Diaryloxy methano phenanthrenes: a new class of antituberculosis agents.
A new series of diaryloxy methano phenanthrenes were prepared through tertiary-aminoalkylations of [(methoxy-phenyl)-phenanthren-9-yl-methyl]-phenols obtained from Friedel-Crafts alkylations on (methoxy-phenyl)-phenanthren-9-yl-methanols. These series of compounds were evaluated against Mycobacterium tuberculosis H37Rv and showed the desired activity in the range of 6.25 microg/mL in vitro. One of the compound 12j protects the mice from the challenge of M. tuberculosis in vivo, as 30% of the mice were survived at treatment of 50 mg/kg body weight.
Panda
Gautam
G
Medicinal and Process Chemistry Division, Central Drug Research Institute, Lucknow 226001, UP, India. gautam_panda@lycos.com
Shagufta
Mishra
Jitendra Kumar
JK
Chaturvedi
Vinita
V
Srivastava
Anil K
AK
Srivastava
Ranjana
R
Srivastava
Brahm S
BS
D000818:Animals; D000995:Antitubercular Agents / Q000138:chemical synthesis* / Q000494:pharmacology* / Q000627:therapeutic use; D005260:Female; D051379:Mice; D009169:Mycobacterium tuberculosis / Q000187:drug effects*; D010616:Phenanthrenes / Q000138:chemical synthesis* / Q000494:pharmacology* / Q000627:therapeutic use; D014376:Tuberculosis / Q000188:drug therapy
D000995:Antitubercular Agents; D010616:Phenanthrenes