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Page 1
Identification of Reversible Small Molecule Inhibitors of Endothelial Lipase (EL) That Demonstrate HDL-C Increase In Vivo.
Tora G, Kim SH, Pi Z, Johnson JA, Jiang J, