally feature one double bond in conjugation with the furan moiety. A recent study produced evidence for the occurrence of two pairs of E-/Z-uFuFA isomers structurally related to saturated uFuFAs. Here, we present a strategy that allowed such trace compounds to be enrichedto a level suited for structure determination by NMR. Given the low amounts and the varied abundance ratio of the four uFuFA isomers, the isolation of individual compounds was not pursued. Instead, the entire isomer mixture was enriched to an amount and purity suitable for structure investigation with contemporary NMR methods. Specifically, lipid extracted from 150g latex, the richest known source of FuFAs, was subsequently fractionated by countercurrent chromatography (CCC), silver ion, and silica gel column chromatography. Analysis of the resulting mixture of four uFuFAs isomers (2.4mg in an abundance ratio of 56:23:11:9) by different NMR techniques including PSYCHE verified that the structures of the two most abundant isomers were E-9-(3-methyl-5-pentylfuran-2-yl)non-8-enoic acid and E-9-(3-methyl-5-pent-1-enylfuran-2-yl)nonanoic acid. Additionally, we introduced a computer-based method to generate an averaged chromatogram from freely selectable GC/MS runs of CCC fractions without the necessity of pooling aliquots. This method was found to besuitable to simplify subsequent enrichment steps.

Influence of Thermal Treatments, Extraction Methods, and Storage Conditions on Lycopene Content of Foods

Lycopene is one of the main carotenoids in our daily diet. Fruit variety, environmental conditions, and maturity stage are the factors affecting the content of lycopene. Various processing techniques and extraction methods may also affect the level of lycopene in different food products, consequently changing the biological role of lycopene. The biological role of lycopene is to defend the tissues of tomatoes (conjugate bonds) and attract predators (red colour). Moreover, storage conditions also impact the lycopene content of fruits, vegetables, and their products. Efficient and novel technological interventions are required for stabilizing lycopene content during postharvest procedures, such as refrigeration, heating, extraction, and transportation. Therefore, the study of different crucial factors concerning the change in lycopene content is required. The present review explores the lycopene content of different food commodities and the effect of postharvest operations and processing techniques on lycopene content. It also highlights the storage impact on the concentration of lycopene which may be useful for future studies.

Abstract 2131: Immunoaffinity isolation of EpCAM expressing exosomes utilizing high throughput microfluidic chip with IEDDA chemistry (EpCAM-TCOOncoBean Chip)

Abstract The overall objective of this study is to investigate the microfluidic isolation of tumor derived exosome (TDEs) using the OncoBean Chip, functionalized with the unique inverse electron demand Diels-Alder (IEDDA) for downstream analysis of patient TDEs for therapeutic applications. This chemistry allows for capture and subsequent release of exosomes for immunomodulation and functional studies. We developed an approach for targeting TDEs in patient’s blood plasma by using the epithelial cell adhesion molecule (EpCAM) antibody, a highly expressed biomarker associated with non-small cell lung cancer.The OncoBean Chip is a high throughput radial-flow microfluidic device designed for the specific isolation of TDEs. The bean shaped micro-nodes allow for a varying shear profile to better capture nanosized particles by positioning them towards the middle curvature. We optimized the device using exosomes extracted from cell culture media by ultracentrifugation. First, the surface of the device was salinized with (3-Aminopropyl) triethoxysilane, as an anchor, following plasma activation of the surface. Then, bonded with 3,3'-dithiobis(sulfosuccinimidyl propionate) as a crosslinker, to facilitate the release. Finally, trans-cyclooctene (TCO) is attached as the exposed agent for capture of TDEs. The exosome sample is functionalized with an EpCAM antibody (Ab) conjugated to a tetrazine (Tz) molecule via incubation. The anti-EpCAM-Tz conjugate bonds to surface EpCAM on the TDEs creating a TDE-EpCAM-Tz complex for isolation. The TDEs are processed through the functionalized OncoBean Chip for Ab specific isolation. We tested and validated the EpCAM specific isolation and confirmed TDEs were forming complexes with the Ab-Tz conjugates and not arbitrarily sticking to the nodes. This was done by flowing a sample of TDE-Tz through a functionalized device where little to no capture was expected. Then we evaluated the isolation of EpCAM specific TDEs by using H1650 and A549 exosomes and comparing the capture with CD63, a common exosome marker. Limited capture is expected in the A549 group due to low EpCAM expression for the Ab-Tz conjugate to bind too.Additionally, EV isolation was confirmed and quantified by NTA which reveals capture efficiency up to 90% for the H1650 TDEs. Capture efficiency of the no Ab control was found to be at 30% and below while the A549 control, was found to be at about 20% and below. Hence, our OncoBean Chip with IEDDA chemistry has successfully demonstrated efficient and specific isolation of EpCAM and CD63 expressing TDEs from two different cell lines. Data from Western Blot analysis and scanning electron microscopy further confirm the physical characteristics and protein expression of the TDEs established by the International Society of Extracellular Vesicles (ISEV). Citation Format: Nna-Emeka Onukwugha, Sunitha Nagrath, Henry McEacheron. Immunoaffinity isolation of EpCAM expressing exosomes utilizing high throughput microfluidic chip with IEDDA chemistry (EpCAM-TCOOncoBean Chip) [abstract]. In: Proceedings of the American Association for Cancer Research Annual Meeting 2023; Part 1 (Regular and Invited Abstracts); 2023 Apr 14-19; Orlando, FL. Philadelphia (PA): AACR; Cancer Res 2023;83(7_Suppl):Abstract nr 2131.

