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Results: 1 to 20 of 118

1.

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]
2.

Synthesis of proline analogues as potent and selective cathepsin S inhibitors.

Kim M, Jeon J, Song J, Suh KH, Kim YH, Min KH, Lee KO.

Bioorg Med Chem Lett. 2013 Jun 1;23(11):3140-4. doi: 10.1016/j.bmcl.2013.04.023. Epub 2013 Apr 16.

PMID:
23639544
[PubMed - indexed for MEDLINE]
3.

Discovery of novel fatty acid synthase (FAS) inhibitors based on the structure of ketoaceyl synthase (KS) domain.

Zeng XF, Li WW, Fan HJ, Wang XY, Ji P, Wang ZR, Ma S, Li LL, Ma XF, Yang SY.

Bioorg Med Chem Lett. 2011 Aug 15;21(16):4742-4. doi: 10.1016/j.bmcl.2011.06.075. Epub 2011 Jun 23.

PMID:
21752639
[PubMed - indexed for MEDLINE]
4.

In vitro phase I cytochrome P450 metabolism, permeability and pharmacokinetics of SB639, a novel histone deacetylase inhibitor in preclinical species.

Venkatesh PR, Goh E, Zeng P, New LS, Xin L, Pasha MK, Sangthongpitag K, Yeo P, Kantharaj E.

Biol Pharm Bull. 2007 May;30(5):1021-4.

PMID:
17473456
[PubMed - indexed for MEDLINE]
Free Article
5.

Discovery and characterization of a novel potent, selective and orally active inhibitor for mammalian ELOVL6.

Shimamura K, Nagumo A, Miyamoto Y, Kitazawa H, Kanesaka M, Yoshimoto R, Aragane K, Morita N, Ohe T, Takahashi T, Nagase T, Sato N, Tokita S.

Eur J Pharmacol. 2010 Mar 25;630(1-3):34-41. doi: 10.1016/j.ejphar.2009.12.033. Epub 2010 Jan 4.

PMID:
20045404
[PubMed - indexed for MEDLINE]
6.

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]
7.

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]
8.

Identification and optimisation of a series of substituted 5-pyridin-2-yl-thiophene-2-hydroxamic acids as potent histone deacetylase (HDAC) inhibitors.

Price S, Bordogna W, Braganza R, Bull RJ, Dyke HJ, Gardan S, Gill M, Harris NV, Heald RA, van den Heuvel M, Lockey PM, Lloyd J, Molina AG, Roach AG, Roussel F, Sutton JM, White AB.

Bioorg Med Chem Lett. 2007 Jan 15;17(2):363-9. Epub 2006 Oct 24.

PMID:
17107790
[PubMed - indexed for MEDLINE]
9.

Beta-lactam congeners of orlistat as inhibitors of fatty acid synthase.

Zhang W, Richardson RD, Chamni S, Smith JW, Romo D.

Bioorg Med Chem Lett. 2008 Apr 1;18(7):2491-4. doi: 10.1016/j.bmcl.2008.02.043. Epub 2008 Feb 19.

PMID:
18343106
[PubMed - indexed for MEDLINE]
10.

Novel fatty acid synthase (FAS) inhibitors: design, synthesis, biological evaluation, and molecular docking studies.

Wang X, Lin J, Chen Y, Zhong W, Zhao G, Liu H, Li S, Wang L, Li S.

Bioorg Med Chem. 2009 Mar 1;17(5):1898-904. doi: 10.1016/j.bmc.2009.01.050. Epub 2009 Jan 29.

PMID:
19223187
[PubMed - indexed for MEDLINE]
11.

Discovery and optimization of novel fatty acid transport protein 1 (FATP1) inhibitors.

Matsufuji T, Ikeda M, Naito A, Hirouchi M, Takakusa H, Kanda S, Izumi M, Harada J, Shinozuka T.

Bioorg Med Chem Lett. 2012 Aug 1;22(15):5067-70. doi: 10.1016/j.bmcl.2012.05.130. Epub 2012 Jun 19.

PMID:
22749869
[PubMed - indexed for MEDLINE]
12.

5,5-Dimethyl-3-(5-methyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazol-4-yl)-1-phenyl-3-(trifluoromethyl)-3,5,6,7-tetrahydro-1H-indole-2,4-dione, a potent inhibitor for mammalian elongase of long-chain fatty acids family 6: examination of its potential utility as a pharmacological tool.

