Discovery of novel antitubercular 2,10-dihydro-4aH-chromeno[3,2-c]pyridin-3-yl derivatives

Add time:08/09/2019    Source:sciencedirect.com

Twenty two novel 2,10-dihydro-4aH-chromeno[3,2-c]pyridin-3-yl derivatives were synthesized by reacting 3-formyl chromone, (sub)-2-amino pyridines, N1-(prop-2-ynyl)arylamides in the presence of indium triflate. The compounds were evaluated their preliminary in-vitro and in-vivo activity against Mycobacterium tuberculosis H37Rv (MTB) and multi-drug resistant M. tuberculosis (MDR-TB). Among them N-[(4aS)-2-(3-methyl-2-pyridinyl)-10-oxo-2,10-dihydro-4aH-chromeno[3,2-c]pyridin-3-yl]methyl-4-ethylbenzenecarboxamide 4d was found to be the most active compound in-vitro with MIC's of 0.22 and 0.07 μg/mL against MTB and MDR-TB respectively. In the in-vivo animal model 4d decreased the bacterial load in lung and spleen tissues with 1.11 and 2.94-log10 protections respectively at 25 mg/kg body weight dose.

We also recommend Trading Suppliers and Manufacturers of N-(4-FORMYL-PYRIDIN-3-YL)-2,2-DIMETHYL-PROPIONAMIDE (cas 127446-35-9). Pls Click Website Link as below: cas 127446-35-9 suppliers

Prev:Spectral, structural, solvatochromism, biological and computational investigation of some new azo–azomethines containing N-alkylpyridinium salts
Next:Survey reactivity of some N-aryl formamides with pentafluoropyridine)