Whole-Genome Sequence of Streptomyces kaniharaensis Shomura and Niida SF-557.

Streptomyces kaniharaensis is a Gram-positive bacterium that produces formycin A 5'-phosphate, a C nucleotide with antimicrobial and anticancer activity. Here, we report the sequencing, assembly, and annotation of the draft genome sequence of Streptomyces kaniharaensis Shomura and Niida

Microwave-Assisted, Metal-Free, Base-Mediated C-N Bond Formation/Cleavage: Synthesis of Benzimidazo[1,2-a]quinazoline Derivatives

© 2016 American Chemical Society. A novel, rapid, and efficient microwave-assisted, metal-free, base-mediated approach has been developed for the construction of benzimidazo[1,2-a]quinazolines from readily available building blocks. This synthetic strategy affords a diverse range of benzimidazo[1,2-a]quinazoline derivatives in moderate to good yields.status: publishe

Synthesis and anti-inflammatory activity evaluation of novel triazolyl-isatin hybrids

New isatin-triazole based hybrids have been synthesized and evaluated for their inhibitory activity of TNF-α induced expression of Intercellular Adhesion Molecule-1 (ICAM-1) on the surface of human endothelial cells. Structure-activity relationship (SAR) studies revealed that the presence of the electron-attracting bromo substituent at position-5 of the isatin moiety played an important role in enhancing the anti-inflammatory potential of the synthesized compounds. Z-1-[3-(1H-1,2,4-Triazol-1-yl)propyl]-5-bromo-3-[2-(4-methoxyphenyl)hydrazono]indolin-2-one (19) with an IC50 = 20 μM and 89% ICAM-1 inhibition with MTD at 200 μM was found to be the most potent of all the synthesized derivatives. Introduction of 1,2,4-triazole ring and electron-donating methoxy group on the phenylhydrazone moiety resulted in four-fold increase of the anti-inflammatory activity.status: publishe