血管紧张素转化酶抑制剂——卡托普利酯类衍生物的合成和药理作用
SYNTHESIS OF ANGIOTENSIN CONVERTING ENZYME INHIBITOR, CAPTOPRIL ESTER DERIVATIVES
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摘要: 卡托普利(巯甲丙脯酸)为一新型的血管紧张素转化酶抑制剂,临床用于治疗高血压和充血性心力衰竭,但半衰期短。为延长药物作用时间和提高药效,本文合成了它的酯类衍生物。初步药理试验结果表明,某些酯类化合物呈现明显降压恬性和延长作用时间。Abstract: Captcpril is an orally activ angiotensin converting enzyme inhibitor and is used for hypertensive and congestive heart failure diseases. The drawback of the drug is associated with its short biological half life. In order to search for new derivatives with longer duration of action and higher activity, captopril diesters and triesters were synthesized. In preliminary pharmacological tests some esters showed higher hypotensive acitivity and longer duration of action than that of captopril.
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