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Items: 1 to 20 of 120

1.

Identification of benzoxazin-3-one derivatives as novel, potent, and selective nonsteroidal mineralocorticoid receptor antagonists.

Hasui T, Matsunaga N, Ora T, Ohyabu N, Nishigaki N, Imura Y, Igata Y, Matsui H, Motoyaji T, Tanaka T, Habuka N, Sogabe S, Ono M, Siedem CS, Tang TP, Gauthier C, De Meese LA, Boyd SA, Fukumoto S.

J Med Chem. 2011 Dec 22;54(24):8616-31. doi: 10.1021/jm2011645. Epub 2011 Nov 29.

PMID:
22074142
2.

Discovery of 6-[5-(4-fluorophenyl)-3-methyl-pyrazol-4-yl]-benzoxazin-3-one derivatives as novel selective nonsteroidal mineralocorticoid receptor antagonists.

Hasui T, Ohyabu N, Ohra T, Fuji K, Sugimoto T, Fujimoto J, Asano K, Oosawa M, Shiotani S, Nishigaki N, Kusumoto K, Matsui H, Mizukami A, Habuka N, Sogabe S, Endo S, Ono M, Siedem CS, Tang TP, Gauthier C, De Meese LA, Boyd SA, Fukumoto S.

Bioorg Med Chem. 2014 Oct 1;22(19):5428-45. doi: 10.1016/j.bmc.2014.07.038. Epub 2014 Aug 12.

PMID:
25187277
3.

(S)-N-{3-[1-cyclopropyl-1-(2,4-difluoro-phenyl)-ethyl]-1H-indol-7-yl}-methanesulfonamide: a potent, nonsteroidal, functional antagonist of the mineralocorticoid receptor.

Bell MG, Gernert DL, Grese TA, Belvo MD, Borromeo PS, Kelley SA, Kennedy JH, Kolis SP, Lander PA, Richey R, Sharp VS, Stephenson GA, Williams JD, Yu H, Zimmerman KM, Steinberg MI, Jadhav PK.

J Med Chem. 2007 Dec 27;50(26):6443-5. Epub 2007 Nov 27.

PMID:
18038968
4.

Discovery of novel cyanodihydropyridines as potent mineralocorticoid receptor antagonists.

Arhancet GB, Woodard SS, Iyanar K, Case BL, Woerndle R, Dietz JD, Garland DJ, Collins JT, Payne MA, Blinn JR, Pomposiello SI, Hu X, Heron MI, Huang HC, Lee LF.

J Med Chem. 2010 Aug 26;53(16):5970-8. doi: 10.1021/jm100506y.

PMID:
20672820
5.

Discovery of (3S,3aR)-2-(3-chloro-4-cyanophenyl)-3-cyclopentyl-3,3a,4,5-tetrahydro-2H-benzo[g]indazole-7-carboxylic acid (PF-3882845), an orally efficacious mineralocorticoid receptor (MR) antagonist for hypertension and nephropathy.

Meyers MJ, Arhancet GB, Hockerman SL, Chen X, Long SA, Mahoney MW, Rico JR, Garland DJ, Blinn JR, Collins JT, Yang S, Huang HC, McGee KF, Wendling JM, Dietz JD, Payne MA, Homer BL, Heron MI, Reitz DB, Hu X.

J Med Chem. 2010 Aug 26;53(16):5979-6002. doi: 10.1021/jm100505n.

PMID:
20672822
6.

Design, synthesis, and structure-activity relationships of dihydrofuran-2-one and dihydropyrrol-2-one derivatives as novel benzoxazin-3-one-based mineralocorticoid receptor antagonists.

Hasui T, Ohra T, Ohyabu N, Asano K, Matsui H, Mizukami A, Habuka N, Sogabe S, Endo S, Siedem CS, Tang TP, Gauthier C, De Meese LA, Boyd SA, Fukumoto S.

Bioorg Med Chem. 2013 Oct 1;21(19):5983-94. doi: 10.1016/j.bmc.2013.07.043. Epub 2013 Jul 31.

PMID:
23958516
7.

Tetrahydroisoquinoline derivatives as highly selective and potent Rho kinase inhibitors.

Fang X, Yin Y, Chen YT, Yao L, Wang B, Cameron MD, Lin L, Khan S, Ruiz C, Schröter T, Grant W, Weiser A, Pocas J, Pachori A, Schürer S, Lograsso P, Feng Y.

J Med Chem. 2010 Aug 12;53(15):5727-37. doi: 10.1021/jm100579r.

PMID:
20684608
8.

Identification of (R)-6-(1-(4-cyano-3-methylphenyl)-5-cyclopentyl-4,5-dihydro-1H-pyrazol-3-yl)-2-methoxynicotinic acid, a highly potent and selective nonsteroidal mineralocorticoid receptor antagonist.

Casimiro-Garcia A, Piotrowski DW, Ambler C, Arhancet GB, Banker ME, Banks T, Boustany-Kari CM, Cai C, Chen X, Eudy R, Hepworth D, Hulford CA, Jennings SM, Loria PM, Meyers MJ, Petersen DN, Raheja NK, Sammons M, She L, Song K, Vrieze D, Wei L.

J Med Chem. 2014 May 22;57(10):4273-88. doi: 10.1021/jm500206r. Epub 2014 Apr 30.

PMID:
24738581
9.

