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

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Authors:

Sakaki, Junichi

Murata, Toshiki

Yuumoto, Yoko

Nakamura, Ikushi

Frueh, Thomas

Pitterna, Thomas

Iwasaki, Genji

Oda, Kyoko

Yamamura, Takaki

Hayakawa, Kenji

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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

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