Potential tuberculostatic agents: micelle-forming copolymer poly(ethylene glycol)-poly(aspartic acid) prodrug with isoniazid.
With the objective of obtaining slow-acting isoniazid derivatives, of potential use as chemoprophylactics or chemotherapeutics in tuberculosis, the micelle-forming copolymer of poly(ethylene glycol)-poly(aspartic acid) prodrug with isoniazid was synthesized. The derivative obtained was found to be active in Mycobacterium tuberculosis culture, with a minimal inhibitory concentration (MIC) 5.6 times lower than that of the tuberculostatic drug.
Silva
M
M
Faculdade de Ciências Farmacêuticas, Universidade Estadual Paulista, CP502, 14801-902, Araraquara, SP, Brazil. hajudan@usp.br
Lara
A S
AS
Leite
C Q
CQ
Ferreira
E I
EI
D000995:Antitubercular Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D005079:Excipients; D007538:Isoniazid / Q000737:chemistry* / Q000494:pharmacology*; D008823:Micelles; D008826:Microbial Sensitivity Tests; D009169:Mycobacterium tuberculosis / Q000187:drug effects; D010455:Peptides; D011092:Polyethylene Glycols; D011355:Prodrugs / Q000138:chemical synthesis* / Q000494:pharmacology*
D000995:Antitubercular Agents; D005079:Excipients; D008823:Micelles; D010455:Peptides; D011355:Prodrugs; C017645:polyaspartate; D011092:Polyethylene Glycols; D007538:Isoniazid