Compounds 4a-f Research Articles

N-(5-Morpholino-2-arylimidazo[2,1-b][1,3,4]thiadiazol-6-yl)carboxamides as Potential Fer/FerT Kinase Inhibitors. Homology Modeling, Molecular Docking Studies and In Silico ADMET Profiling

This study has comparatively evaluated the degree of affinity of N-(5-morpholino-2-arylimidazo[2,1-b][1,3,4]thiadiazol-6-yl)carboxamides 2a-f and 6-(4-isopropylphenyl)-2-(4-((4-methylpiperazin-1-yl)methyl)piperidin-1-yl)imidazo[2,1-b][1,3,4]thiadiazole (E260) to Fer kinase using molecular modeling methods. The Fer kinase model has been generated by homology modeling. It has been shown that compounds 2a-f predominantly form stronger complexes with this enzyme than the reference drug E260. In silico ADMET prediction of the properties of compounds 2a-f and E260 has been carried out. Comparative analysis of the obtained results has shown that compounds 2a-f are not inferior to the reference drug - E260 and even surpass it in most parameters. All examined compounds 2a-f have shown good results under in silico experimental conditions and can be recommended for further study on tumor cell cultures.

Design, synthesis, PASS prediction, in-silico ADME and molecular docking studies of substituted-(Z)-3-benzylidine-5-aza-2-oxindole derivatives (Part-1)

Abstract In this research article we report a simple protocol for the synthesis of series novel of substituted (Z)-3-benzylidine-5-aza-2-oxindole derivatives (5a-f) by employing optimized reaction condition of Knoevenagel condensation. Among the reaction conditions attempted, the reaction in ethanol and piperidine at 80 °C afforded the desired products (5a-f) in satisfactory yields and enhanced purity via trituration and recrystallization. The physicochemical as well as spectroscopic evidences established the assigned structures of the compounds without any ambiguity. The anti-inflammatory proficiency assessment for the synthesized compounds has been carried out on the basis of Prediction of Activity Spectra for Substances (PASS) technique and compared with standard tenidap. Furthermore, to validate the results of PASS prediction, molecular docking studies of the synthesized compounds (5a-f) were carried out on the TNF-α target protein (PDB ID: 2AZ5 ). The compounds displayed less docking energies in the range of -6.9 to -7.5 Kcal/mol than tenidap (-8.8 Kcal/mol). Additionally, in silico ADME analysis was carried out to check drug ability and toxicity issues.

Microwave Assisted, Antimicrobial Activity and Molecular Modeling of Some Synthesized Newly Pyrimidine Derivatives Using 1, 4-diazabicyclo[2.2.2]octane as a Catalyst

Background:Pyrimidine ring is one of the most important heterocyclic scaffolds due to its biological benefits as antimicrobial agents via acting as competitive suppressors of dihydropteroate synthase (DHPS) enzyme, inhibiting dihydrofolate reductase or glucosamine N-phosphate synthase.Objective:The objective of this work is preparing twenty four derivatives of pyrimidine heterocycle 1a-f, 2a-f, 3a-f and 4a-f via a facile one step reaction with antimicrobial potential.Methods:Novel twenty four derivatives of pyrimidine heterocycle 1a-f, 2a-f, 3a-f and 4a-f were prepared via a facile one step reaction by treating substituted aldehydes, urea and / or thiourea and active methylene derivatives (diethyl malonate and / or ethyl cyanoacetate) using 1,4- diazabicyclo[2.2.2]octane (DABCO) as a basic catalyst. The chemical structures of all these novel targets were proved by 1HNMR, 13CNMR, MS and elemental analyses. All the twenty four new targets 1a-f, 2a-f, 3a-f and 4a-f were assessed for their antimicrobial activity towards bacteria as Bacillus subtilis, Staphylococcus aureus, Pseudomonas aeruginosa and Escherichia coli and against fungi represented by Aspergillus flavus and Candida albicans.Results:Most of the compounds exhibited very good antimicrobial activity, especially; compound (1c) exhibited the most activity against three types of bacteria Escherichia coli, Bacillus subtilis, Staphylococcus aureus. Moreover, this derivative 1c displayed similar antifungal activity towards Candida albicans as that exhibited by amphotericin B.Conclusion:All the screened compounds 1a-f, 2a-f, 3a-f and 4a-f showed antibacterial activity with inhibition zone diameter range 6-21 mm/mg, while, regarding the antifungal activity, all the novel derivatives except 2b, 2d, 3a, 3c, 3e did not have any effect towards Aspergillus flavus and 3d did not reveal any inhibitory activity towards both fungal species.

