Potential Antimicrobial Agents Research Articles

Synthesis of N-Benzylidene-N'-(2-chloroquinolin-3-ylmethylene)hydrazine Derivatives and Their Evaluation as Potential Antimicrobial Agents

Synthesis of N-Benzylidene-N'-(2-chloroquinolin-3-ylmethylene)hydrazine Derivatives and Their Evaluation as Potential Antimicrobial Agents

Synthesis and characterization of luminescent Cu2+-doped fluorapatite nanocrystals as potential broad-spectrum antimicrobial agents.

Nanomaterials based on metal-doped fluorapatite (FAP) have attracted considerable interest as potential next-generation antimicrobial agents. In this study, Cu2+-doped FAP nanocrystals have been successfully synthesized by a neutralization method at room temperature. Their structural, optical, antimicrobial, and hemcompatible properties have been investigated. XRD, FTIR, FESEM, and N2 adsorption-desorption studies indicate the formation of single-phase FAP mesoporous nanopowders, composed of rod-like particles. TEM images confirmed the formation of nanorodes with a length of 60nm and a width of about 18nm. Rietveld analysis shows that the Cu2+ ions preferentially substitute Ca2 (6h) sites in the hexagonal fluorapatite crystal structure. Fluorescence spectroscopy accompanied by MCR-ALS method confirms substitution of Cu2+ ions in FAP crystal lattice with extracting additional d-d band transition at green color from FAP broadband self-activated luminescence in violet-blue color. Antimicrobial studies conducted on Staphylococcus aureus, Escherichia coli and Micrococcus lysodeikticus showed that FAP nanopowder with the highest Cu2+ content have strong bacteriostatic action on Staphylococcus aureus bacterial strain in mediums containing nutrition matters. In addition, this sample in comparison to pure FAP achieved a high percentage of relative reduction of bacterial population for all three species, being >90% in most cases. Fungistatic action is noticed too, throwgh the slowing down mycelium growth of fungus Aspergillus niger, Aspergillus flavus and Penicillium roqueforti and reduction of sporulation of Aspergillus niger species. Cu2+-doped FAP nanocrystals shows a synergistic antimicrobial effect with Cu2+ and F- ions. Concerning the potential biomedical applications, the hemolysis ratios of the Cu2+-doped FAP samples were below 5%. The obtained results pointed out the possible use of the synthesized nanocrystals as broad-spectrum antimicrobial agents for various biomedical and health care preparations.

Isolation of Antimicrobial Peptides (AMPs) From Different Sources: A Review

Antimicrobial peptides (AMPs) are small peptide molecules produced by a wide range of species, from bacteria to higher vertebrates, as a part of the innate immune system. These naturally produced peptides fight against intrusive microbes like viruses, bacteria, and fungi. AMPs are produced in various body parts by different organisms, such as skin secretion of amphibians; leaf, stem, fruits, or whole parts of plants; glandular secretion of mammals; the venom of reptiles and arthropods, etc. Due to this source variation, there is no universal method for the isolation, i.e., extraction and purification of the AMPs. Therefore, several techniques have been established to extract and purify these natural peptides from various sources. Generally, solid-phase extraction and chemical extraction techniques are the most common methods used for the extraction of AMPs. For purification and identification purposes, chromatography, gel electrophoresis, filtration, Edman degradation, circular dichroism, mass spectrometry, etc. are mainly adopted. In this review, we provide a brief discussion on the isolation process of AMPs based on their sources. This study would be helpful in isolating newer AMPs that could be used as potential antimicrobial agents. Bangladesh Pharmaceutical Journal 26(1): 99-111, 2023 (January)

Novel benzenesulfonamide bearing 1,2,4-triazoles as potent anti-microbial and anti-oxidant agents

Novel benzenesulfonamide bearing 1,2,4-triazoles as potent anti-microbial and anti-oxidant agents

Antimicrobial potency of Punica granatum peel extract: Against multidrug resistant clinical isolates

