Synthesis of substituted pyrimidines, pyrazole[3,4-d]pyrimidines and imidazo[4,5-d]pyrimidines and evaluation of their antifungal activity.
Some pyrimidines, pyrazolo[3,4-d]pyrimidines and imidazo[4,5-d]pyrimidines bearing the 5-nitro- and 5-aminothienyl-2-sulfide functionalities on the pyrimidine nucleus were synthesized and evaluated for their antifungal activity against several strains of yeasts and dermatophytes. 4-Amino-2-pyrimidinyl-5'-nitro-2'-thienylsulfide (Va) resulted active against both yeasts and dermatophytes (about 30 fold less potent than Miconazole). Compds. (II b), (V b) and (VIII b) showed only a slight activity against dermatophytes, while the other compounds were inactive.
Ronsisvalle
G
G
Istituto di Chimica Farmaceutica e Tossicologica, Università di Trieste, Italy.
Pappalardo
M S
MS
Vittorio
F
F
Pasquinucci
L
L
Bousquet
E
E
Oliveri
S
S
Cammarata
E
E
D000107:Acetylation; D000935:Antifungal Agents / Q000138:chemical synthesis*; D055598:Chemical Phenomena; D002621:Chemistry; D005658:Fungi / Q000187:drug effects; D007093:Imidazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D008826:Microbial Sensitivity Tests; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000494:pharmacology
D000935:Antifungal Agents; D007093:Imidazoles; D011720:Pyrazoles; D011743:Pyrimidines