Design, green synthesis, molecular docking and anticancer evaluations of diazepam bearing sulfonamide moieties as VEGFR-2 inhibitors

Novel series of diazepam bearing sulfonamide moieties 5a-f and 7a-c were designed, synthesized and evaluated for anticancer activity against HepG2, HCT-116 and MCF-7 cell lines. MCF-7 was the most sensitive cell line to the influence of the new derivatives. In particular, compound 5d was found to be the most potent derivative overall the tested compounds against the three HepG2, HCT116 and MCF-7 cancer cell lines with IC50 = 8.98 ± 0.1, 7.77 ± 0.1 and 6.99 ± 0.1 µM respectively. Compound 5d exhibited higher activity than sorafenib, (IC50 = 9.18 ± 0.6, 5.47 ± 0.3 and 7.26 ± 0.3 µM respectively), against HepG2 and MCF-7 but exhibited lower activity against HCT116 cancer cell lines respectively. Also, this compound displayed lower activity than doxorubicin, (IC50 = 7.94 ± 0.6, 8.07 ± 0.8 and 6.75 ± 0.4 µM respectively), against HepG2 and MCF-7 but higher activity against HCT116 cell lines respectively. Compounds 5b, 5c, 5d, 5e, 5f and 7c are respectively, 5.77, 8.58, 9.54, 5.71, 4.68 and 2.31 fold times more toxic in breast cancer cell lines (MCF-7, the most sensitive cells) than in VERO normal cells. All the synthesized compounds 5a-f and 7a-c were evaluated for their inhibitory activities against VEGFR-2. Among them, compound 5d was found to be the most potent derivative that inhibited VEGFR-2 at IC50 value of 0.10 ± 0.01 µM, which is equipotent to sorafenib IC50 value (0.10 ± 0.02 µM). Compound 5c exhibited excellent activity with IC50 value of 0.12 ± 0.01 µM which nearly equipotent to that of sorafenib. Compounds 5b, 5e and 5f exhibited very good activity with the same IC50 value of 0.14 ± 0.02 µM. Also, compounds 7c and 7b possessed good VEGFR-2 inhibition with IC50 values of 0.16 ± 0.06 and 0.17 ± 0.06 µM respectively which are more than the half activity of that of sorafenib. The data obtained from docking studies were highly correlated with that obtained from the biological screening.

Synthesis, density functional theory (DFT) studies and urease inhibition activity of chiral benzimidazoles

A variety of benzimidazole by the heterocyclization of orthophenylenediamine were synthesized in 69–86% yields. The synthesized compounds 3a-f and 6a-f were characterized and further investigated as jack bean urease inhibitors. Density functional theory (DFT) studies were performed utilizing the basis set B3LYP/6-31G (d, p) to acquire perception into their structural properties. Frontier molecular orbital (FMO) analysis of all compounds 3a–f and 6a-f was computed at the same level of theory to get a notion about their chemical reactivity and stability. The mapping of the molecular electrostatic potential (MEP) over the entire stabilized molecular geometry indicated the reactive centers. They exhibited urease inhibition activity with IC50 between 22 and 99 μM. Compounds containing withdrawing groups on the benzene ring (3d, 6d) were not showing significant urease inhibition. The value obtained for 3a, 3b, 3f had shown their significant urease inhibition for both theoretical and experimental. Notably, the compound having S-configuration (3a) (22.26 ± 6.2 μM) was good as compared to its R enantiomer 3f (31.42 ± 23.3 μM). Despite this, we elaborated the computational studies of the corresponding compounds, to highlight electronic effect which include HOMO, LUMO, Molecular electrostatic potential (MEP) and molecular docking.

