title: In vitro advanced antimycobacterial screening of isoniazid-related hydrazones, hydrazides and cyanoboranes: part 14.
abstract: As a part of an ongoing search for new isoniazid-related isonicotinoylhydrazones (ISNEs), 2'-monosubstituted isonicotinohydrazides and cyanoboranes, some analogues belonging to these three series of compounds were further evaluated in an in vitro advanced antimycobacterial screening. The results here reported allowed us to extend their structure-activity relationships. A general correlation emerged between their lipophilicity and effectiveness against intracellular M. tuberculosis. On the whole, the most interesting result of this research was that some hydrazides and ISNEs proved to be more effective antimycobacterial agents than parental isoniazid in a TB-infected macrophage model.
authors.affiliation: Dipartimento Farmaco-chimico, Facoltà di Farmacia, Università di Messina, Viale SS. Annunziata, 98168 Messina, Italy. rmaccari@pharma.unime.it
authors.forename: Rosanna
authors.initials: R
authors.lastname: Maccari
authors.forename: Rosaria
authors.initials: R
authors.lastname: Ottanà
authors.forename: Maria Gabriella
authors.initials: MG
authors.lastname: Vigorita
mesh_terms: D000995:Antitubercular Agents / Q000737:chemistry / Q000494:pharmacology*; D001880:Boranes / Q000494:pharmacology*; D006835:Hydrazones / Q000494:pharmacology*; D007538:Isoniazid / Q000737:chemistry / Q000494:pharmacology*; D009169:Mycobacterium tuberculosis / Q000187:drug effects*
chemical_list: D000995:Antitubercular Agents; D001880:Boranes; D006835:Hydrazones; D007538:Isoniazid