Novel fluoroquinolones: design, synthesis, and in vivo activity in mice against Mycobacterium tuberculosis H37Rv.
Novel 6,8-difluoro-1-alkyl-5-amino-1,4-dihydro-4-oxo-7-{4-substituted piperazin-1-yl}-quinoline-3-carboxylic acids, with the substituents at 4th position of piperazine being -[2(pyridine-4-carbonyl) hydrazono]propyl and -2 [(pyrazine-2-carbonyl) amino] ethyl, were synthesized and evaluated in vivo against Mycobacterium tuberculosis H(37)Rv in Swiss albino mice. Test compounds exhibited activity comparable to that of sparfloxacin (survival rate, reduction of splenomegaly and reduced tubercular lesions) at a dose of 200 mg/kg.
Shindikar
Anand V
AV
Department of Pharmaceutical Chemistry, The Bombay College of Pharmacy, Kalina, Santacruz (East), Mumbai 400098, India. anandshindikar@yahoo.com
Viswanathan
C L
CL
D000818:Animals; D000995:Antitubercular Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D024841:Fluoroquinolones / Q000138:chemical synthesis* / Q000494:pharmacology; D051379:Mice; D008826:Microbial Sensitivity Tests; D009169:Mycobacterium tuberculosis / Q000187:drug effects*; D000077489:Piperazine; D010879:Piperazines / Q000737:chemistry*; D013154:Spleen / Q000378:metabolism
D000995:Antitubercular Agents; D024841:Fluoroquinolones; D010879:Piperazines; D000077489:Piperazine; C061363:sparfloxacin