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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. J Med Chem. 2004 Apr 8;47(8):1969-86. doi: 10.1021/jm030528p. J Med Chem. 2004. PMID: 15055997 Clinical Trial.
Nonpeptide endothelin antagonists in clinical development.
Wu C, Decker ER, Holland GW, Brown PM, Stavros FD, Brock TA, Dixon RA. Wu C, et al. Drugs Today (Barc). 2001 Jul;37(7):441-453. doi: 10.1358/dot.2001.37.7.844187. Drugs Today (Barc). 2001. PMID: 12750762
557 results