Synthesis and biological screening of aminothiadiazine dioxides related to trimethoprim.
New derivatives of 3-amino-1,2,6-thiadiazine 1,1-dioxide have been synthesized and their antibacterial, antifungal and DHFR inhibitory activities evaluated. Their chemical structures have been established by means of analytical and NMR spectroscopic data. Among the compounds studied, the 4,4-dibromo derivative 11 showed fungistatic activity against C. albicans.
Alkorta
I
I
Instituto de Quimica Médica, Madrid, Spain.
Goya
P
P
Nombela
C
C
Medina
R
R
Pérez Martín
C
C
D000818:Animals; D000900:Anti-Bacterial Agents; D000890:Anti-Infective Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D001419:Bacteria / Q000187:drug effects; D002176:Candida albicans / Q000187:drug effects; D002417:Cattle; D005493:Folic Acid Antagonists; D008099:Liver / Q000201:enzymology; D009682:Magnetic Resonance Spectroscopy; D008826:Microbial Sensitivity Tests; D013829:Thiadiazines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D014295:Trimethoprim / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology
D000900:Anti-Bacterial Agents; D000890:Anti-Infective Agents; D005493:Folic Acid Antagonists; D013829:Thiadiazines; D014295:Trimethoprim