Facile synthesis and in silico studies of benzothiazole-linked hydroxypyrazolones targeting α-amylase and α-glucosidase.

Aim: The objective of the present investigation was to design and synthesize new heterocyclic hybrids comprising benzothiazole and indenopyrazolone pharmacophoric units in a single molecular framework targeting α-amylase and α-glucosidase enzymatic inhibition. Materials & methods: 20 new benzothiazole-appended indenopyrazoles, 3a-t, were synthesized in good yields under environment-friendly conditions via cycloaddition reaction, and assessed for antidiabetic activity against α-amylase and α-glucosidase, using acarbose as the standard reference. Results: Among all the hydroxypyrazolones, 3p and 3r showed the best inhibition against α-amylase and α-glucosidase, which finds support from molecular docking and dynamic studies. Conclusion: Compounds 3p and 3r have been identified as promising antidiabetic agents against α-amylase and α-glucosidase and could be considered valuable leads for further optimization of antidiabetic agents.

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Convenient synthesis of benzothiazinoisoindol-11-ones and benzoindenothiazin-11-ones, and antimicrobial testing thereof.

Benzo[5,6][1,4]thiazino[3,4-a]isoindol-11-ones 5a-t and benzo[b]indeno[1,2-e][1,4]thiazin-11(10aH)-ones 6a-e were synthesized conveniently via cyclocondensation of 2-bromo-2-(2/3-substitutedphenyl)-1H-indene-1,3(2H)-diones and 2-aminobenzenethiols in freshly dried ethanol with 70-85% yields. The synthesized derivatives were well characterized by employing different spectral techniques (FTIR, 1H & 13C NMR and HRMS) and X-ray crystallographic analysis. Further, all the reported compounds were tested for their antibacterial and antifungal activities using Ciprofloxacin and Fluconazole as standard drugs, respectively. The results of antimicrobial evaluation revealed that compounds 5o and 5t displayed remarkable inhibitory activity against B. subtilis, S. aureus, P. aeruginosa and A. niger with MIC values in the range of 0.0141-0.0283 µmol/mL, whereas 5j was found active against E. coli and C. albicans with MIC values of 0.0286 µmol/mL and 0.0143 µmol/mL, respectively. Additionally, among all the benzo[b]indeno[1,2-e][1,4]thiazin-11(10aH)-ones, 6c exhibited excellent inhibition against all the tested bacterial and fungal strains with MIC values ranging from 0.0143 to 0.1145 µmol/mL. Structure activity relationships were also established for all the tested benzo[5,6][1,4]thiazino[3,4-a]isoindol-11-ones 5a-t.

Recent Progress in Anticancer Agents Incorporating Pyrazole Scaffold.

The search for new anticancer agents is considered a dynamic field of medicinal chemistry. In recent years, the synthesis of compounds with anticancer potential has increased and a large number of structurally varied compounds displaying potent anticancer activities have been published. Pyrazole is an important biologically active scaffold that possesses nearly all types of biological activities. The aim of this review is to collate literature work reported by researchers to provide an overview on in vivo and in vitro anticancer activities of pyrazole based derivatives among the diverse biological activities displayed by them and also to present recent efforts made on this heterocyclic moiety regarding anticancer activities. This review has been driven by the increasing number of publications on this issue, which have been reported in the literature since the end of the 20th century (from 1995-to date).