Amide bond surrogates: A study in thiophenesulfonamide based endothelin receptor antagonists

B Raju, I Okun, F Stavros, MF Chan

Index: Raju; Okun, Ilya; Stavros, Fiona; Chan, Ming Fai Bioorganic and Medicinal Chemistry Letters, 1997 , vol. 7, # 7 p. 939 - 944

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Citation Number: 9

Abstract

The potential proteolytic instability of the amide bond present in some ETA selective thiophenesulfonamide endothelin antagonists exemplified by TBC-10708 led us to investigate the replacement of this moiety with stable amide bond surrogates such as a trans double bond and an ethylene spacer. The effect of these replacements on the binding affinity is described.

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