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Endothelin antagonists: substituted mesitylcarboxamides with high potency and selectivity for ET(A) receptors.
J Med Chem. 1999 Nov 4;42(22):4485-99. doi: 10.1021/jm9900063.
J Med Chem. 1999.
PMID: 10579813
Discovery, modeling, and human pharmacokinetics of N-(2-acetyl-4,6-dimethylphenyl)-3-(3,4-dimethylisoxazol-5-ylsulfamoyl)thiophene-2-carboxamide (TBC3711), a second generation, ETA selective, and orally bioavailable endothelin antagonist.
Wu C, Decker ER, Blok N, Bui H, You TJ, Wang J, Bourgoyne AR, Knowles V, Berens KL, Holland GW, Brock TA, Dixon RA.
Wu C, et al. Among authors: bourgoyne ar.
J Med Chem. 2004 Apr 8;47(8):1969-86. doi: 10.1021/jm030528p.
J Med Chem. 2004.
PMID: 15055997
Clinical Trial.
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Acyl substitution at the ortho position of anilides enhances oral bioavailability of thiophene sulfonamides: TBC3214, an ETA selective endothelin antagonist.
Wu C, Decker ER, Blok N, Li J, Bourgoyne AR, Bui H, Keller KM, Knowles V, Li W, Stavros FD, Holland GW, Brock TA, Dixon RA.
Wu C, et al. Among authors: bourgoyne ar.
J Med Chem. 2001 Apr 12;44(8):1211-6. doi: 10.1021/jm000349x.
J Med Chem. 2001.
PMID: 11312921
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