Normal human flora such as Staphylococcus aureus, Staphylococcus epidermidis, Cutibacterium acnes, Corynebacterium kroppenstedtii, and Escherichia coli could emerge as highly potent opportunistic skin and enteric pathogens. Due to their emerging resistance towards antibiotics, the scope of existing antibacterial therapy and treatment regime is very limited. In the present study, Punica granatum (P. granatum) peel extract is used as an antibacterial agent active against multidrug-resistant bacteria. Interaction with P. granatum peel extract showed strong antibacterial activity with minimum inhibitory concentration value and zone of inhibition ranging between 780 μg/ml to 6250 μg/ml and 20 ± 0.0 to 24.33 ± 2.082 mm respectively. These values evident a strong antibacterial efficacy against antibiotic-resistant Gram-positive (S. aureus, S. epidermidis, C. acnes, and C. kroppenstedtii clinical isolate NB-2) and Gram-negative (E. coli) bacteria. Interestingly, PGP extract also showed a concentration-dependent reduction of biofilm-embedded bacteria, observed 93.2 % ± 1.8 eradication at 25,000 μg/ml with respect to control, in S. epidermidis ATCC 35984 bacterium. PGP extract exhibited strong antioxidant activity and observed 94.7 ± 0.06 % scavenging activity at 1000 μg/ml PGP extract concentration as determined by the cell-free assay. Further, a promising synergistic effect of PGP extract with the commercial antimicrobials such as piroctolamine, zinc pyrithione, and tetracycline against multi-drug resistant, C. kroppenstedtii clinical isolate NB-2 is evaluated. Greater antibacterial potential of the synergistic effect of the peel's extract with the drugs has been observed when compared to the drug alone suggesting that the P. granatum could be the potent antimicrobial agent against antibiotic-resistant skin infection-causing bacteria.

Glycerol based carbon sulfonic acid catalyzed synthesis, in silico studies and in vitro biological evaluation of isonicotinohydrazide derivatives as potent antimicrobial and anti-tubercular agents

The present pathway involves synthesis of isonicotinohydrazide derivatives using isoniazid and diversely substituted aldehydes in the presence of EtOH and catalytic amount of glycerol based carbon sulfonic acid catalyst. The developed pathway has so many merits like excellent yields (91–98%), short reaction time (4–10 min), easy reaction set up, no need of column chromatography, large substrate scope, easily recyclable and reusable catalyst. The synthesized compounds were screened for antimicrobial and anti-tubercular activity and it was observed that compounds possessed high biological potency against the Gram positive and Gram negative bacterial and fungal strains. Regarding anti-tubercular activity, compound 3m exhibited high % inhibition against Mycobacterium tuberculosis H37RV strain. Based on the outcome of in vitro studies, all the synthesized compounds were docked against E. coli (1KZN), C. albicans (1IYL), and M. tuberculosis H37Rv strain (2NSD). The synthesized derivatives were docked within the binding site of 1KZN, and 1IYL. However, with 2NSD, apart from 3h, all the derivatives displayed interaction within the binding cavity of the protein. All the crucial interactions with Asn46, Asp73, and Arg136 in 1KZN, His227, Leu451 in 1IYL, and Tyr158 in 2NSD were witnessed in the top-scored docked candidates. Molecular docking studies revealed the importance of the substitution at R position on isonicotinohydrazide scaffold. The nitrogen atoms of hydrazide moiety were involved in forming hydrogen bonding with the active site amino acids, and the substitution at the R position occupy the hydrophobic position in the binding pocket. Also, the functional groups present on the substituted R position were involved in forming hydrogen bonding with the crucial active site residues.

Synthesis, characterization of 1,2,4-triazolidine-3-thione tethered beta-aryl butanoic acid and butanoate derivatives as potent antimicrobial and antioxidant agents and their molecular docking studies

As a tactic for the drug discovery and development framework to tackle resistance to antibiotics, the target triazolidine-3-thione substituted butanoic acid and butanoate derivatives were synthesized using an effective and environmentally friendly protocol. IR, NMR, and LC-MS spectroscopy were used to characterize the synthesized moieties and subjected to in vitro antimicrobial activity evaluation. Some of the molecules have shown promising results especially against C. albicans with lower minimum inhibitory concentration (MIC). The compounds have also shown very good DPPH radical scavenging ability when compared to the standard gallic acid. Further, the cytotoxicity evaluation of the molecules against HeLa cells associated with acetyl CoA enzyme assay with minimum inhibition of the enzyme have shown lower toxicity of the molecules. The molecular docking study against Staph gyrase B enzyme revealed excellent interaction of molecules with the enzyme's active site.

