Discovery of IRL 3461: A novel and potent endothelin antagonist with balanced ET(A)/ET(B) affinity

DOI: 10.1016/S0960-894X(98)00387-4

Source and publish data:

Bioorganic and Medicinal Chemistry Letters p. 2241 - 2246 (1998)

Update date:2022-08-05

Topics:

Authors:

Sakaki, Junichi

Murata, Toshiki

Yuumoto, Yoko

Nakamura, Ikushi

Frueh, Thomas

Pitterna, Thomas

Iwasaki, Genji

Oda, Kyoko

Yamamura, Takaki

Hayakawa, Kenji

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

Article abstract of DOI:10.1016/S0960-894X(98)00387-4

IRL 3461, N-butanesulfonyl-[N-(3,5-dimethylbenzoyl)-N-methyl-3-[4-(5- isoxazolyl)-phenyl]-alanyl]-(L)-valineamide, a potent and bifunctional (ET(A) + ET(B)) [Ki(ET(A))=1.8 nM, Ki(ET(B))=1.2 nM] antagonist was discovered by structural modification of IRL 2500, an ET(B) selective antagonist. IRL 3461 was found to be stable on incubation with human, rat, mouse, and guinea pig plasmas.

Full text of DOI:10.1016/S0960-894X(98)00387-4

Products guided by the article

Product name:Phenylalanine, 4-(5-isoxazolyl)-, ethyl ester

Cas No:184698-53-1

R&D Labs maybe for 184698-53-1

Guangzhou Probig Fine Chemical Co., Ltd.

Contact:020-86297874

Address:No.2, 1/F, No.20, Hetai Road,Hebian Village, Baiyun District,Guangzhou,China
Gulang Hailun Fine Chemicals Co., Ltd.

Contact:13605738876 0573-84772866

Address:No. 4 Bridge, Xinjing port, Yaozhuang Town, Jiashan County, Zhejiang, China
Reliability Assessment Solutions (Changhzou) Co., Ltd.

Contact:86-519-85607515

Address:RM 601-603 BD1 Fuchen Mansion, 8 Taihu East RD, Xinbei District, Changhou, Jiangsu 213022, China
Huixian Tiankai Paper Making Agent CO.,Ltd.

Contact:+86-373-6899808

Address:Mengdian Industrial Avenue,Huixian,Xinxiang,Henan,China
Nanjing Qirui Material Co., Ltd.

Contact:+86-25-52320053

Address:F4-5, #17 Building, Chuang Yi Yuan, No.6 Guanghua East Street, Nanjing, 210007 P.R.China

Relevant to this article

Exploitation of palladium-catalyzed reductive enyne cyclization in the synthesis of (-)-4a,5-dihydrostreptazolin

Doi:10.1016/S0040-4039(96)02032-1
(1996)
Efficient Syntheses of (1R,2R)- and (1S,2S)-2-Amino-1-alkyl(or aryl)-1,3-propanediols by Regioselective Ring Opening of Aziridine-2-methanols

Doi:10.1021/jo961168z
(1997)
Regio- and stereoselective synthesis of (Z)-β-silylalkenylboranes by silaboration of alkynes catalyzed by palladium and platinum complexes

Doi:10.1016/S0040-4020(99)00444-5
(1999)
Mizoroki–Heck Cyclizations of Amide Derivatives for the Introduction of Quaternary Centers

Doi:10.1002/anie.201703174
(2017)
Metal cation binding to acetylenic tetrathiafulvalene–pyridine conjugates: affinity tuned by preorganization and cavity size

Doi:10.1016/j.tet.2016.08.001
(2016)
Synthesis of some phosphino- and arsinobenzenechromium tricarbonyl derivatives and metal carbonyl clusters

Doi:10.1139/v96-244
(1996)

Article Doi