Antitubercular activity of alpha,omega-diaminoalkanes, H2N(CH2)nNH2.
A series of 11 alpha,omega-diaminoalkanes, (H(2)N(CH(2))(n)NH(2), n=2-12) have been evaluated for their in vitro antibacterial activity against Mycobacterium tuberculosis H37Rv. Compounds, (H(2)N(CH(2))(n)NH(2), n=9-12), exhibited a very good activities in the range 2.50-3.12 microg/mL, which can be compared with that of the first line drug, ethambutol (3.12 microg/mL). These results and a preliminary QSAR study can be considered an important start point for the rational design of new leads for anti-TB compounds.
Vergara
Fátima M F
FM
Instituto de Tecnologia em Fármacos-Far-Manguinhos, Rua Sizenando Nabuco 100, Manguinhos, Rio de Janeiro, RJ, Brazil.
Henriques
Maria das G M O
Md
Candea
André L P
AL
Wardell
Jim L
JL
De Souza
Marcus V N
MV
D000473:Alkanes / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity; D000818:Animals; D000995:Antitubercular Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity; D002460:Cell Line; D004977:Ethambutol / Q000737:chemistry / Q000494:pharmacology*; D051379:Mice; D009169:Mycobacterium tuberculosis / Q000187:drug effects; D021281:Quantitative Structure-Activity Relationship
D000473:Alkanes; D000995:Antitubercular Agents; D004977:Ethambutol