Shimamura K, Kitazawa H, Miyamoto Y, Kanesaka M, Nagumo A, Yoshimoto R, Aragane K, Morita N, Ohe T, Takahashi T, Nagase T, Sato N, Tokita S.

J Pharmacol Exp Ther. 2009 Jul;330(1):249-56. doi: 10.1124/jpet.109.150854. Epub 2009 Apr 9.

PMID:
19359527
[PubMed - indexed for MEDLINE]
Free Article
13.

Discovery of GSK837149A, an inhibitor of human fatty acid synthase targeting the beta-ketoacyl reductase reaction.

Vázquez MJ, Leavens W, Liu R, Rodríguez B, Read M, Richards S, Winegar D, Domínguez JM.

FEBS J. 2008 Apr;275(7):1556-67. doi: 10.1111/j.1742-4658.2008.06314.x. Epub 2008 Feb 25.

PMID:
18312417
[PubMed - indexed for MEDLINE]
14.

3-Aryl-4-hydroxyquinolin-2(1H)-one derivatives as type I fatty acid synthase inhibitors.

Rivkin A, Kim YR, Goulet MT, Bays N, Hill AD, Kariv I, Krauss S, Ginanni N, Strack PR, Kohl NE, Chung CC, Varnerin JP, Goudreau PN, Chang A, Tota MR, Munoz B.

Bioorg Med Chem Lett. 2006 Sep 1;16(17):4620-3. Epub 2006 Jun 19.

PMID:
16784844
[PubMed - indexed for MEDLINE]
15.

Potent and novel 11β-HSD1 inhibitors identified from shape and docking based virtual screening.

Xia G, Xue M, Liu L, Yu J, Liu H, Li P, Wang J, Li Y, Xiong B, Shen J.

Bioorg Med Chem Lett. 2011 Oct 1;21(19):5739-44. doi: 10.1016/j.bmcl.2011.08.019. Epub 2011 Aug 8.

PMID:
21873057
[PubMed - indexed for MEDLINE]
16.

Preclinical pharmacokinetics and metabolism of 6-(4-(2,5-difluorophenyl)oxazol-5-yl)-3-isopropyl-[1,2,4]-triazolo[4,3-a]pyridine, a novel and selective p38alpha inhibitor: identification of an active metabolite in preclinical species and human liver microsomes.

Kalgutkar AS, Hatch HL, Kosea F, Nguyen HT, Choo EF, McClure KF, Taylor TJ, Henne KR, Kuperman AV, Dombroski MA, Letavic MA.

Biopharm Drug Dispos. 2006 Nov;27(8):371-86.

PMID:
16944451
[PubMed - indexed for MEDLINE]
17.

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
18.

Discovery of a novel class of potent and orally bioavailable sphingosine 1-phosphate receptor 1 antagonists.

Ibrahim MA, Johnson HW, Jeong JW, Lewis GL, Shi X, Noguchi RT, Williams M, Leahy JW, Nuss JM, Woolfrey J, Banica M, Bentzien F, Chou YC, Gibson A, Heald N, Lamb P, Mattheakis L, Matthews D, Shipway A, Wu X, Zhang W, Zhou S, Shankar G.

J Med Chem. 2012 Feb 9;55(3):1368-81. doi: 10.1021/jm201533b. Epub 2012 Jan 24.

PMID:
22214363
[PubMed - indexed for MEDLINE]
19.

Indole naphthyridinones as inhibitors of bacterial enoyl-ACP reductases FabI and FabK.

Seefeld MA, Miller WH, Newlander KA, Burgess WJ, DeWolf WE Jr, Elkins PA, Head MS, Jakas DR, Janson CA, Keller PM, Manley PJ, Moore TD, Payne DJ, Pearson S, Polizzi BJ, Qiu X, Rittenhouse SF, Uzinskas IN, Wallis NG, Huffman WF.

J Med Chem. 2003 Apr 24;46(9):1627-35.

PMID:
12699381
[PubMed - indexed for MEDLINE]
20.

Discovery and structure-activity relationships of pentanedioic acid diamides as potent inhibitors of 11beta-hydroxysteroid dehydrogenase type I.

Roche D, Carniato D, Leriche C, Lepifre F, Christmann-Franck S, Graedler U, Charon C, Bozec S, Doare L, Schmidlin F, Lecomte M, Valeur E.

Bioorg Med Chem Lett. 2009 May 15;19(10):2674-8. doi: 10.1016/j.bmcl.2009.03.140. Epub 2009 Apr 1.

PMID:
19395260
[PubMed - indexed for MEDLINE]

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