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@ ScienceNode.dll
2025-05-19 19:49:48
๐๐๐ฏ๐๐ฅ๐จ๐ฉ๐ฆ๐๐ง๐ญ ๐จ๐ ๐๐๐๐ข (A) The natural peptide SQ 20881 (sequence EWPRPQIPP), discovered in Bothrops jararaca venom, is an inhibitor of ACE, inducing a drop in blood pressure. Squibb company synthetized a derivative which led, after optimization, to the captopril (1981). Because of the side effects of the thiol group, Merck replaced the latter with a carboxylate, resulting in the enalaprilat molecule (1985). However, as this modification resulted in the loss of oral bioavailability, the esterification of the enalaprilat was considered by Merck to solve the problem successfully and created the enalapril (1985). (B) Interaction between captopril and ACE. By preventing the binding of the inert Angiotensin I to ACE, captopril inhibits the formation of Angiotensin II.
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