Background: Postprandial hyperglycemia can be reduced by inhibiting major carbohydrate hydrolyzing enzymes, such as α-glucosidase and α-amylase which is an effective approach in both preventing and treating diabetes. Objective: The aim of this study was to synthesize a series of 2,4-dichloro-5-[(N-aryl/alkyl)sulfamoyl] benzoic acid derivatives and evaluate α-glucosidase and α-amylase inhibitory activity along with molecular docking and in silico ADMET property analysis. Method: Chlorosulfonation of 2,4-dichloro benzoic acid followed by reaction with corresponding anilines/amines yielded 2,4-dichloro-5-[(N-aryl/alkyl)sulfamoyl]benzoic acid derivatives. For evaluating their antidiabetic potential α-glucosidase and α-amylase inhibitory assays were carried out. In silico molecular docking studies of these compounds were performed with respect to these enzymes and a computational study was also carried out to predict the drug-likeness and ADMET properties of the title compounds. Results: Compound 3c (2,4-dichloro-5-[(2-nitrophenyl)sulfamoyl]benzoic acid) was found to be highly active having 3 fold inhibitory potential against α-amylase and 5 times inhibitory activity against α-glucosidase in comparison to standard drug acarbose. Conclusion: Most of the synthesized compounds were highly potent or equipotent to standard drug acarbose for inhibitory potential against α-glucosidase and α-amylase enzyme and hence this may indicate their antidiabetic activity. The docking study revealed that these compounds interact with active site of enzyme through hydrogen bonding and different pi interactions.

Background: Heterocyclic compounds are an integral part of the chemical and life sciences and constitute a considerable quantum of the modern research that is being currently pursued throughout the world. Methods: This review was prepared by collecting the available literature reports on various databases and an extract was prepared for each report after thorough study and compiling the recent literature reports on heterocyclic amides from 2007 to 2018. Results: This review summarizes the bio-potential of heterocyclic amides as antimicrobial, anticancer, anti-tubercular and antimalarial agents which would be very promising in the field of medicinal chemistry. Conclusion: A wide variety of heterocyclic amides have already been reported and some are currently being used as active medicaments for the treatment of disease. Still, the research groups are focusing on the development of newer heterocyclic amide derivatives with better efficacy, potency and lesser side effects. This area has got the tremendous potential to come up with new chemical entities of medicinal importance.

A series of 2-chloro-5-[(4-chlorophenyl)sulfamoyl]-N-(alkyl/aryl)-4-nitrobenzamide derivatives (5a-5v) has been synthesized and confirmed by physicochemical(R f , melting point) and spectral means (IR, 1 HNMR, 13 CNMR). The results of in vitro antidiabetic study against α-glucosidase indicated that compound 5o bearing 2-CH 3-5-NO 2 substituent on phenyl ring was found to be the most active compound against both enzymes. The electron donating (CH 3) group and electron withdrawing (NO 2) group on a phenyl ring highly favoured the inhibitory activity against these enzymes. The docking simulations study revealed that these synthesized compounds displayed hydrogen bonding, electrostatic and hydrophobic interactions with active site residues. The structure activity relationship studies of these compounds were also corroborated with the help of molecular modeling studies. Molecular dynamic simulations have been done for top most active compound for validating its α-glucosidase and α-amylase inhibitory potential, RMSD analysis of ligand protein complex suggested the stability of top most active compound 5o in binding site of target proteins. In silico ADMET results showed that synthesized compounds were found to have negligible toxicity, good solubility and absorption profile as the synthesized compounds fulfilled Lipinski's rule of 5 and Veber's rule.

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A series of new quinoline pyrazolyl‐chalcone hybrids (4 a–4 s) was obtained from 4‐acetyl‐5‐methylquinolylpyrazole and aromatic aldehydes and the structure of these hybrids were established with the help of FTIR, 1D NMR (1H and 13C), 2D NMR and HRMS data. The anticancer potential of selected quinoline pyrazolyl‐chalcone hybrids was evaluated against colon cancer (HT‐29, HCT‐116), lung cancer (A549), and prostate cancer (PC‐3) cell lines. (E)‐1‐(5‐Methyl‐1‐(4‐methylquinolin‐2‐yl)‐1H‐pyrazol‐4‐yl)‐3‐(2,4,6‐trimethoxyphenyl)prop‐2‐en‐1‐one (4 j) displayed good cytotoxicity with IC50 values of 5.4, 3.2 and 2.8 μM against HT‐29, A549, and PC‐3 cancer cell lines, respectively. The antimicrobial potential of quinoline pyrazolyl‐chalcone hybrids was tested against three bacterial strains (B. subtilis, S. aureus and E. coli) and two fungal strains (A. niger and C. albicans). (E)‐1‐(5‐Methyl‐1‐(4‐methylquinolin‐2‐yl)‐1H‐pyrazol‐4‐yl)‐3‐(3‐nitrophenyl)prop‐2‐en‐1‐one (4 r) exhibited significant activity against Gram positive bacteria (B. subtilis and S. aureus) and fungal strains with MIC value of 15.6 μM. Molecular docking analysis was conducted to determine the binding interactions of quinoline pyrazolyl‐chalcone hybrids with their respective biochemical targets viz. Epidermal growth factor receptor tyrosine kinase (EGFR), Thymidylate kinase (TMK) and C. albicans N‐myristoyltransferase.