Pratima P. Mogle

Antidiabetic and allied biochemical roles of new chromeno-pyrano pyrimidine compounds: synthesis, in vitro and in silico analysis

Diabetes is embracing the human population in logarithmic fashion both in developed as well as developing countries. Aldose reductase is one of the important enzymes of polyol pathway of sugar metabolism in humans. Aldose reductase inhibition has been identified as one of the important target for developing novel antidiabetic agents. In this report, we present an effective synthesis of 7-(substituted phenyl) chromeno-pyrano [2,3-d]pyrimidine-6,8,10-(7H,9H,11H)-trione derivatives and demonstrate their aldose reductase inhibition potential in order to identify novel schemes for finding putative aldose reductase inhibitors. The antioxidant activity of all the synthesized compounds with negligible toxicity demonstrates the biological efficacy of the synthesized compounds. The in silico molecular docking and structural analysis of docked poses conducted in the current investigation sheds light on the structural rationale of the observed aldose reductase inhibition by all the newly synthesized compounds.

Synthesis and molecular docking studies of a new series of bipyrazol-yl-thiazol-ylidene-hydrazinecarbothioamide derivatives as potential antitubercular agents

Various substituted 2-(2-(5-(3/4-substituted phenyl)-4-hydroxy-3′-(3/4-substituted phenyl)-1′-phenyl-1H,1′H-[3,4′-bipyrazol]-1-yl)thiazol-4(5H)ylidene) hydrazinecarbothioamide derivatives have been synthesized in good yields by an efficient method. The synthesized compounds (6a–r) were evaluated for their in vitro antitubercular activity against the Mycobacterium tuberculosis (MTCC 300) strain. Compounds 6o (MIC-3.90 μg mL−1), 6p (MIC-3.90 μg mL−1), and 6q (MIC-7.81 μg mL−1), exhibited significant activity against Mycobacterium tuberculosis. The molecular docking studies revealed an interesting binding profile with very high receptor affinity.

Bleaching earth clay pH 12.5/PEG-400 catalytic system for synthesis of some novel α, β-unsaturated ketones (chalcones)

We report bleaching earth clay pH 12.5/PEG-400 as an efficient catalytic system for preparation of α,β-unsaturated ketones (chalcones). The method presents one or more advantages over existing methodologies such as shorter reaction time, excellent yield, and low cost. All synthesized products were characterized by spectroscopic and analytical measurements.

A rapid, mild, and efficient method for C-5 iodination/thiocyanation of 2-aminothiazoles

GRAPHICAL ABSTRACT ABSTRACT An efficient, green, rapid multitasking protocol for the selective C-5 substitution of 2-aminothiazole using iodic acid and aqueous PEG-400 was developed. The method found suitable for C-5 substitution i.e. iodination and thiocyanation of 2-amino thiazole using iodine and ammonium thiocyanate respectively. Iodic acid was found to be a good oxidant and aqueous PEG-400 as green reaction solvent.

Bleaching earth clay (pH 12.5)/PEG-400: an efficient recyclable catalytic system for synthesis of 5,6,7,8-tetrahydroquinoline-3-carbonitrile derivatives

A green, efficient, and simple method for synthesis of 5,6,7,8-tetrahydroquinoline-3-carbonitrile derivatives via one-pot three-component condensation of 2,6-bis(substituted benzylidene)cyclohexanone, arylamines/substituted 2-aminothiazoles, and malononitrile in the presence of bleaching earth clay pH 12.5 (basic catalyst) as a recyclable and green catalyst in PEG-400 is described. Catalyst recyclability, good to excellent product yield, shorter reaction time, and avoidance of hazardous reagents are the main advantages of this methodology.