Three Innovations of Next-Generation Antibiotics: Evolvability, Specificity, and Non-Immunogenicity

Antimicrobial resistance is a silent pandemic exacerbated by the uncontrolled use of antibiotics. Since the discovery of penicillin, we have been largely dependent on microbe-derived small molecules to treat bacterial infections. However, the golden era of antibiotics is coming to an end, as the emergence and spread of antimicrobial resistance against these antibacterial compounds are outpacing the discovery and development of new antibiotics. The current antibiotic market suffers from various shortcomings, including the absence of profitability and investment. The most important underlying issue of traditional antibiotics arises from the inherent properties of these small molecules being mostly broad-spectrum and non-programmable. As the scientific knowledge of microbes progresses, the scientific community is starting to explore entirely novel approaches to tackling antimicrobial resistance. One of the most prominent approaches is to develop next-generation antibiotics. In this review, we discuss three innovations of next-generation antibiotics compared to traditional antibiotics as specificity, evolvability, and non-immunogenicity. We present a number of potential antimicrobial agents, including bacteriophage-based therapy, CRISPR-Cas-based antimicrobials, and microbiome-derived antimicrobial agents. These alternative antimicrobial agents possess innovative properties that may overcome the inherent shortcomings of traditional antibiotics, and some of these next-generation antibiotics are not merely far-fetched ideas but are currently in clinical development. We further discuss some related issues and challenges such as infection diagnostics and regulatory frameworks that still need to be addressed to bring these next-generation antibiotics to the antibiotic market as viable products to combat antimicrobial resistance using a diversified set of strategies.

Coumarin Triazoles as Potential Antimicrobial Agents.

Currently, in hospitals and community health centers, microbial infections are highly common diseases and are a leading cause of death worldwide. Antibiotics are generally used to fight microbial infections; however, because of the abuse of antibiotics, microbes have become increasingly more resistant to most of them. Therefore, medicinal chemists are constantly searching for new or improved alternatives to combat microbial infections. Coumarin triazole derivatives displayed a variety of therapeutic applications, such as antimicrobial, antioxidant, and anticancer activities. This review summarizes the advances of coumarin triazole derivatives as potential antimicrobial agents covering articles published from 2006 to 2022.

Effect of Length of Storage and Chemical Additives on the Nutritive Value and Starch Degradability of Reconstituted Corn Grain Silage

The aim of this study was to evaluate the feed quality of reconstituted corn grain silage (RCGS), treated with chemical additives and stored for 15, 30, or 60 d in 5-L plastic buckets. Dry ground corn was rehydrated to 350 g·kg−1 and treated with either polysorbate 80 (2 L·t−1) (POL), propionic acid 28% (2 L·t−1) (PRO), Mycoflake™ (2 L·t−1-blend polysorbate 80 and propionic acid) (MYC) or nothing (CON). The effect of the length of storage was combined in a factorial arrangement with the additives. Ammonia-N increased from d-15 of storage. A treatment × storage length interaction was observed for ethanol content at d-60 of storage, and all treatments had lower ethanol concentration than CON. There was an interaction for butyric acid content at d-30 and d-60 of storage; CON showed higher butyric acid concentration than treated silages. Aerobic stability increased from d-15 to d-30. At d-15 of storage, the PRO and MYC treatments decreased the DM losses. The length of storage increased the ruminal in situ degradability of starch, and DM and MYC increased the DM degradability in 3.6 percentage units at 12 h of incubation, compared with POL. In conclusion, increasing the length of storage of the RCGS from d-15 to d-60 improved the starch and DM degradability. Mycoflake increased the availability of nutrients, and the length of storage enhanced the aggregation of particles; further, polysorbate 80 (Tween 80) might be further studied as a potential antimicrobial agent in silages.

Development of Nanoparticle Adaptation Phenomena in Acinetobacter baumannii: Physiological Change and Defense Response.

