190520-98-0Relevant articles and documents
Amide bond surrogates: A study in thiophenesulfonamide eased endothelin receptor antagonists
Raju,Okun, Ilya,Stavros, Fiona,Chan, Ming Fai
, p. 939 - 944 (2007/10/03)
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.