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Results: 1 to 20 of 100

1.

Mineralocorticoid receptor antagonists: identification of heterocyclic amide replacements in the oxazolidinedione series.

Cox JM, Chu HD, Yang C, Shen HC, Wu Z, Balsells J, Crespo A, Brown P, Zamlynny B, Wiltsie J, Clemas J, Gibson J, Contino L, Lisnock J, Zhou G, Garcia-Calvo M, Bateman T, Xu L, Tong X, Crook M, Sinclair P.

Bioorg Med Chem Lett. 2014 Apr 1;24(7):1681-4. doi: 10.1016/j.bmcl.2014.02.057. Epub 2014 Mar 1.

PMID:
24630411
[PubMed - in process]
2.

Discovery of novel oxazolidinedione derivatives as potent and selective mineralocorticoid receptor antagonists.

Yang C, Shen HC, Wu Z, Chu HD, Cox JM, Balsells J, Crespo A, Brown P, Zamlynny B, Wiltsie J, Clemas J, Gibson J, Contino L, Lisnock J, Zhou G, Garcia-Calvo M, Bateman T, Xu L, Tong X, Crook M, Sinclair P.

Bioorg Med Chem Lett. 2013 Aug 1;23(15):4388-92. doi: 10.1016/j.bmcl.2013.05.077. Epub 2013 Jun 4.

PMID:
23777778
[PubMed - indexed for MEDLINE]
3.

Structure-activity relationship studies of novel 3-oxazolidinedione-6-naphthyl-2-pyridinones as potent and orally bioavailable EP3 receptor antagonists.

Morales-Ramos ÁI, Li YH, Hilfiker M, Mecom JS, Eidam P, Shi D, Tseng PS, Brooks C, Zhang D, Wang N, Jaworski JP, Morrow D, Fries H, Edwards R, Jin J.

Bioorg Med Chem Lett. 2011 May 15;21(10):2806-11. doi: 10.1016/j.bmcl.2011.03.107. Epub 2011 Apr 5.

PMID:
21514150
[PubMed - indexed for MEDLINE]
4.

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
[PubMed - indexed for MEDLINE]
5.

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
[PubMed - in process]
6.

Novel 3-Oxazolidinedione-6-aryl-pyridinones as Potent, Selective, and Orally Active EP3 Receptor Antagonists.

Jin J, Morales-Ramos A, Eidam P, Mecom J, Li Y, Brooks C, Hilfiker M, Zhang D, Wang N, Shi D, Tseng PS, Wheless K, Budzik B, Evans K, Jaworski JP, Jugus J, Leon L, Wu C, Pullen M, Karamshi B, Rao P, Ward E, Laping N, Evans C, Leach C, Holt D, Su X, Morrow D, Fries H, Thorneloe K, Edwards R.

ACS Med Chem Lett. 2010 May 14;1(7):316-20. doi: 10.1021/ml100077x. eCollection 2010 Oct 14.

PMID:
24900213
[PubMed]
Free PMC Article
7.

Tryptophan-derived NK1 antagonists: conformationally constrained heterocyclic bioisosteres of the ester linkage.

Lewis RT, Macleod AM, Merchant KJ, Kelleher F, Sanderson I, Herbert RH, Cascieri MA, Sadowski S, Ball RG, Hoogsteen K.

J Med Chem. 1995 Mar 17;38(6):923-33.

PMID:
7699709
[PubMed - indexed for MEDLINE]
8.

Novel methylene-linked heterocyclic EP1 receptor antagonists.

Hall A, Bit RA, Brown SH, Chowdhury A, Giblin GM, Hurst DN, Kilford IR, Lewell X, Naylor A, Scoccitti T.

Bioorg Med Chem Lett. 2008 Mar 1;18(5):1592-7. doi: 10.1016/j.bmcl.2008.01.071. Epub 2008 Jan 19.

PMID:
18262416
[PubMed - indexed for MEDLINE]
9.

Evaluation of amide replacements in CCR5 antagonists as a means to increase intrinsic permeability. Part 2: SAR optimization and pharmacokinetic profile of a homologous azacyle series.

Wanner J, Chen L, Lemoine RC, Kondru R, Jekle A, Heilek G, deRosier A, Ji C, Berry PW, Rotstein DM.

Bioorg Med Chem Lett. 2010 Nov 15;20(22):6802-7. doi: 10.1016/j.bmcl.2010.08.118. Epub 2010 Sep 18.

PMID:
20855212
[PubMed - indexed for MEDLINE]
10.

