Bitopic fluorescent antagonists of the A adenosine receptor based on pyrazolo[4,3-][1,2,4]triazolo[1,5-]pyrimidin-5-amine functionalized congeners.

A pyrazolo[4,3-][1,2,4]triazolo[1,5-]pyrimidin-5-amine antagonist of the A adenosine receptor (AR) was functionalized as amine congeners, fluorescent conjugates and a sulfonate, and the AAR binding modes were predicted computationally. The optimal -butyl spacer was incorporated into the following AAR-selective (, nM) conjugates: BODIPY630/650 derivative (MRS7396, 24.6) and AlexaFluor488 derivative (MRS7416, 30.

Hydroxamates of para-aminobenzoic acid as selective inhibitors of HDAC8.

A series of hydroxamates (4a-4l) were prepared from p-aminobenzoic acid to inhibit HDAC8. The idea is to substitute rigid aromatic ring in place of less rigid piperazine ring of hydroxamates reported earlier by our group. It is expected to increase potency retaining the selectivity.

Anti-inflammatory potential of thienopyridines as possible alternative to NSAIDs.

The present study was designed to evaluate the anti-inflammatory and antiarthritic activity of the new synthetic thienopyridine analogs. The anti-inflammatory activity of thienopyridines was assayed by using carrageenan; dextran and arachidonic acid induced paw edema models (acute), cotton pellet granuloma model (Sub acute) and Freund's complete adjuvant induced arthritis (chronic) in experimental rats. The compounds BN-4, BN-14 and BN-16 have shown significant inhibition of edema in carrageenan and arachidonic acid induced paw edema model at a dose of 100mg/kg compared to the dextran induced paw edema model and also showed significant inhibition in granuloma tissue formation and Freund's complete adjuvant induced arthritis in experimental rats.

Synthesis, antimicrobial and anticancer activity of new thiosemicarbazone derivatives.

Thiosemicarbazones of p-aminobenzoic acid (PABA) were synthesized and tested for their antimicrobial and anticancer activity. Hydroxamate derivatives 4a-4l were found to have better antimicrobial and anticancer activity than their acid counterpart. Compound 4d was found to have good antimicrobial activity against Escherichia coli, Klebsiella pneumoniae, Staphylococcus aureus, Vibrio cholerae, and Bacillus subtilis with IC(50) value of about 1 µM.

Synthesis, antimicrobial evaluation, and docking studies of novel 4-substituted quinazoline derivatives as DNA-gyrase inhibitors.

Quinazoline derivatives are reported to have anti-inflammatory, analgesic, antibacterial, and anticancer activities. The incorporation of "OCH₂CONH₂" (oxymethylcarbamide) at 4th position of the quinazoline ring was found to influence the biological activities of the molecules. With this rationale, some new oxadiazolyl methyloxy quinazolines, pyrazolyl acetoxy methyl quinazolines, triazolylmethyloxy quinazolines were synthesized from anthranilic acid through quinazolyl oxyacetylhydrazide intermediates.