150726-07-1Relevant articles and documents
Modifications and structure-activity relationships at the 2-position of 4-sulfonamidopyrimidine derivatives as potent endothelin antagonists
Morimoto, Hiroshi,Shimadzu, Hideshi,Hosaka, Toshihiro,Kawase, Yasushi,Yasuda, Kosuke,Kikkawa, Kohei,Yamauchi-Kohno, Rikako,Yamada, Koichiro
, p. 81 - 84 (2007/10/03)
To improve water solubility and to study structure-activity relationships, we modified the structure of the pyrimidine nucleus of each of a series of potent ETA antagonists, 3a and 4a, at the 2-position. In a previous study, each of these antag
Discovery of Ro 48-5695: A potent mixed endothelin receptor antagonist optimized from Bosentan
Neidhart, Werner,Breu, Volker,Burri, Kaspar,Clozel, Martine,Hirth, Georges,Klinkhammer, Uwe,Giller, Thomas,Ramuz, Henri
, p. 2223 - 2228 (2007/10/03)
Implementation of a pyridylcarbamoyl group and an isopropylpyridylsulfonamide substituent as key components in the scaffold of Bosentan resulted in the identification of the potent orally active endothelin receptor antagonist Ro 48-5695. It shows affinities for ET(A) and ET(B) receptors in the low nanomolar range and high functional antagonistic potency in vitro.
SULFONAMIDES
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, (2008/06/13)
The novel sulfonamides of formula I, STR1 in which the symbols R. sup.1-R 9, R a, R b, X, Y and n have the significance given in the description and salts thereof can be used for the treatment of circulatory disorders, especially hypertension, ischemia, vasopasms and angina pectoris.