具有潜在抗菌活性的孕酮杂环衍生物的合成。
Synthesis of progesterone heterocyclic derivatives of potential antimicrobial activity.
作者信息
Mohareb Rafat M, Hana Hanaa Y
机构信息
Department of Organic Chemistry, Faculty of Pharmacy, University of Modern Sciences and Arts (MSA), October City, Giza, Egypt.
出版信息
Acta Pharm. 2008 Mar;58(1):29-42. doi: 10.2478/v10007-007-0043-3.
The aim of this work was to synthesize steroidal heterocycles and to elucidate the potential role of these compounds as antimicrobial agents. The synthesis of steroidal heterocycles containing the pyrazole, isoxazole, thiazole, pyrane, pyridine, pyridazine, or benzopyrane ring attached to the pregnene nucleus is reported. Progesterone (1) reacts with dimethyl formamide dimethyl acetal to form enamine 2. Heterocyclization of 2 with hydrazines, hydroxylamine, glycine, ethyl acetoacetate or cyanomethylene afforded novel steroidal heterocyclic derivatives. The in vitro antimicrobial evaluation showed that all synthesized compounds show activity against the used strains of Gram positive bacteria and fungi.
这项工作的目的是合成甾体杂环化合物，并阐明这些化合物作为抗菌剂的潜在作用。本文报道了含有连接到孕烯核上的吡唑、异恶唑、噻唑、吡喃、吡啶、哒嗪或苯并吡喃环的甾体杂环化合物的合成。孕酮（1）与二甲基甲酰胺二甲基缩醛反应形成烯胺2。烯胺2与肼、羟胺、甘氨酸、乙酰乙酸乙酯或氰基亚甲基进行杂环化反应，得到新型甾体杂环衍生物。体外抗菌评估表明，所有合成化合物对所用的革兰氏阳性菌和真菌菌株均有活性。
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