title: Potential tuberculostatic agents. Topliss application on benzoic acid [(5-nitro-thiophen-2-yl)-methylene]-hydrazide series.
abstract: Nitroaromatic compounds such as nifuroxazide are used in many human enteropathogenic bacteria infections without causing an increase in the plasmidial antibiotic resistance of the aerobic Gram-negative intestinal Enterobacteriaceae. For these reasons, these compounds have been synthesized using the rational approach of Topliss' decision tree. Generally, this approach allows us to obtain the most active derivative from the series in a few steps. These compounds were tested against Mycobacterium tuberculosis in vitro and the most active of the series identified. A new lead for potential tuberculostatic activity has been predicted and will be used in further QSAR studies.
authors.affiliation: Fac. de Ciências Farmacêuticas, USP, Av. Prof. Lineu Prestes, 580, São Paulo-SP 05508-900, Brazil.
authors.forename: Daniela G
authors.initials: DG
authors.lastname: Rando
authors.forename: Dayse N
authors.initials: DN
authors.lastname: Sato
authors.forename: Leonardo
authors.initials: L
authors.lastname: Siqueira
authors.forename: Alberto
authors.initials: A
authors.lastname: Malvezzi
authors.forename: Clarice Q F
authors.initials: CQ
authors.lastname: Leite
authors.forename: Antonia T
authors.initials: AT
authors.lastname: do Amaral
authors.forename: Elizabeth I
authors.initials: EI
authors.lastname: Ferreira
authors.forename: Leoberto C
authors.initials: LC
authors.lastname: Tavares
mesh_terms: D000995:Antitubercular Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D003663:Decision Trees; D015195:Drug Design; D006834:Hydrazines / Q000138:chemical synthesis / Q000494:pharmacology; D062385:Hydroxybenzoates / Q000138:chemical synthesis* / Q000494:pharmacology; D008826:Microbial Sensitivity Tests; D009169:Mycobacterium tuberculosis / Q000187:drug effects; D009581:Nitrofurans / Q000138:chemical synthesis* / Q000494:pharmacology; D011724:Pyridazines / Q000138:chemical synthesis / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D000995:Antitubercular Agents; D006834:Hydrazines; D062385:Hydroxybenzoates; D009581:Nitrofurans; D011724:Pyridazines; C013150:nifuroxazide