Structure-activity relationships of cyclic pentapeptide endothelin A receptor antagonists

…, T Mase, S Nakajima, T Fukuroda, T Saeki

Index: Fukami; Nagase; Fujita; Hayama; Niiyama; Mase; Nakajima; Fukuroda; Saeki; Nishikibe; Ihara; Yano; Ishikawa Journal of Medicinal Chemistry, 1995 , vol. 38, # 21 p. 4309 - 4324

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Citation Number: 39

Abstract

Analogues of the natural product endothelin A (ETA) receptor antagonists c~ c~ o (-DT~~~- DG~ u~-Ala3-D-Vd4-LeU5-)(1) and cyc~ o (-D-~ 1-D-~~ uz-~ a 3-D-~ o~ e 4-~ u 5-)(2) were prepared and tested for inhibitory activity against [12511endothelin (ET-1) binding to protein ETA receptors. The DDLDL chirality sequence of the natural products appeared to be critical for inhibitory activity because conversion of either D-Trp or DG~ u (or both) in 1 to the ...