Synthesis and Antibacterial and Antifungal Activity of New Thieno[2,3-d]Pyrimidin-4(3H)-One Derivatives

A series of new 2-(4/3-substitutedbenzyl)thieno[2,3-d]pyrimidin-4(3H)-ones (2a-f) and 2-(4/3-substituted benzyl)-5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidin-4(3H)-one derivatives (3a-f) were synthesized for the first time by the reaction of corresponding 2-aminothiophene-3-carboxamide derivatives and appropriate iminoester hydrochlorides under suitable conditions. Using microdilution method, the antibacterial and antifungal activities of the synthesized compounds were tested against selected strains of Gram positive and Gram negative bacteria (Staphylococcus aureus, Enterecoccus faecalis, Escherichia coli and Pseudomonas aeruginosa) and yeast-like fungi (Candida albicans, C. krusei and C. parapsilosis). In these tests, compounds 3a-f showed higher antifungal activity than fluconazole against Candida fungus species. 2-Substituted thieno-[2,3-d]pyrimidin-4(3H)-ones (2a-f) showed better antibacterial activity than 2-substituted 5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidin-4(3H)-one derivatives (3a-f).

Synthesis, Anticancer and Molecular Docking Studies of N-(1H-benzimidazol-2-yl-carbamothioyl)benzamide Analogues

A series of novel N-(1H-benzimidazole-2-yl-carbamothioyl)benzamide derivatives were synthesized under microwave irradiation and evaluated for anticancer activity. The synthesized compounds were characterized by IR, 1H-NMR, and mass spectral data. Complexity associated with cancer disease and prevalence of diversified cell populations vindicates highly specific treatment options for treatment of cancer. Resistance to these anticancer agents has posed a great hindrance in successful treatment of cancer. Pondering this ongoing situation, it was speculated to develop novel compounds targeting cancer. All the newly synthesized compounds 3a-f were further evaluated for anticancer activity against MCF-7 cell lines using MTT assay. Molecular docking studies were performed using VLife MDS 4.3 software. The compounds 3c exhibited good docking scores of -60.37. The anticancer and docking results highlight the fact that the synthesized compounds 3c could be considered as possible hit as therapeutic agents. A significant correlation was observed between the in silico and the in vitro studies.

Synthesis and antibacterial evaluation of 3-acetyl-2H-selenopyrano[2,3-b]quinolin-2-ones

Abstract In the present study, we have worked out a convenient route for the synthesis of new series of novel 3-acetyl-2H-selenopyrano[2,3-b]quinolin-2-ones (4a-f) by the cyclization of 3-formyl-2-selenoquinolines (3a-f) using ethyl acetoacetate in the presence of catalytic amount of piperidine in acetonitrile as a solvent. The structures of all the synthesized products were confirmed with their elemental analysis, IR, 1H NMR, 13C NMR and mass spectral analysis. All the newly synthesized compounds (4a-f) were screened for in vitro antibacterial activities of three (Staphylococcus aureus, Micrococcus roseus) and (Escherichia coli) by disk diffusion method using ampicillin as positive and Dimethylformamide (DMF) as negative control. The tested, compounds 4d and 4e were highly active against S. aureus and M. roseus (gram positive) and moderately active against E. coli (gram negative), compound 4c was slightly active against M. roseus and E. coli. Compound 4e was slightly active against S. aureus and M. roseus and compounds 4a and 4b were slightly active against M. roseus.

N-alkylated linear heptamethine polyenes as potent non-azole leads against Candida albicans fungal infections

In this study, eighteen heptamethine dyes were synthesised and their antifungal activities were evaluated against three clinically relevant yeast species.. The eighteen dyes were placed within classes based on their core subunit i.e. 2,3,3-trimethylindolenine (5a-f), 1,1,2-trimethyl-1H-benzo[e]indole (6a-f), or 2-methylbenzothiazole (7a-f). The results presented herein imply that the three families of cyanine dyes, in particular compounds 5a-f, show high potential as selective scaffolds to treat C. albicans infections. This opens up the opportunity for further optimisation and investigation of this class compounds for potential antifungal treatment.