Degradation of the Chromophore Functions of Dyes in Irradiated Solutions

Radiolysis damages the system of conjugated bonds and thus leads to the degradation of the chromophore functions of dyes in aqueous solutions. Ten representatives of quinophthalone, indigo, triphenylmethane, and azo dyes exhibited the same type of correlations between the absorbed dose and the degree of discoloration. It was shown using the method of competing scavengers that the color of aerated solutions decreased mainly due to the addition of OH radicals to the dyes. The radiation-chemical yields of discoloration ranged from 0.03 to 0.11 μmol/J and increased depending on the length of bond conjugation in the dye molecules. For practical electron-beam discoloration of dye solutions with a concentration of 20 mg/dm3, anabsorbed dose of 1–1.5 kGy was sufficient.

Acridine as Bioinspired Corrosion Inhibitors

AbstractMild steel has been considerably exploited in various manufacturing and commercial fields due to its tremendous mechanical performance. However, mild steel's high susceptibility to corrosion under acidic conditions leads to vast economic losses and environmental consequences. Inhibitors used for steel corrosion in the acidic medium are ordinarily polar heteroaromatic molecules with electronegative atoms. Acridines are one type of inhibitor with several advantages, such as heteroatoms, functional groups and their polarity, double bond conjugation, and importantly efficient and non‐hazardous synthetic routes. The polar moieties of such inhibitors are considered to augment their adsorption on steel surface, thus creating a shielding to inhibit steel corrosion. Acridine analogs are N‐heterocyclic organic compounds that can be easily produced owing to impeccable inhibition capacity. The current review discusses the chemistry, synthesis, corrosion inhibition mechanism, and properties of acridines and their derivatives.

Geometrical and positional isomers of unsaturated furan fatty acids in food.

Furan fatty acids (FuFA) are important antioxidants found in low concentrations in many types of food. In addition to conventional FuFA which normally feature saturated carboxyalkyl and alkyl chains, a few previous studies indicated the FuFA co-occurrence of low shares of unsaturated furan fatty acids (uFuFA). For their detailed analysis, the potential uFuFA were enriched by centrifugal partition chromatography (CPC) or countercurrent chromatography (CCC) followed by silver ion chromatography from a 4,7,10,13,16,19-docosahexaenoic acid ethyl ester oil, a 5,8,11,14,17-eicosapentaenoic acid ethyl ester oil and a latex glove extract. Subsequent gas chromatography with mass spectrometry (GC/MS) analysis enabled the detection of 16 individual uFuFA isomers with a double bond in conjugation with the central furan moiety. In either case, four instead of two uFuFA isomers previously reported in food, respectively, were detected by GC/MS. These isomers showed characteristic elution and abundance patterns in GC/MS chromatograms which indicated the presence of two pairs of cis/trans-isomers (geometrical isomers).

Extended Double Bond Conjugation in the Chalcone Framework Favours MAO-B Inhibition: A Structural Perspective on Molecular Dynamics.

The monotropic membrane protein monoamine oxidase B (MAO-B) has been shown to be a crucial drug target for the treatment of neurodegenerative diseases. The design of recent inhibitor therapeutic agents of MAO-B involves conjugation and modification of a chalcone scaffold comprising two aryl or heteroaryl rings connected via a short spacer unit with rotatable bonds. Supported by experimental data, these modifications often result in high potent inhibitor compounds. In this study, we employ molecular dynamics simulations to unravel the impact of extended double bond conjugation in two novel compounds, F1 and MO10, toward the inhibition of the MAO-B protein. It was revealed that extended double bond conjugation induced a unidirectional orientation and motion of F1 and MO10, suggesting a stable binding pocket anchorage favouring high-affinity pocket interactions. Conformational analyses also revealed that the incorporated double bond extension impeded the motion of individual binding pocket residues, which subsequently disrupted the functionality of MAO-B. Real-time structural dynamics also revealed that the extended double bond conjugation mediated peculiar interactions with MAO-B binding pocket residues characterized by π-alkyl, π-π stacking, and π-sulphur interactions which buried both compounds into the hydrophobic core of MAO-B and ultimately induced higher binding affinities of both F1 and MO10. These insights present useful structural perspectives of the extended double bond conjugation associated with the experimentally reported enhanced inhibitory activity of F1 and MO10 against MAO-B.

Recent Advancement and Novel Application of Organocatalyzed Aldol Condensation Reactions: A Comprehensive Review

Background: Aldol reactions play an important role in the development of organic synthesis- owing to their critical importance for the conjugation of carbon-carbon bonds while concurrently, one or two chiral centers are reported. In the modern scenario, the Aldol condensation reaction has arisen as perhaps the most significant reaction for the formation of novel medicinal agents, revealing promising pharmacological activities. Objective: The purpose of this study is to present newer synthetic approaches through Aldol condensation reaction for the synthesis of diverse scaffolds to explore the numerous remarkable biological activities. Methods: Aldol condensation concerns the nucleophilic addition reaction of a ketone enolate to an aldehyde to form aldol or β- hydroxy ketone. Occasionally, the aldol addition product losing water molecule yields an α, β-unsaturated ketone. Results: Results showed that peptides of amino acids are utilized as chiral catalysts. As of now, the arrangement of catalysts is intensely one-sided towards proline Conclusion: The present study thus provides useful insight concerning the promising coherent way for the synthesis of prolinamide analogue of proline, through a direct asymmetric aldol condensation reaction. Thus, the current study summarizes various Aldol condensation reactions for the synthesis of novel agents as well as their promising pharmacological importance.