Discovery and synthesis of a potent sulfonamide ET(B) selective antagonist
The synthesis and structure-activity relationships of a series of sulfonamide endothelin antagonists are described. In the course of our modification studies, we discovered ET(B) selective antagonists. The most potent compound 15f displays IC50 values of 1.7 μM and 0.002 μM to ET(A) and ET(B) receptors, respectively. (C) 2000 Elsevier Science Ltd. All rights reserved.
Directed lithiation of N-(tert-butoxycarbonyl)aminoisoxazole: Synthesis of 4-substituted aminoisoxazoles
Directed lithiation of 3-(Boc-amino)isoxazole 4 and 5-(Boc-amino)isoxazole 9 is described. Dilithioisoxazoles reacted with a variety of electrophiles to give the corresponding 4-substituted isoxazoles.
Konoike, Toshiro,Kanda, Yasuhiko,Araki, Yoshitaka
p. 3339 - 3342
(2007/10/03)
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