The present work describes the evolution of a resistance phenotype to a multitargeting antimicrobial agent, namely, silver nanoparticles (nanosilver; NAg), in the globally prevalent bacterial pathogen Acinetobacter baumannii. The Gram-negative bacterium has recently been listed as a critical priority pathogen requiring novel treatment options by the World Health Organization. Through prolonged exposure to the important antimicrobial nanoparticle, the bacterium developed mutations in genes that encode the protein subunits of organelle structures that are involved in cell-to-surface attachment as well as in a cell envelope capsular polysaccharide synthesis-related gene. These mutations are potentially correlated with stable physiological changes in the biofilm growth behavior and with an evident protective effect against oxidative stress, most likely as a feature of toxicity defense. We further report a different adaptation response of A. baumannii to the cationic form of silver (Ag+). The bacterium developed a tolerance phenotype to Ag+, which was correlated with an indicative surge in respiratory activity and changes in cell morphology, of which these are reported characteristics of tolerant bacterial populations. The findings regarding adaptation phenomena to NAg highlight the risks of the long-term use of the nanoparticle on a priority pathogen. The findings urge the implementation of strategies to overcome bacterial NAg adaptation, to better elucidate the toxicity mechanisms of the nanoparticle, and preserve the efficacy of the potent alternative antimicrobial agent in this era of antimicrobial resistance. IMPORTANCE Several recent studies have reported on the development of bacterial resistance to broad-spectrum antimicrobial silver nanoparticles (nanosilver; NAg). NAg is currently one of the most important alternative antimicrobial agents. However, no studies have yet established whether Acinetobacter baumannii, a globally prevalent nosocomial pathogen, can develop resistance to the nanoparticle. The study herein describes how a model strain of A. baumannii with no inherent silver resistance determinants developed resistance to NAg, following prolonged exposure. The stable physiological changes are correlated with mutations detected in the bacterium genome. These mutations render the bacterium capable of proliferating at a toxic NAg concentration. It was also found that A. baumannii developed a "slower-to-kill" tolerance trait to Ag+, which highlights the unique antimicrobial activities between the nanoparticulate and the ionic forms of silver. Despite the proven efficacy of NAg, the observation of NAg resistance in A. baumannii emphasises the potential risks of the repeated overuse of this agent on a priority pathogen.

The role of aggregation and ionization in the chemical instability of Amphotericin B in aqueous methanol

Amphotericin B (AmB) is a potent antimicrobial agent used in clinical practice. Nevertheless, the mechanism of its aqueous instability remains not yet fully understood, especially the role that its aggregation state plays in this process. Therefore, the current study used an aqueous methanol media to evaluate the AmB instability as a function of pH-, organic solvent- and concentration-dependent ionization and aggregation. To reach this goal, the aggregation status and instability were determined using UV–vis spectroscopy, LC-MS and HPLC. Moreover, not only the hydrolytic degradation products were identified by UV–vis spectroscopy and LC-MS, but also, the degradation rate constants were estimated by nonlinear regression. The results indicated that monomeric AmB was the predominant species under pH conditions, wherein the substrate was cationic (pH < 4) or anionic (pH > 9). On the other hand, aggregated AmB form was the predominant species for the zwitterionic substrate (at methanol concentration < 30 %(v/v)). Anionic substrate degraded by specific base-catalyzed lactone hydrolysis. Oxidation accounted for the loss of zwitterionic substrate. Aggregated zwitterionic AmB exhibited lower stability than monomeric zwitterionic AmB under neutral pH conditions. These studies are a step forward in comprehending the degradation kinetics of AmB in aqueous medium. In fact, along with our previous research on AmB instability in oils, it leads to a better understanding of the AmB stability in complex systems with an oil–water interface, such as disperse lipid systems.

Facile synthesis, antimicrobial screening and docking studies of pyrrole-triazole hybrids as potential antimicrobial agents

Facile synthesis, antimicrobial screening and docking studies of pyrrole-triazole hybrids as potential antimicrobial agents

Assessment of Iris albicans lange as potential antimicrobial and analgesic agent.

Objective of the present work was to evaluate the presence of phytochemical constituents and pharmacological activities (antimicrobial and anti-nociceptive) of crude extract isolated from Iris albicans and its corresponding fractions. Extraction was made with methanol and extract was evaluated for the presence of different bioactive constituents, as per standard protocols. Extract and its corresponding fractions were evaluated for their antimicrobial and anti-nociceptive potential. Well diffusion method was used to evaluate the antibacterial effects while anti-nociceptive effect was studied using in-vivo models (acetic acid induced writhing, hotplate and tail immersion tests) at different dose level (100, 200 and 300 mg/kg of body weight) and compared with diclofenac sodium (dose = 10 mg/kg body weight). Results showed that the I. albicans extracts contained secondary metabolites including alkaloids, phytosterols, flavonoids, saponins, terpenoids, tannins, phenols, steroids, fixed oil, glycosides and carbohydrates. Furthermore, it was observed that different fractions in decreasing polarity order such as chloroform >n-Hexane > Ethyl acetate > Crude Methanol > Aqueous extract exhibited effective antimicrobial response against all test organisms. Results of the study showed that the extracts have significant antimicrobial and analgesic activity, providing evidence for its folklore use.