Synthesis and characterization of novel ethyl 2-oxo-2H-selenopyrano[2,3-b]quinoline-3-carboxylates and studied their antimicrobial activities

The present study involves the synthesis of substituted novel ethyl 2-oxo-2H-selenopyrano[2,3-b]quinoline-3-carboxylates (4a-f) by the reaction of 3-formyl-2-selenoquinolines (3a-f) with diethyl malanoate in the presence of piperidine. 3-Formyl-2-selenoquinolines (3a-f) were prepared by the action of NaHSe on substituted 2-chloroquinoline-3-carbaldehydes (2a-f). A series of 2-chloroquinoline-3-carbaldehydes (2a-f) were synthesized from substituted acetanilides (1a-f) using available protocol method. The structures of all the newly synthesized compounds were characterized by their elemental analysis, IR, 1H NMR, 13C-NMR and mass spectral data. All the newly synthesized compounds (4a-f) were evaluated for antimicrobial activities. Among the compounds tested, 4d and 4e were highly active against S. aureus and M. roseus.

Synthesis, Characterization, Pass prediction, In-silico ADME, Molecular docking and Cyclic voltammetry studies of 1, 4, 5-trisubstituted 1, 2, 3-triazole ethanone and ethanol derivatives via Metal free approach

Abstract In the present investigation, we focused our interest on the synthesis of 1, 4, 5-disubstituted 1, 2, 3-triazoles ethanone derivative through metal free cycloaddition reaction and their reduced ethanol derivatives. The structures of the compound were established on the basis of spectral data such as FTIR, multi nuclear NMR (1H &13C) and Elemental analysis. Estimation of the pharmacological potential (antimicrobial, antimycobacterial, anti-inflammatory and antineoplastic) of the synthesised compounds has been carried out on the basis Prediction of activity spectra for substances (PASS). Interestingly, PASS prediction of the compounds (5a-f) & (6a-f) showed that none of the synthesised compounds act as antineoplastic agents compared to standard CAI an potent antineoplastic agent (Pa Table 1 ).

Benzofuran-selenadiazole hybrids as novel α-glucosidase and cyclooxygenase-2 inhibitors with antioxidant and cytotoxic properties.

Series of 2-arylbenzofuran-1,2,3-selenodiazole hybrids were prepared via multiple reactions and then evaluated in vitro through enzymatic assay for inhibitory effect against α-glucosidase and cyclooxygenase-2 (COX-2) activities including antioxidant activity. The presence of 1,2,3-selenodiazole moiety resulted in increased inhibitory effect for compounds 4a-f against α-glucosidase and COX-2 activities, and increased free radical scavenging activity. 6-Acetoxy-2-phenyl-5-(1,2,3-selenadiazol-4-yl)benzofuran (4a) and its 2-(4-methoxyphenyl) substituted derivative (4f) were, in turn, screened for antiproliferation against the breast MCF-7 cancer cell line and for cytotoxicity on the human embryonic kidney derived Hek293-T cells. A cell-based antioxidant activity assay involving lipopolysaccharide induced reactive oxygen species production in these cells was performed. Molecular docking has also been performed on these two compounds to predict protein-ligand interactions against α-glucosidase and COX-2.

Synthesis, Characterization and in vitro Antimicrobial Screening of Some Novel Series of 2-Azetidinone Derivatives Integrated with Quinoline, Pyrazole and Benzofuran Moieties

A series of 5-(benzofuran-2-yl)-N-(3-chloro-4-(2-(p-tolyloxy) substituted quinolin-3-yl)-2-oxoazetidin-1-yl)-1-phenyl-1H-pyrazole-3-carboxamide derivatives (4a-f) were synthesized with excellent yields by cyclocondensation reaction of 5-(benzofuran-2-yl)-N′-(2-(p-tolyloxy) substituted quinolin-3-yl)methylene)-1-phenyl-1H-pyrazole-3-carbohydrazide (3a-f) with chloroacetyl chloride in presence of triethylamine in DMF. One pot condensation of 5-(benzofuran-2-yl)-1-phenyl-1H-pyrazole-3-carbohydrazide (1) with 2-(p-tolyloxy) substituted quinoline-3-carbaldehyde (2a-f) in ethanol solvent in presence of catalytic amount of acetic acid gave intermediate compounds (3a-f). The structures of newly synthesized compounds have been substantiated through elemental analysis and spectral studies viz. 1H NMR, 13C NMR, IR and mass spectra. All the synthesized compounds were screened for their in vitro antibacterial activity against pathogenic bacteria such as S. aureus and E. coli at different concentrations.

