Metabolism study and biological evaluation of bosentan derivatives.
Lepri S, Goracci L, Valeri A, Cruciani G.
Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2016.06.006 PUBLIKATIONSREGISTRET
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18 träffarThe discovery of N-[5-(4-bromophenyl)-6-[2-[(5-bromo-2-pyrimidinyl)oxy]ethoxy]-4-pyrimidinyl]-N'-propylsulfamide (Macitentan), an orally active, potent dual endothelin receptor antagonist.
Bolli MH, Boss C, Binkert C, Buchmann S, Bur D, Hess P, Iglarz M, Meyer S, Rein J, Rey M, Treiber A, Clozel M, Fischli W, Weller T.
J Med Chem · journal article · DOI 10.1021/jm3009103Synthesis and pharmacological activity of 1,3,6-trisubstituted-4-oxo-1,4-dihydroquinoline-2-carboxylic acids as selective ET(A) antagonists.
Patel HJ, Olgun N, Lengyel I, Reznik S, Stephani RA.
Bioorg Med Chem Lett · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmcl.2010.08.074Chemical function based pharmacophore generation of endothelin-A selective receptor antagonists.
Funk OF, Kettmann V, Drimal J, Langer T.
J Med Chem · journal article · DOI 10.1021/jm031041jDiscovery, 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.
J Med Chem · clinical trial; clinical trial, phase i; randomized controlled trial; journal article · DOI 10.1021/jm030528pCarbazolothiophene-2-carboxylic acid derivatives as endothelin receptor antagonists.
Babu G, Yu HM, Yang SM, Fang JM.
Bioorg Med Chem Lett · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmcl.2003.12.067Characterization of the drug resistance and transport properties of multidrug resistance protein 6 (MRP6, ABCC6).
Belinsky MG, Chen ZS, Shchaveleva I, Zeng H, Kruh GD.
Cancer Res · research support, u.s. gov't, p.h.s.; research support, non-u.s. gov't; journal articleIdentification of a novel human organic anion transporting polypeptide as a high affinity thyroxine transporter.
Pizzagalli F, Hagenbuch B, Stieger B, Klenk U, Folkers G, Meier PJ.
Mol Endocrinol · research support, non-u.s. gov't; journal article · DOI 10.1210/me.2001-0309Functional characterization of the mouse organic-anion-transporting polypeptide 2.
van Montfoort JE, Schmid TE, Adler ID, Meier PJ, Hagenbuch B.
Biochim Biophys Acta · research support, non-u.s. gov't; journal article · DOI 10.1016/s0005-2736(02)00445-5Localization of organic anion transporting polypeptide 4 (Oatp4) in rat liver and comparison of its substrate specificity with Oatp1, Oatp2 and Oatp3.
Cattori V, van Montfoort JE, Stieger B, Landmann L, Meijer DK, Winterhalter KH, Meier PJ, Hagenbuch B.
Pflugers Arch · comparative study; research support, non-u.s. gov't; journal article · DOI 10.1007/s004240100697Organic anion-transporting polypeptide B (OATP-B) and its functional comparison with three other OATPs of human liver.
Kullak-Ublick GA, Ismair MG, Stieger B, Landmann L, Huber R, Pizzagalli F, Fattinger K, Meier PJ, Hagenbuch B.
Gastroenterology · comparative study; research support, non-u.s. gov't; journal article · DOI 10.1053/gast.2001.21176Transport function and hepatocellular localization of mrp6 in rat liver.
Madon J, Hagenbuch B, Landmann L, Meier PJ, Stieger B.
Mol Pharmacol · research support, non-u.s. gov't; journal article · DOI 10.1124/mol.57.3.634Carrier-mediated hepatic uptake of peptidic endothelin antagonists in rats.
Akhteruzzaman S, Kato Y, Kouzuki H, Suzuki H, Hisaka A, Stieger B, Meier PJ, Sugiyama Y.
J Pharmacol Exp Ther · research support, non-u.s. gov't; journal article · DOI 10.1016/s0022-3565(24)35012-8Localization and function of the organic anion-transporting polypeptide Oatp2 in rat liver.
Reichel C, Gao B, Van Montfoort J, Cattori V, Rahner C, Hagenbuch B, Stieger B, Kamisako T, Meier PJ.
Gastroenterology · comparative study; research support, non-u.s. gov't; journal article · DOI 10.1016/s0016-5085(99)70463-4Primary active transport of peptidic endothelin antagonists by rat hepatic canalicular membrane.
Akhteruzzaman S, Kato Y, Hisaka A, Sugiyama Y.
J Pharmacol Exp Ther · research support, non-u.s. gov't; journal article · DOI 10.1016/s0022-3565(24)37992-3Biphenylsulfonamide endothelin antagonists: structure-activity relationships of a series of mono- and disubstituted analogues and pharmacology of the orally active endothelin antagonist 2'-amino-N- (3,4-dimethyl-5-isoxazolyl)-4'-(2-methylpropyl)[1, 1'-biphenyl]-2-sulfonamide (BMS-187308).
Murugesan N, Gu Z, Stein PD, Bisaha S, Spergel S, Girotra R, Lee VG, Lloyd J, Misra RN, Schmidt J, Mathur A, Stratton L, Kelly YF, Bird E, Waldron T, Liu EC, Zhang R, Lee H, Serafino R, Abboa-Offei B, Mathers P, Giancarli M, Seymour AA, Webb ML, Hunt JT.
J Med Chem · journal article · DOI 10.1021/jm970872kSelective endothelin A receptor antagonists. 3. Discovery and structure-activity relationships of a series of 4-phenoxybutanoic acid derivatives.
Astles PC, Brealey C, Brown TJ, Facchini V, Handscombe C, Harris NV, McCarthy C, McLay IM, Porter B, Roach AG, Sargent C, Smith C, Walsh RJ.
J Med Chem · journal article · DOI 10.1021/jm9707131Endothelin: a new challenge.
Doherty AM.
J Med Chem · review; journal article · DOI 10.1021/jm00087a001