167403-78-3Relevant articles and documents
The use of sulfonylamido pyrimidines incorporating an unsaturated side chain as endothelin receptor antagonists
Bolli, Martin H.,Boss, Christoph,Clozel, Martine,Fischli, Walter,Hess, Patrick,Weller, Thomas
, p. 955 - 959 (2007/10/03)
A series of compounds structurally related to bosentan 1 featuring an unsaturated side chain at position 6 of the core pyrimidine have been studied for their potential to block the ETA and ETB receptor. Incorporation of a 2-butyne-1,4-diol linker bearing a pyridyl carbamoyl moiety led to in vitro highly potent endothelin receptor antagonists (e.g., 70 and 75). The propargyl derivative 26 significantly reduced blood pressure in in vivo model studies with hypertensive salt-sensitive Dahl rats.
Pyrimidine derivatives as endothelin antagonists
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, (2008/06/13)
The present invention is directed to a pyrimidine derivative of the following formula (1) or a salt of the derivative: STR1 ?wherein R1 represents a hydroxyl group, a lower alkoxy group, a phenyloxy group which may have a substituent, an aralkyloxy group which may have a substituent, or --NR2 R3 ; X represents an oxygen atom or N--R4 ; m is 2 or 3; and n is 1 or 2 (wherein each of R2 and R3, which are identical to or different from each other, represents a hydrogen atom, a hydroxyl group, a lower alkyl group which may have a substituent, a phenyl group which may have a substituent, an aralkyl group which may have a substituent, or a heterocyclic group which may have a substituent; R4 represents a lower alkyl group, a phenyl group, a formyl group, or a lower alkoxycarbonyl group)!, as well as to a medicine containing the derivative or salt as the active ingredient. The compounds exhibit strong binding inhibitory activity against endothelin having potent vasoconstrictive effect. Therefore, the compounds are effective as remedies for various diseases including circulatory diseases.