Synthesis, Characterization and Biological Evaluation of Some Novel Regioisomers of Ropivacaine Analogues: An Anaesthetic Drug

A series of ropivacaine analogues were synthesized by altering the methyl group substituent in the aromatic ring. The synthesized compounds (2a-f and 3a-f) were characterized by using IR, NMR and HRMS analysis and then compounds 3a-3f were screened in vitro anticancer (MTT assay) activity against breast cancer cell line (MCF-7), antibacterial and antioxidant (DPPH scavenging assay) studies. The biological studies revealed that the compounds 3c and 3f have shown a good inhibitory activity against MCF-7 cell line. Compounds 3e, 3b, 3c and 3f showed moderate antioxidant activity. There was no inhibition observed against both Gram-positive and Gram-negative bacteria.

Synthesis and Characterization of Novel 1,3,5-Thiadiazine Derivatives Integrated with Quinoline Moiety as Potent Antimicrobial Agents

An expeditious synthesis of series of novel 1,3,5-thiadiazine (5a-f) and (6a-f) derivatives have been described. These compounds were synthesized by reaction of 1-(N-((6-methyl-2-(p-tolyloxy)quinoline- 3-yl)methylene)carbamimidoyl)-3-arylthiourea (3a-b) derivatives with N-aryl isocyanodichloride (4a-c) in chloroform followed by basification with dilute NH4OH to give the target compounds 5a-f; which were acetylated further to afford six novel 1,3,5-thiadiazin-3-(6H)-yl)ethanone (6a-f) derivatives. Synthesis of intermediate compounds 3a-b was obtained by reacting 6-methyl-2-(p-tolyloxy)quinoline-3- carbaldehyde (2a) and 1-carbamimidoyl-3-aryllthiourea (1a-b) in chloroform. Structures of compounds 5a-f and 6a-f were established by FTIR, 1H & 13C NMR, mass spectra and further supported by elemental analysis. All synthesized compounds were investigated for their in vitro antimicrobial screening against a panel of pathogenic microorganism comprising S. aureus as Gram positive while E. coli, P. vulgaris, S. typhi as Gram-negative bacterial strains.

Inhibitory effects of triarylpyrazole derivatives on LPS-induced nitric oxide and PGE2 productions in murine RAW 264.7 macrophages

In this article, a series of 22 triarylpyrazole derivatives were evaluated for in vitro antiinflammatory activity as inhibitors of nitric oxide (NO) and prostaglandin E2 (PGE2) release induced by lipopolysaccharide (LPS) in murine RAW 264.7 macrophages. The synthesized compounds 1a-h, 2a-f and 3a-h were first examined for their cytotoxicity for determination of the non-toxic concentration for antiinflammatory screening, so that the inhibitory effects against NO and PGE2 production were not caused by non-specific cytotoxicity. Compounds 1h and 2f were the most active PGE2 inhibitors with IC50 values of 2.94 μM and 4.21 μM, respectively. Western blotting and cell-free COX-2 screening revealed that their effects were due to inhibition of COX-2 protein expression. Moreover, compound 1h exerted strong inhibitory effect on the expression of COX-2 mRNA in LPS-induced murine RAW 264.7 macrophages.

Synthesis, in-Vitro Cytotoxicity and Antimicrobial Evaluations of Some Novel Thiazole Based Heterocycles.

Condensation of rhodanine (1) with pyrazol-3(2H)-one derivatives (2a-f) gave 5-substituted-2-thioxo-1,3-thiazolidin-4-one derivatives (3a-f). Reaction of compound (1) with 2-arylmethylidene-malononitrile (4a-d) yielded the unexpected derivatives (5a-d). The latter compounds were subjected to cyclization reactions with malononitrile under different basic conditions, hydroxylamine hydrochloride and/or thiourea to furnish the fused thiazole derivatives (6a-d) and (8-10a-d). Coupling of (1) with diazotized aromatic amines (11a-c) in pyridine afforded the arylhydrazones (12a-c). Fusion of latter compounds with malononitrile afforded the thiazolopyridazine derivatives (13a-c). The structures of the newly synthesized compounds were elucidated via spectral data and elemental analyses. The in-vitro cytotoxic activity of compounds (3a-f) against the cell line MCF-7 was evaluated. Also, the synthesized products were investigated for their antibacterial and antifungal activities against six standard organisms including the G+ bacteria, Staphylococcus aureus and Bacillus subtilis, G- bacteria, Escherichia coli and Proteus vulgaris in addition to fungi, Candida albicans and Aspergillus flavus.