New thioxothiazolidinyl-acetamides derivatives as potent urease inhibitors: design, synthesis, in vitro inhibition, and molecular dynamic simulation

To identify potent urease inhibitors, in the current study, a series of thioxothiazolidinyl-acetamides were designed and synthesized. The prepared compounds were characterized by spectroscopic techniques, including FTIR, 1HNMR, 13CNMR, and elemental analysis. In the enzymatic assessments, it was demonstrated that all derivatives had significant urease inhibition with IC50 values in the range of 1.473–9.274 µM in comparison with the positive control hydroxyurea (IC50 = 100.21 ± 2.5 µM) and thiourea (IC50 = 23.62 ± 0.84 µM). Compound 6i (N-benzyl-3-butyl-4-oxo-2-thioxothiazolidine-5-carboxamide) was the most active agent with an IC50 value of 1.473 µM. Additionally, kinetic investigation and in silico assessments of 6i was carried out to understand the type of inhibition and behavior of the most potent derivative within the binding site of the enzyme. Noteworthy, the anti-urease assay against P. vulgaris revealed 6e and 6i as the most active agents with IC50 values of 15.27 ± 2.40 and 17.78 ± 3.75 µg/mL, respectively. Antimicrobial evaluations of all compounds reveal that compounds 6n and 6o were the most potent antimicrobial agents against the standard and resistant S. aureus. 6n and 6o also showed 37 and 27% inhibition in the development of biofilm by S. aureus at 512 µg/ml. Furthermore, the MTT test showed no toxicity up to 100 µM. Taken together, the study suggests that the synthesized thioxothiazolidinyl-acetamides bases derivatives may serve as potential hits as urease inhibitors.

Effect of Panax quinquefolius extract on Mycobacterium abscessus biofilm formation

Mycobacterium abscessus (M. abscessus) can exist either as planktonic bacteria or as a biofilm. Biofilm formation is one of the important causes of conversion to resistance to antibiotics of bacteria that were previously sensitive when in their planktonic form, resulting in infections difficult to manage. Panax quinquefolius and its active ingredient ginsenosides have the potential ability in fighting pathogenic infections. In this study, the P. quinquefolius extract (PQE) showed good antibacterial/bactericidal activity against the M. abscessus planktonic cells. The extract reduced the biomass, thickness, and number of M. abscessus in the biofilm and altered its morphological characteristics as well as the spatial distribution of dead/alive bacteria. Moreover, the ginsenoside CK monomer had a similar inhibitory effect on M. abscessus planktonic bacteria and biofilm formation. Therefore, PQE and its monomer CK might be potential novel antimicrobial agents for the clinical prevention and treatment of M. abscessus, including biofilms in chronic infections.

A Review on Efficacy of Spices and Herbs as per Ayurveda and Their Role as a Potent Antioxidant and Antimicrobial Agents

Bioactive compounds from spices and herbs play an important role to immunize our body system. From ancient time they are used as Ayurvedic medicine. This review mainly focuses on to the traditional medicinal uses of spices and herbs as per Ayurveda and their efficacy as a natural potent antioxidant and antimicrobial agents over synthetic one. The chemical component of essential oils were analysed by GC-MS and GC-FID techniques. Antioxidant activity was confirmed by different assays like DPPH assay, FRAP assay, ABTS assay, Hydroxy radical scavenging assay, NO scavenging assay etc. Quantitative estimation of phenol and flavonoid from different solvent extracts revealed the proportional relationship between concentration of polyphenols and antioxidant activity. Zone of inhibition (in mm), MIC and MBC were measured to assess the antimicrobial activity against different pathogens like Escherichia coli, Staphylococcus aureus, Staphylococcus epidermidis, Bacillus subtilis, Bacillus cereus, Pseudomonas aeruginosa, Streptococcus pyogensis etc. Spices and herbs can be used as potent and safe Ayurvedic drug along with their use in cooking and seasoning different foods.

Iron metabolism in the cell as a target in the development of potential antimicrobial and antiviral agents.

