Synthesis and antitubercular activity of new L-serinyl hydrazone derivatives.
A series of 32 L-serinyl hydrazone derivatives have been synthesized and evaluated for their in vitro antibacterial activity against Mycobacterium tuberculosis H37Rv, being also evaluated their cell viabilities in non infected and infected macrophages with Mycobacterium bovis Bacillus Calmette-Guerin (BCG). The compounds 8c, 8e, 8h and 8i, were non-cytotoxic and exhibited an important minimum inhibitory concentration (MIC) activity between 25 and 100 μg/mL, which can be compared with that of the tuberculostatic drug D-cicloserine (5-20 μg/mL).
Fundação Oswaldo Cruz, Instituto de Tecnologia em Fármacos-Far Manguinhos, Fundação Oswaldo Cruz, 21041-250, Rio de Janeiro, RJ, Brazil.
Alessandra Campbell
AC
Pinheiro
Carlos Roland
CR
Kaiser
Thais Cristina Mendonça
TC
Nogueira
Samir Aquino
SA
Carvalho
Edson Ferreira
EF
da Silva
Larisse de Oliveira
Lde O
Feitosa
Maria das Graças Müller de Oliveira
Md
Henriques
André Luís Peixoto
AL
Candéa
Maria Cristina Silva
MC
Lourenço
Marcus Vinícius Nora
MV
de Souza
D000995:Antitubercular Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D002470:Cell Survival / Q000187:drug effects; D003523:Cycloserine / Q000737:chemistry / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D006835:Hydrazones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D008264:Macrophages / Q000187:drug effects / Q000382:microbiology; D008826:Microbial Sensitivity Tests; D008958:Models, Molecular; D015394:Molecular Structure; D009163:Mycobacterium bovis / Q000302:isolation & purification; D009169:Mycobacterium tuberculosis / Q000166:cytology / Q000187:drug effects*; D012694:Serine / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
D000995:Antitubercular Agents; D006835:Hydrazones; D012694:Serine; D003523:Cycloserine