Enoxacin-based derivatives: antimicrobial and antibiofilm agent: a biology-oriented drug synthesis (BIODS) approach.

To find alternative molecules against ,  and methicillin-resistant , new enoxacin derivatives were synthesized and screened. All derivatives exhibited promising antibacterial activities as compared to standard enoxacin (2 μg/ml) and standard cefixime (82 μg/ml). Compounds , and significantly downregulated the gene expression of biofilm-forming genes.

New isatin derivative inhibits neurodegeneration by restoring insulin signaling in brain.

Diabetes is associated with neurodegeneration. Glycation ensues in diabetes and glycated proteins cause insulin resistance in brain resulting in amyloid plaques and NFTs. Also glycation enhances gliosis by promoting neuroinflammation.

Synthesis, structure-activity relationships studies of benzoxazinone derivatives as α-chymotrypsin inhibitors.

A series of benzoxazinones 1-28 were synthesized via reaction of anthranilic acid with various substituted benzoyl chlorides in the presence of triethylamine in chloroform. Compounds 1-18 showed a good inhibition of α-chymotrypsin with IC±SEM values between 6.5 and 341.

Synthesis, spectroscopic characterization and antimicrobial activities of benzoxazolone derivatives.

Unlabelled: : Background: Pathogenic microbial diseases are now the key virulence in our daily life. Significant research has been carried out in order to trigger the bacterial infections. Amongst the organic molecules, oxazolone and derivatives were found to have excellent bioactivities including antimicrobial activities.

A new glycotoxins inhibitor attenuates insulin resistance in liver and fat cells.

Glycotoxins/Advanced glycation end products (AGEs) have implications in development of diabetes and related diseases. In the present study we deciphered the mechanisms of action of URM-II-81, a new derivative of isatin, in alleviation of insulin resistance in human hepatocytes and murine adipocytes. URM-II-81 reduced AGEs formation and receptor for advanced glycation end products (RAGE) expression in both cell types.

A bis-Schiff base of isatin improves methylglyoxal mediated insulin resistance in skeletal muscle cells.

Methylglyoxal (MGO) is a highly reactive advanced glycation end products (AGEs) precursor and its abnormal accumulation causes damage to various tissues and organs. In our previous study, we synthesized a novel MGO inhibitor, MK-I-81, a bis-Schiff base derivative of isatin. In this study we demonstrate the mechanism of action of MK-I-81, on insulin resistance in skeletal muscle cells.

Evaluation of the thiazole Schiff bases as β-glucuronidase inhibitors and their in silico studies.

Twenty eight (28) derivatives 2-29 were synthesized and four analogs were found to exhibit single-digit IC(50) values as β-glucuronidase inhibitors. Molecular modeling indicates that three factors: substituent R, lone pair on the nitrogen of azomethine part, and the interactions made by the main skeleton of the molecule, determined the enzyme inhibitory potential of these compounds. The planar conformation of the molecules allows them to fit deep inside the pocket while blocking the entry of other physiological substrates seems to play an important role in their activity.