Design, synthesis, α-amylase and glucose diffusion inhibition, and molecular docking studies of new indenopyrazolones bearing benzothiazole derivatives.

An eco-friendly facile synthesis of a series of twenty 1-(4/6-substitutedbenzo[d]thiazol-2-yl)-3-(phenyl/substitutedphenyl)indeno[1,2-c]pyrazol-4(1H)-ones 7a-t was achieved by the reaction of 2-(benzoyl/substitutedbenzoyl)-(1H)-indene-1,3(2H)-dione 3a-t and 2-hydrazinyl-4/6-substitutedbenzo[d]thiazole 6a-t in presence of freshly dried ethanol and glacial acetic acid under reflux conditions in good yields. The newly synthesized derivatives were well characterized using different physical and spectral techniques (FTIR, H NMR & C NMR, and HRMS). All the compounds were subjected to assess their in vitro α-amylase and glucose diffusion inhibitory activity.

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.

Synthesis, Type II diabetes inhibitory activity, antimicrobial evaluation and docking studies of indeno[1,2-]pyrazol-4(1)-ones.

We report a convenient and efficient synthesis of indeno[1,2-]pyrazol-4(1)-ones () by the reaction of a variety of 2-acyl-(1)-indene-1,3(2)-diones () and 2-hydrazinylbenzo[]thiazole/2-hydrazinyl-6-substitutedbenzo[]thiazoles () in the presence of glacial acetic acid in good yields. The structure of the compounds thus prepared were confirmed by analytical and spectral (FT-IR, H NMR, C NMR, and HRMS) techniques. All the synthesized indeno[1,2-]pyrazol-4(1)-ones () were assayed for their in vitro Type II diabetes inhibitory activity by using Acarbose as standard drug and in vitro antimicrobial activity utilizing Streptomycin and Fluconazole as reference drugs.

Convenient and efficient synthesis of novel 11-benzo[5,6][1,4]thiazino[3,4-]isoindol-11-ones derived from 2-bromo-(2/3-substitutedphenyl)-1-indene-1,3(2)-diones.

An unprecedented formation of 11-benzo[5,6][1,4]thiazino[3,4-]isoindol-11-ones through a one-step reaction of differently substituted 2-aminobenzenethiols and 2-bromo-(2/3-substitutedphenyl)-1-indene-1,3(2)-diones in freshly dried ethanol under reflux conditions has been investigated. This unique transformation probably occurs through an initial nucleophilic substitution followed by ring opening and subsequent intramolecular cyclization. The structures of all the synthesized benzo[1,4]thiazino isoindolinones were established by FTIR, H NMR, C NMR, HRMS, and X-ray crystallographic analysis.