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Results: 1 to 20 of 114

1.

Novel benzoxazole inhibitors of mPGES-1.

Kablaoui N, Patel S, Shao J, Demian D, Hoffmaster K, Berlioz F, Vazquez ML, Moore WM, Nugent RA.

Bioorg Med Chem Lett. 2013 Feb 1;23(3):907-11. doi: 10.1016/j.bmcl.2012.10.040. Epub 2012 Oct 16.

PMID:
23266122
[PubMed - indexed for MEDLINE]
2.

Synthesis and biological evaluation of substituted benzoxazoles as inhibitors of mPGES-1: use of a conformation-based hypothesis to facilitate compound design.

Walker DP, Arhancet GB, Lu HF, Heasley SE, Metz S, Kablaoui NM, Franco FM, Hanau CE, Scholten JA, Springer JR, Fobian YM, Carter JS, Xing L, Yang S, Shaffer AF, Jerome GM, Baratta MT, Moore WM, Vazquez ML.

Bioorg Med Chem Lett. 2013 Feb 15;23(4):1120-6. doi: 10.1016/j.bmcl.2012.11.107. Epub 2012 Dec 12.

PMID:
23298810
[PubMed - indexed for MEDLINE]
3.

Selective inducible microsomal prostaglandin E(2) synthase-1 (mPGES-1) inhibitors derived from an oxicam template.

Wang J, Limburg D, Carter J, Mbalaviele G, Gierse J, Vazquez M.

Bioorg Med Chem Lett. 2010 Mar 1;20(5):1604-9. doi: 10.1016/j.bmcl.2010.01.060. Epub 2010 Jan 25.

PMID:
20144869
[PubMed - indexed for MEDLINE]
4.

Identification of novel mPGES-1 inhibitors through screening of a chemical library.

Park SJ, Han SG, Ahsan HM, Lee K, Lee JY, Shin JS, Lee KT, Kang NS, Yu YG.

Bioorg Med Chem Lett. 2012 Dec 15;22(24):7335-9. doi: 10.1016/j.bmcl.2012.10.085. Epub 2012 Oct 23.

PMID:
23147075
[PubMed - indexed for MEDLINE]
Free Article
5.

Discovery and SAR of PF-4693627, a potent, selective and orally bioavailable mPGES-1 inhibitor for the potential treatment of inflammation.

Arhancet GB, Walker DP, Metz S, Fobian YM, Heasley SE, Carter JS, Springer JR, Jones DE, Hayes MJ, Shaffer AF, Jerome GM, Baratta MT, Zweifel B, Moore WM, Masferrer JL, Vazquez ML.

Bioorg Med Chem Lett. 2013 Feb 15;23(4):1114-9. doi: 10.1016/j.bmcl.2012.11.109. Epub 2012 Dec 6.

PMID:
23260349
[PubMed - indexed for MEDLINE]
6.

Fragment-based discovery of novel and selective mPGES-1 inhibitors Part 1: identification of sulfonamido-1,2,3-triazole-4,5-dicarboxylic acid.

Lee K, Pham VC, Choi MJ, Kim KJ, Lee KT, Han SG, Yu YG, Lee JY.

Bioorg Med Chem Lett. 2013 Jan 1;23(1):75-80. doi: 10.1016/j.bmcl.2012.11.019. Epub 2012 Nov 15.

PMID:
23218602
[PubMed - indexed for MEDLINE]
7.

Effects of AF3442 [N-(9-ethyl-9H-carbazol-3-yl)-2-(trifluoromethyl)benzamide], a novel inhibitor of human microsomal prostaglandin E synthase-1, on prostanoid biosynthesis in human monocytes in vitro.

Bruno A, Di Francesco L, Coletta I, Mangano G, Alisi MA, Polenzani L, Milanese C, Anzellotti P, Ricciotti E, Dovizio M, Di Francesco A, Tacconelli S, Capone ML, Patrignani P.

Biochem Pharmacol. 2010 Apr 1;79(7):974-81. doi: 10.1016/j.bcp.2009.11.011. Epub 2009 Nov 27.

PMID:
19925781
[PubMed - indexed for MEDLINE]
8.

Distinction of microsomal prostaglandin E synthase-1 (mPGES-1) inhibition from cyclooxygenase-2 inhibition in cells using a novel, selective mPGES-1 inhibitor.

Mbalaviele G, Pauley AM, Shaffer AF, Zweifel BS, Mathialagan S, Mnich SJ, Nemirovskiy OV, Carter J, Gierse JK, Wang JL, Vazquez ML, Moore WM, Masferrer JL.

Biochem Pharmacol. 2010 May 15;79(10):1445-54. doi: 10.1016/j.bcp.2010.01.003. Epub 2010 Jan 11.

PMID:
20067770
[PubMed - indexed for MEDLINE]
9.

Structure-activity relationship of nonacidic quinazolinone inhibitors of human microsomal prostaglandin synthase 1 (mPGES 1).

Rörsch F, Buscató E, Deckmann K, Schneider G, Schubert-Zsilavecz M, Geisslinger G, Proschak E, Grösch S.

J Med Chem. 2012 Apr 26;55(8):3792-803. doi: 10.1021/jm201687d. Epub 2012 Apr 11.

PMID:
22449023
[PubMed - indexed for MEDLINE]
10.

Synthesis and SAR study of imidazoquinolines as a novel structural class of microsomal prostaglandin E₂ synthase-1 inhibitors.

Shiro T, Takahashi H, Kakiguchi K, Inoue Y, Masuda K, Nagata H, Tobe M.

Bioorg Med Chem Lett. 2012 Jan 1;22(1):285-8. doi: 10.1016/j.bmcl.2011.11.015. Epub 2011 Nov 11.

