Long-acting angiotensin II inhibitors containing hexafluorovaline in position 8.
K H Hsieh, P Needleman, G R Marshall
文献索引:J. Med. Chem. 30(6) , 1097-100, (1987)
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摘要
An improved synthesis of hexafluorovaline (Hfv) derivatives, i.e., DL-Hfv-OBzl and Boc-DL-Hfv, is described. Incorporation of hexafluorovaline into angiotensin resulted in [Sar1,Hfv8]AII and [Sar1,D-Hfv8]AII. At the nanogram/milliliter dose range, the L congener was 20-100 times more active as either angiotensin agonist or angiotensin antagonist than its D diastereomer on isolated tissue preparations. At the microgram dose range, both [Sar1,Hfv8]AII and [Sar1,D-Hfv8]AII were significantly more effective than [Sar1,Leu8]AII as angiotensin II inhibitors, producing prolonged blockade of the pressor response toward angiotensin II for over 1 h.
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1981-09-01
[J. Med. Chem. 24(9) , 1043-7, (1981)]