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

DOI: 10.1016/S0960-894X(97)00400-9

Source and publish data:

Bioorganic and Medicinal Chemistry Letters p. 2223 - 2228 (1997)

Update date:2022-08-04

Topics:

Authors:

Neidhart, Werner

Breu, Volker

Burri, Kaspar

Clozel, Martine

Hirth, Georges

Klinkhammer, Uwe

Giller, Thomas

Ramuz, Henri

Read Full Text PDF DownLoad Join now for total 90,000,000 free articles

Article abstract of DOI:10.1016/S0960-894X(97)00400-9

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.

Full text of DOI:10.1016/S0960-894X(97)00400-9

Products guided by the article

Product name:4,6-Dichloro-2-isopropyl-5-(2-methoxy-phenoxy)-pyrimidine

Cas No:150727-05-2

R&D Labs maybe for 150727-05-2

HANGZHOU ZHONGCHANG SCIENTIFIC CO.,LTD

Contact:+86-571-88932183

Address:Hangzhou
Suzhou Kangrun Pharmaceutical, Inc

Contact:86-512-63912376，63913329

Address:Building 2, No. 2358 ,Chang'an Rd, Wujiang Economic Development Zone Pioneering park, china
SPRING CHEMICAL INDUSTRY CO.,LTD

Contact:86-187-66672125

Address:linchi industry park.zouping
Nanjing HuiBaiShi Biotechnology Co.,Ltd.

Contact:+86 (25)58745219

Address:No.606 Ningliu Road,LiuHe District.
Shijiazhuang Haotian Chemical Co., Ltd.

Contact:86-311-85044374

Address:293 Donggang Road

Relevant to this article

α-Aminoamides as ligands in Goldberg amidations

Doi:10.1016/j.tetlet.2013.09.099
(2013)
Synthesis of sugar-like amino-carboxylic acids from D-mannitol

Doi:10.1016/00404-0399(50)14024-
(1995)
Synthesis of Methoxy-, Methylenedioxy-, Hydroxy-, and Halo-Substituted Benzophenanthridinone Derivatives as DNA Topoisomerase IB (TOP1) and Tyrosyl-DNA Phosphodiesterase 1 (TDP1) Inhibitors and Their Biological Activity for Drug-Resistant Cancer

Doi:10.1021/acs.jmedchem.1c00318
(2021)
Intramolecular Diels-Alder Reaction of Vinylsulfonates Derived from Hydroxyalkyl Substituted 1,3-Dienes and Oxidative Desulfurization of the Resultant Sultones

Doi:10.1016/0040-4020(94)00969-2
(1995)
Synthesis of new 2-substituted 6,7-dimethoxy-1-(methylcarbamoyl)- 4-spirocyclopentane-1,2,3,4-tetrahydroisoquinolines

Doi:10.1134/S1070428013110122
()
Synthesis of cationic rhodium(I) and iridium(I) carbonyl complexes of tetradentate P(CH₂CH₂PPh₂)₃ ligand: An implication of steric inhibition and catalytic hydroformylation reaction

Doi:10.1016/j.molcata.2013.10.016
(2014)

Article Doi