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取代嘧啶、吡唑并[3,4-d]嘧啶和咪唑并[4,5-d]嘧啶的合成及其抗真菌活性评价。

Synthesis of substituted pyrimidines, pyrazole[3,4-d]pyrimidines and imidazo[4,5-d]pyrimidines and evaluation of their antifungal activity.

作者信息

Ronsisvalle G, Pappalardo M S, Vittorio F, Pasquinucci L, Bousquet E, Oliveri S, Cammarata E

机构信息

Istituto di Chimica Farmaceutica e Tossicologica, Università di Trieste, Italy.

出版信息

Farmaco. 1989 Apr;44(4):383-90.

PMID:2775419
Abstract

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.

摘要

合成了一些嘧啶、吡唑并[3,4 - d]嘧啶和咪唑并[4,5 - d]嘧啶,这些化合物在嘧啶核上带有5 - 硝基和5 - 氨基噻吩 - 2 - 硫醚官能团,并对其针对几种酵母菌株和皮肤真菌的抗真菌活性进行了评估。4 - 氨基 - 2 - 嘧啶基 - 5'- 硝基 - 2'- 噻吩硫醚(Va)对酵母和皮肤真菌均有活性(效力约为咪康唑的30倍)。化合物(II b)、(V b)和(VIII b)仅对皮肤真菌表现出轻微活性,而其他化合物则无活性。

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