title: Synthesis and preliminary in vitro evaluation of antimycobacterial activity of new pyrrolo[1,2-a] quinoxaline-carboxylic acid hydrazide derivatives.
abstract: New pyrrolo[1,2-a]quinoxaline-2- or -4-carboxylic acid hydrazide derivatives were synthesized from nitroaniline or 1,2-phenylenediamine, and evaluated in vitro for their antimycobacterial activity as part of a TAACF TB screening program. Two compounds 7c and 13 showed an interesting activity at 6.25 microg/mL against Mycobacterium tuberculosis H37Rv, with a 94 and 100 percentage inhibition, respectively.
authors.affiliation: EA 2962 - Pharmacochimie, UFR des Sciences Pharmaceutiques, Université Victor Segalen Bordeaux 2, 33076 Bordeaux Cedex, France.
authors.forename: Jean
authors.initials: J
authors.lastname: Guillon
authors.forename: Robert C
authors.initials: RC
authors.lastname: Reynolds
authors.forename: Jean-Michel
authors.initials: JM
authors.lastname: Leger
authors.forename: Marie-Aude
authors.initials: MA
authors.lastname: Guie
authors.forename: Stephane
authors.initials: S
authors.lastname: Massip
authors.forename: Patrick
authors.initials: P
authors.lastname: Dallemagne
authors.forename: Christian
authors.initials: C
authors.lastname: Jarry
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D000995:Antitubercular Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000493:pharmacokinetics; D002264:Carboxylic Acids / Q000737:chemistry*; D049109:Cell Proliferation / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D002522:Chlorocebus aethiops; D018360:Crystallography, X-Ray; D004353:Drug Evaluation, Preclinical; D006834:Hydrazines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D066298:In Vitro Techniques; D008958:Models, Molecular; D015394:Molecular Structure; D009169:Mycobacterium tuberculosis / Q000187:drug effects*; D011810:Quinoxalines / Q000737:chemistry*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D014709:Vero Cells
chemical_list: D000900:Anti-Bacterial Agents; D000995:Antitubercular Agents; D002264:Carboxylic Acids; D006834:Hydrazines; D011810:Quinoxalines