In-vitro Anti-cancer assay and apoptotic cell pathway of newly synthesized benzoxazole-N-heterocyclic hybrids as potent tyrosine kinase inhibitors.

A series of benzoxazole-N-heterocyclic hybrids have been synthesized by a one-pot strategy. Molecular docking study revealed that such compounds have the ability to inhibit enzyme protein tyrosine kinase. The findings of this work have been the successful synthesis of benzoxazole scaffolds, featuring hybrids of benzoxazole with quinoline and quinoxaline respectively. The molecular docking studies have showed these compounds to be inhibitors of tyrosine kinase enzyme which triggers growth of cancer cells. The cytotoxicity study of compounds 4a-f showed better potency against breast cancer cell lines MCF-7 and MDA-MB-231 in contrast to oral and lung cancer cell lines KB and A549. The tyrosine kinase activity was measured using Universal Tyrosine Kinase Assay kit using horseradish peroxide (HRP)-conjugated anti-phosphotyrosine kinase solution as a substrate. The compounds 4c exhibited maximum inhibition in the activity of enzyme tyrosine kinase with IC50 value 0.10 ± 0.16 µM, than other compounds which were studied and thus proved to be inhibitors of enzyme tyrosine kinase. The selective index of all four compounds was found out to be greater than two, indicating the non-toxic behaviour, i.e. good anti-cancer activity. Further, fluorescence microscopic study helped to characterize the mode of cell death, which was found to be late apoptosis as indicated by the orange fluorescence. The SAR analysis has also been carried out.

Synthesis and anticancer potential of aminomethyl derivatives of methyl-substituted asymmetrical curcumin mono-carbonyl

A series of new aminomethyl derivatives of methyl-substituted asymmetrical curcumin mono-carbonyl was synthesized and evaluated for their anticancer potential by means of cytotoxicity and selectivity determination against Hela, MCF-7, WiDr, A549, PLC/PRF/5, and Chang Liver cells lines using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) proliferation assay. The results showed that all the synthesized compounds (3a-f) exhibited high cytotoxic against WiDr cells lines, but only 3a-e had high cytotoxic against MCF-7 cells lines, and only 3b showed high cytotoxic against HeLa, A549 and PLC/PRF/5 cell lines. However, 3b and 3c exhibited high cytotoxic against Chang Liver (normal liver) cells lines. Further evaluations showed that compound 3d, 3e, and 3f exhibited a potent and selective cytotoxic agent (IC50 = 5.70, 5.55, and 2.97 µM) against WiDr (colorectal carcinoma) cells lines with selectivity index (SI) = 4.43, 2.69, and 2.04, respectively. The compounds performed better cytotoxic activity than 5-fluorouracil and curcumin (IC50 = 8.29 and >100 µM; and SI = 1.28 and < 1). So, compound 3d, 3e, and 3f were potential as an anticancer agent for colorectal carcinoma and should be further studied for investigating their mechanism of action and their effectivity in preclinical studies using an animal model.

Synthesis and Biological Evaluation of Benzothiazole-piperazinesulfonamide Conjugates and Their Antibacterial and Antiacetylcholinesterase Activity

Two series of N-2-benzothiazolyl-4-(arylsulfonyl)-1-piperazineacetamides/propanamides were synthesized from substituted 2-aminobenzothiazoles and were assayed for their in vitro antimicrobial activities against a panel of different pathogenic bacterial strains such as Micrococcus luteus, S. aureus, S. aureus MLS-16, B. subtilis, Escherichia coli, Pseudomonas aeruginosa, Klebsiella planticola and Candida albicans. Among the synthesized compounds 5e,f,g and 6g,h,i showed promising antifungal activity against C. albicans as compared to the reference drug, miconazole. Further, compounds 6g,h,i showed broad spectrum antibacterial activity against all the tested bacterial strains, while the compounds 6a-f,j-m showed significant antibacterial activity against all the tested bacterial strains as compared to the reference drug, ciprofloxacin. In addition, the target compounds were evaluated for their acetylcholinesterase (AChE) inhibitory activity, and, among the tested, compounds 5j,k,l and 6i showed promising AChE inhibitory activity.