Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 45, Issue 2, Pages 682-688Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2009.11.011
Keywords
Friedlander annulation; Thienoquinoline; 5-Aryldihydro-3(2H)-thiophenone; 2-Aminobenzophenone; Antimycobacterial activity; Mycobacterium tuberculosis; Multi-drug resistant Mycobacterium tuberculosis
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Funding
- Department of Science and Technology, New Delhi [SR/S1/OC-70/2006]
- IRHPA
- FIST
- University Grants Commission, New Delhi
- DRS
- ASIST
- [36-155/2008(SR)]
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A series of 2,9-diaryl-2,3-dihydrothieno[3,2-b]quinolines have been synthesized regioselectively by Friedlander annulation of 5-aryldihydro-3(2H)-thiophenones and 2-aminobenzophenones in the presence of trifluoroacetic acid in good yields under microwave irradiation at 100 degrees C. The 2,9-diatyl-2,3-dihydrothieno[3,2-b]quinolines were screened for in vitro antimycobacterial activity against Mycobacterium tuberculosis H37Rv (MTB) and multi-drug resistant M. tuberculosis (MDR-TB). Among the 17 compounds screened, 7-chloro-2-(2,4-dichlorophenyl)-9-phenyl-2,3-dihydrothieno-[3,2-b]quinoline and 7-chloro-2-(3-nitrophenyl)-9-phenyl-2,3-dihydrothieno[3,2-b]quinoline display maximum activity with MIC of 0.90 and 0.95 mu M against MTB and MDR-TB respectively. (C) 2009 Elsevier Masson SAS. Ail rights reserved.
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