Bioorganic and Medicinal Chemistry Letters p. 939 - 944 (1997)
Update date:2022-08-04
Topics:
Raju
Okun, Ilya
Stavros, Fiona
Chan, Ming Fai
The potential proteolytic instability of the amide bond present in some ET(A) 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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