The search and creation of innovative antimicrobial drugs, acting against resistant and multiresistant strains of bacteria and fungi, are one of the most important tasks of modern bioorganic chemistry and pharmaceuticals. Since iron is essential for the vital activity of almost all organisms, including mammals and bacteria, the proteins involved in its metabolism can serve as potential targets in the development of new promising antimicrobial agents. Such targets include endogenous mammalian biomolecules, heme oxygenases, siderophores, protein 24p3, as well as bacterial heme oxygenases and siderophores. Other proteins that are responsible for the delivery of iron to cells and its balance between bacteria and the host organism also attract certain particular interest. The review summarizes data on the development of inhibitors and inducers (activators) of heme oxygenases, selective for mammals and bacteria, and considers the characteristic features of their mechanisms of action and structure. Based on the reviewed literature data, it was concluded that the use of hemin, the most powerful hemooxygenase inducer, and its derivatives as potential antimicrobial and antiviral agents, in particular against COVID-19 and other dangerous infections, would be a promising approach. In this case, an important role is attributed to the products of hemin degradation formed by heme oxygenases in vitro and in vivo. Certain attention has been paid to the data on the antimicrobial action of iron-free protoporphyrinates, namely complexes with Co, Ga, Zn, Mn, their advantages and disadvantages compared to hemin. Modification of the well-known antibiotic ceftazidime with a siderophore molecule increased its effectiveness against resistant bacteria.

Synthesis and pharmacological evaluation of 1,3-diaryl substituted pyrazole based (thio)urea derivatives as potent antimicrobial agents against multi-drug resistant Staphylococcus aureus and Mycobacterium tuberculosis.

The urgent development of newer alternatives has been deemed a panacea for tackling emerging antimicrobial resistance effectively. Herein, we report the design, synthesis, and biological evaluation of 1,3-diaryl substituted pyrazole-based urea and thiourea derivatives as antimicrobial agents. Preliminary screening results revealed that compound 7a (3,4-dichlorophenyl derivative) exhibited potent activity against S. aureus (MIC = 0.25 μg mL-1) and compound 7j (2,4-difluorophenyl derivative) against Mycobacterium tuberculosis (MIC = 1 μg mL-1). Compounds 7a and 7j were non-toxic to Vero cells with a favorable selectivity index of 40 and 200, respectively, and demonstrated good microsomal stability. Compound 7a exhibited equipotent activity (MIC = 0.25 μg mL-1) against various multidrug-resistant strains of S. aureus, which include various strains of MRSA and VRSA, and elicited bacteriostatic properties. In an enzymatic assay, 7a effectively inhibited DNA gyrase supercoiling activity at a concentration of 8 times MIC. Further, molecular modeling studies suggested that compound 7a binds at the active site of DNA gyrase with good affinity.

Synthesis, Characterization and ADME Prediction Study of Heterocyclic Moieties-linked Indole Derivatives as Potential Antimicrobial Agents

Background: Heterocyclic compounds are vital for research due to their diverse pharmacological profiles. They are key structural components of many of the potent antimicrobial drugs available on the market today but still facing the problem of drug resistance by microbes. Indole and its derivatives display versatile pharmacological activities, such as analgesic, antimicrobial, antidepressant, antidiabetic, anti-convulsant, antihelmintic, and anti-inflammatory. Objective: Indole ring was linked to other key heterocyclic moieties, such as morpholine, imidazole, piperidine, and piperazine at the active 3rd position by Schotten-Baumann reaction, and further evaluated against Gram-positive and Gram-negative bacteria with the hope to develop potent antimicrobial agents. Method: Synthesis of derivatives was performed under appropriate conditions and characterized by IR, NMR (1H and 13C), and CHN elemental analysis. Further, in vitro assays were used to evaluate their antimicrobial activity by agar diffusion and agar streak dilution method against Bacillus subtilis (ATCC 6633) and Escherichia coli (ATCC 25922). ADME properties were also calculated using the Swiss ADME online program. Results: Compounds 4b, 4f, 4i, 4k showed maximum potency in both in vitro assays calculated as the zone of inhibition (17±0.5 mm-22±0.25 mm) and minimum inhibitory concentration (MIC= 6.25-25 μg/ml)) comparable to standard drugs ciprofloxacin and ampicillin. ADME results showed zero violation of the Lipinski’s rule. Conclusion: A great deal of work has been done on the synthesis and evaluation of indole derivatives to explore their antimicrobial effect. These findings may lead to the design and development of more effective antimicrobial drug candidates.