Synthesis and structure-activity relationship of a new series of potent AT1 selective angiotensin II receptor antagonists: 5-(biphenyl-4-ylmethyl)pyrazoles.

Almansa C, Gómez LA, Cavalcanti FL, de Arriba AF, García-Rafanell J, Forn J.

J Med Chem. 1997 Feb 14;40(4):547-58.

PMID:
9046346
10.
11.

Optimization of potent, selective, and orally bioavailable pyrrolodinopyrimidine-containing inhibitors of heat shock protein 90. Identification of development candidate 2-amino-4-{4-chloro-2-[2-(4-fluoro-1H-pyrazol-1-yl)ethoxy]-6-methylphenyl}-N-(2,2-difluoropropyl)-5,7-dihydro-6H-pyrrolo[3,4-d]pyrimidine-6-carboxamide.

Zehnder L, Bennett M, Meng J, Huang B, Ninkovic S, Wang F, Braganza J, Tatlock J, Jewell T, Zhou JZ, Burke B, Wang J, Maegley K, Mehta PP, Yin MJ, Gajiwala KS, Hickey MJ, Yamazaki S, Smith E, Kang P, Sistla A, Dovalsantos E, Gehring MR, Kania R, Wythes M, Kung PP.

J Med Chem. 2011 May 12;54(9):3368-85. doi: 10.1021/jm200128m. Epub 2011 Apr 20.

PMID:
21438541
12.

New nonpeptide angiotensin II receptor antagonists. 2. Synthesis, biological properties, and structure-activity relationships of 2-alkyl-4-(biphenylylmethoxy)quinoline derivatives.

Bradbury RH, Allott CP, Dennis M, Fisher E, Major JS, Masek BB, Oldham AA, Pearce RJ, Rankine N, Revill JM, et al.

J Med Chem. 1992 Oct 30;35(22):4027-38.

PMID:
1433210
13.

Discovery of 4-{4-[3-(pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl}-N-(tetrahydro-2H- pyran-4-yl)benzamide (GW788388): a potent, selective, and orally active transforming growth factor-beta type I receptor inhibitor.

Gellibert F, de Gouville AC, Woolven J, Mathews N, Nguyen VL, Bertho-Ruault C, Patikis A, Grygielko ET, Laping NJ, Huet S.

J Med Chem. 2006 Apr 6;49(7):2210-21.

PMID:
16570917
14.

1,3-Dipropyl-8-(1-phenylacetamide-1H-pyrazol-3-yl)-xanthine derivatives as highly potent and selective human A(2B) adenosine receptor antagonists.

Tabrizi MA, Baraldi PG, Preti D, Romagnoli R, Saponaro G, Baraldi S, Moorman AR, Zaid AN, Varani K, Borea PA.

Bioorg Med Chem. 2008 Mar 1;16(5):2419-30. Epub 2007 Nov 28.

PMID:
18077171
15.

Novel potent and selective thrombin inhibitors based on a central 1,4-benzoxazin-3(4H)-one scaffold.

Ilas J, Tomasić T, Kikelj D.

J Med Chem. 2008 May 8;51(9):2863-7. doi: 10.1021/jm701622y. Epub 2008 Apr 16.

PMID:
18412326
16.

Novel 1,3-dipropyl-8-(1-heteroarylmethyl-1H-pyrazol-4-yl)-xanthine derivatives as high affinity and selective A2B adenosine receptor antagonists.

Elzein E, Kalla R, Li X, Perry T, Parkhill E, Palle V, Varkhedkar V, Gimbel A, Zeng D, Lustig D, Leung K, Zablocki J.

Bioorg Med Chem Lett. 2006 Jan 15;16(2):302-6. Epub 2005 Nov 4.

PMID:
16275090
17.
18.

Discovery of a novel class of phosphodiesterase 10A inhibitors and identification of clinical candidate 2-[4-(1-methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)-phenoxymethyl]-quinoline (PF-2545920) for the treatment of schizophrenia.

Verhoest PR, Chapin DS, Corman M, Fonseca K, Harms JF, Hou X, Marr ES, Menniti FS, Nelson F, O'Connor R, Pandit J, Proulx-Lafrance C, Schmidt AW, Schmidt CJ, Suiciak JA, Liras S.

J Med Chem. 2009 Aug 27;52(16):5188-96. doi: 10.1021/jm900521k.

PMID:
19630403
19.

Synthesis, structure-activity relationships, and biological properties of 1-heteroaryl-4-[omega-(1H-indol-3-yl)alkyl]piperazines, novel potential antipsychotics combining potent dopamine D2 receptor antagonism with potent serotonin reuptake inhibition.

Smid P, Coolen HK, Keizer HG, van Hes R, de Moes JP, den Hartog AP, Stork B, Plekkenpol RH, Niemann LC, Stroomer CN, Tulp MT, van Stuivenberg HH, McCreary AC, Hesselink MB, Herremans AH, Kruse CG.

J Med Chem. 2005 Nov 3;48(22):6855-69.

PMID:
16250644
20.

Design, synthesis and pharmacological screening of novel antihypertensive agents using hybrid approach.

Bhandari SV, Bothara KG, Patil AA, Chitre TS, Sarkate AP, Gore ST, Dangre SC, Khachane CV.

Bioorg Med Chem. 2009 Jan 1;17(1):390-400. doi: 10.1016/j.bmc.2008.10.032. Epub 2008 Oct 17.

PMID:
19036593

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