title: Novel fluoroquinolones: design, synthesis, and in vivo activity in mice against Mycobacterium tuberculosis H37Rv.
abstract: 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.
authors.affiliation: Department of Pharmaceutical Chemistry, The Bombay College of Pharmacy, Kalina, Santacruz (East), Mumbai 400098, India. anandshindikar@yahoo.com
authors.forename: Anand V
authors.initials: AV
authors.lastname: Shindikar
authors.forename: C L
authors.initials: CL
authors.lastname: Viswanathan
mesh_terms: 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
chemical_list: D000995:Antitubercular Agents; D024841:Fluoroquinolones; D010879:Piperazines; D000077489:Piperazine; C061363:sparfloxacin