PMID:
22137787
[PubMed - indexed for MEDLINE]
11.

Arylpyrrolizines as inhibitors of microsomal prostaglandin E2 synthase-1 (mPGES-1) or as dual inhibitors of mPGES-1 and 5-lipoxygenase (5-LOX).

Liedtke AJ, Keck PR, Lehmann F, Koeberle A, Werz O, Laufer SA.

J Med Chem. 2009 Aug 13;52(15):4968-72. doi: 10.1021/jm900481c.

PMID:
19719242
[PubMed - indexed for MEDLINE]
12.

Identification of new γ-hydroxybutenolides that preferentially inhibit the activity of mPGES-1.

De Simone R, Bruno I, Riccio R, Stadler K, Bauer J, Schaible AM, Laufer S, Werz O.

Bioorg Med Chem. 2012 Aug 15;20(16):5012-6. doi: 10.1016/j.bmc.2012.06.032. Epub 2012 Jun 23.

PMID:
22795900
[PubMed - indexed for MEDLINE]
13.

Discovery of benzo[g]indol-3-carboxylates as potent inhibitors of microsomal prostaglandin E(2) synthase-1.

Koeberle A, Haberl EM, Rossi A, Pergola C, Dehm F, Northoff H, Troschuetz R, Sautebin L, Werz O.

Bioorg Med Chem. 2009 Dec 1;17(23):7924-32. doi: 10.1016/j.bmc.2009.10.025. Epub 2009 Oct 31.

PMID:
19884011
[PubMed - indexed for MEDLINE]
14.

Design and synthesis of 2-substituted benzoxazoles as novel PTP1B inhibitors.

Chandrasekharappa AP, Badiger SE, Dubey PK, Panigrahi SK, Manukonda SR.

Bioorg Med Chem Lett. 2013 May 1;23(9):2579-84. doi: 10.1016/j.bmcl.2013.02.109. Epub 2013 Mar 7.

PMID:
23528300
[PubMed - indexed for MEDLINE]
15.

Optimization of benzoxazole-based inhibitors of Cryptosporidium parvum inosine 5'-monophosphate dehydrogenase.

Gorla SK, Kavitha M, Zhang M, Chin JE, Liu X, Striepen B, Makowska-Grzyska M, Kim Y, Joachimiak A, Hedstrom L, Cuny GD.

J Med Chem. 2013 May 23;56(10):4028-43. doi: 10.1021/jm400241j. Epub 2013 May 13.

PMID:
23668331
[PubMed - indexed for MEDLINE]
Free PMC Article
16.

Design, synthesis and antifungal activity of isosteric analogues of benzoheterocyclic N-myristoyltransferase inhibitors.

Sheng C, Xu H, Wang W, Cao Y, Dong G, Wang S, Che X, Ji H, Miao Z, Yao J, Zhang W.

Eur J Med Chem. 2010 Sep;45(9):3531-40. doi: 10.1016/j.ejmech.2010.03.007. Epub 2010 Mar 12.

PMID:
20615585
[PubMed - indexed for MEDLINE]
17.

SAR studies on a series of N-benzyl-4-heteroaryl-1-(phenylsulfonyl)piperazine-2-carboxamides: potent inhibitors of the polymerase enzyme (NS5B) of the hepatitis C virus.

Gentles RG, Ding M, Zheng X, Chupak L, Poss MA, Beno BR, Pelosi L, Liu M, Lemm J, Wang YK, Roberts S, Gao M, Kadow J.

Bioorg Med Chem Lett. 2011 May 15;21(10):3142-7. doi: 10.1016/j.bmcl.2011.03.008. Epub 2011 Mar 6.

PMID:
21450465
[PubMed - indexed for MEDLINE]
18.

2-(2-Aminothiazol-4-yl)pyrrolidine-based tartrate diamides as potent, selective and orally bioavailable TACE inhibitors.

Dai C, Li D, Popovici-Muller J, Zhao L, Girijavallabhan VM, Rosner KE, Lavey BJ, Rizvi R, Shankar BB, Wong MK, Guo Z, Orth P, Strickland CO, Sun J, Niu X, Chen S, Kozlowski JA, Lundell DJ, Piwinski JJ, Shih NY, Siddiqui MA.

Bioorg Med Chem Lett. 2011 May 15;21(10):3172-6. doi: 10.1016/j.bmcl.2011.01.002. Epub 2011 Jan 6.

PMID:
21458257
[PubMed - indexed for MEDLINE]
19.

The molecular pharmacology and in vivo activity of 2-(4-chloro-6-(2,3-dimethylphenylamino)pyrimidin-2-ylthio)octanoic acid (YS121), a dual inhibitor of microsomal prostaglandin E2 synthase-1 and 5-lipoxygenase.

Koeberle A, Rossi A, Zettl H, Pergola C, Dehm F, Bauer J, Greiner C, Reckel S, Hoernig C, Northoff H, Bernhard F, Dötsch V, Sautebin L, Schubert-Zsilavecz M, Werz O.

J Pharmacol Exp Ther. 2010 Mar;332(3):840-8. doi: 10.1124/jpet.109.160663. Epub 2009 Nov 24.

PMID:
19934399
[PubMed - indexed for MEDLINE]
Free Article
20.

Discovery of BI 99179, a potent and selective inhibitor of type I fatty acid synthase with central exposure.

Kley JT, Mack J, Hamilton B, Scheuerer S, Redemann N.

Bioorg Med Chem Lett. 2011 Oct 1;21(19):5924-7. doi: 10.1016/j.bmcl.2011.07.083. Epub 2011 Aug 9.

PMID:
21873051
[PubMed - indexed for MEDLINE]

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