抗真菌剂。VIII. 联苯苄唑联吡咯类似物的合成与抗真菌活性
Antifungal agents. VIII. Synthesis and antifungal activities of bipyrryl analogues of bifonazole.
作者信息
di Santo R, Massa S, Costi R, Simonetti G, Retico A, Apuzzo G, Troccoli F
机构信息
Dipartimento di studi farmaceutici, Università di Roma, La Sapienza, Italy.
出版信息
Farmaco. 1994 Apr;49(4):229-36.
Various bipyrryl analogues of bifonazole were synthesized starting from aryl-3-pyrryl-1-imidazolylmethanes. The introduction of a second pyrryl portion was performed by linking an acrylate moiety at 1-position of the pyrrole ring and then by treatment with TosMIC. The bipyrryl esters were hydrolyzed and decarboxylated to afford the required imidazoles. All new imidazole derivatives were tested against Candida albicans and Candida spp using as standard controls miconazole, bifonazole and ketoconazole.
从芳基-3-吡咯基-1-咪唑基甲烷出发，合成了联苯苄唑的各种联吡咯类似物。通过在吡咯环的1-位连接一个丙烯酸酯部分，然后用TosMIC处理来引入第二个吡咯部分。对联吡咯酯进行水解和脱羧反应，得到所需的咪唑。使用咪康唑、联苯苄唑和酮康唑作为标准对照，对所有新的咪唑衍生物进行了抗白色念珠菌和念珠菌属的测试。
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