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
[PubMed - indexed for MEDLINE]
11.

Identification of the first potent, selective and bioavailable PPARα antagonist.

Bravo Y, Baccei CS, Broadhead A, Bundey R, Chen A, Clark R, Correa L, Jacintho JD, Lorrain DS, Messmer D, Stebbins K, Prasit P, Stock N.

Bioorg Med Chem Lett. 2014 May 15;24(10):2267-72. doi: 10.1016/j.bmcl.2014.03.090. Epub 2014 Apr 4.

PMID:
24745969
[PubMed - indexed for MEDLINE]
12.

Rationale for the chemical development of angiotensin II receptor antagonists.

Wexler RR, Carini DJ, Duncia JV, Johnson AL, Wells GJ, Chiu AT, Wong PC, Timmermans PB.

Am J Hypertens. 1992 Dec;5(12 Pt 2):209S-220S. Review.

PMID:
1290616
[PubMed - indexed for MEDLINE]
13.

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
[PubMed - indexed for MEDLINE]
14.

Heterocyclic acetamide and benzamide derivatives as potent and selective beta3-adrenergic receptor agonists with improved rodent pharmacokinetic profiles.

Goble SD, Wang L, Howell KL, Bansal A, Berger R, Brockunier L, DiSalvo J, Feighner S, Harper B, He J, Hurley A, Hreniuk D, Parmee E, Robbins M, Salituro G, Sanfiz A, Streckfuss E, Watkins E, Weber AE, Struthers M, Edmondson SD.

Bioorg Med Chem Lett. 2010 Mar 15;20(6):1895-9. doi: 10.1016/j.bmcl.2010.01.130. Epub 2010 Feb 4.

PMID:
20181479
[PubMed - indexed for MEDLINE]
15.

Amide bond replacements incorporated into CCK-B selective "dipeptoids".

Fincham CI, Higginbottom M, Hill DR, Horwell DC, O'Toole JC, Ratcliffe GS, Rees DC, Roberts E.

J Med Chem. 1992 Apr 17;35(8):1472-84.

PMID:
1573640
[PubMed - indexed for MEDLINE]
16.

Discovery and SAR of a novel series of metabotropic glutamate receptor 5 positive allosteric modulators with high ligand efficiency.

Turlington M, Noetzel MJ, Bridges TM, Vinson PN, Steckler T, Lavreysen H, Mackie C, Bartolomé-Nebreda JM, Conde-Ceide S, Tong HM, Macdonald GJ, Daniels JS, Jones CK, Niswender CM, Conn PJ, Lindsley CW, Stauffer SR.

Bioorg Med Chem Lett. 2014 Aug 1;24(15):3641-6. doi: 10.1016/j.bmcl.2014.04.087. Epub 2014 May 2.

PMID:
24961642
[PubMed - in process]
17.

Discovery of BAY 94-8862: a nonsteroidal antagonist of the mineralocorticoid receptor for the treatment of cardiorenal diseases.

Bärfacker L, Kuhl A, Hillisch A, Grosser R, Figueroa-Pérez S, Heckroth H, Nitsche A, Ergüden JK, Gielen-Haertwig H, Schlemmer KH, Mittendorf J, Paulsen H, Platzek J, Kolkhof P.

ChemMedChem. 2012 Aug;7(8):1385-403. doi: 10.1002/cmdc.201200081. Epub 2012 Jul 12.

PMID:
22791416
[PubMed - indexed for MEDLINE]
18.

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
[PubMed - indexed for MEDLINE]
19.

Discovery of a series of potent and selective human H4 antagonists using ligand efficiency and libraries to explore structure-activity relationship (SAR).

Masood MA, Selby MD, Bell AS, Mansfield AC, Gardner M, Smith GF, Lane C, Kenyon-Edwards H, Osborne R, Jones RM, Liu WL, Brown CD, Clarke N, Perrucio F, Mowbray CE.

Bioorg Med Chem Lett. 2011 Nov 1;21(21):6591-5. doi: 10.1016/j.bmcl.2011.07.114. Epub 2011 Aug 27.

PMID:
21955944
[PubMed - indexed for MEDLINE]
20.

Novel heterocyclic trans olefin analogues of N-{4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butyl}arylcarboxamides as selective probes with high affinity for the dopamine D3 receptor.

Grundt P, Carlson EE, Cao J, Bennett CJ, McElveen E, Taylor M, Luedtke RR, Newman AH.

J Med Chem. 2005 Feb 10;48(3):839-48.

PMID:
15689168
[PubMed - indexed for MEDLINE]
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