Synthesis and biological activity of nifuroxazide and analogs. II.
Nifuroxazyde and six analogs were synthesized by varying the substitute from the para-position of the benzenic ring and the heteroatom of the heterocyclic ring. The MIC of seven resultant compounds was determined by serial dilutions, testing the ATCC 25923 strain of Staphylococcus aureus. A significant increase in the anti-microbial activity of thyophenic analogs, as compared with furanic and pyrrholic analogs, was observed. In addition, unlike the cyano and hydroxyl groups, the acetyl group promoted anti-microbial activity.
Tavares
L C
LC
Departamento de Tecnologia Bioquímico-Farmacêutica Faculdade de Ciências Farmacêuticas Universidade de São Paulo, Brasil.
Chisté
J J
JJ
Santos
M G
MG
Penna
T C
TC
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D001419:Bacteria / Q000187:drug effects; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D062385:Hydroxybenzoates / Q000138:chemical synthesis* / Q000494:pharmacology; D008826:Microbial Sensitivity Tests; D009581:Nitrofurans / Q000138:chemical synthesis* / Q000494:pharmacology
D000900:Anti-Bacterial Agents; D062385:Hydroxybenzoates; D009581:Nitrofurans; C013150:nifuroxazide