179400-53-4

Upstream product

• 1603-41-4 (5-methyl-pyridin-2-yl)amine 
• 18368-64-4 2-chloro-5-methylpyridine 
• 179400-98-7 5-methyl-pyridine-2-sulphonic acid 6-chloro-5-(2-methoxy-phenoxy)-2-morpholin-4-yl-pyrimidin-4-ylamide 
• 167403-76-1 5-(2-methoxy-phenoxy)-2-(morpholin-4-yl)-4,6(1H,5H)-pyrimidinedione 
• 179400-16-9 5-methylpyridine-2-sulfonyl chloride 
• 18368-58-6 2-mercapto-5-methylpyridine 
• 107-21-1 ethylene glycol 
• 167403-77-2 4,6-dichloro-5-(2-methoxy-phenoxy)-2-(morpholin-4-yl)pyrimidine 

Relevant academic research and scientific papers

SULPHONAMIDES

Compounds of the formula STR1 wherein the variables are hereinbelow defined. The compounds of formula I are inhibitors for endothelin receptors. They can be used for the treatment of disorders which are associated with endothelin activities, especially circulatory disorders such as hypertension, ischaemia, vasospasms and angina pectoris.

Discovery of Ro 48-5695: A potent mixed endothelin receptor antagonist optimized from Bosentan

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.