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Discovery of novel antitubercular 2,10-dihydro-4aH-chromeno[3,2-c]pyridin-3-yl derivatives by Dharmarajan Sriram; Perumal Yogeeswari; Murugesan Dinakaran; Debjani Banerjee; Pritesh Bhat; Sunil Gadhwal is a Chemistry article available to read on EtoBox.
What is Discovery of novel antitubercular 2,10-dihydro-4aH-chromeno[3,2-c]pyridin-3-yl derivatives about?
a b s t r a c t 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 mg/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.
Who reads Discovery of novel antitubercular 2,10-dihydro-4aH-chromeno[3,2-c]pyridin-3-yl derivatives?
It is typically read by researchers, students, and practitioners in Chemistry.
- Author
- Dharmarajan Sriram; Perumal Yogeeswari; Murugesan Dinakaran; Debjani Banerjee; Pritesh Bhat; Sunil Gadhwal
- Publisher
- Elsevier Science; Elsevier ; Elsevier BV (ISSN 0223-5234)
- Published
- 2010
- Language
- EN
- Field
- Chemistry (Physical Sciences)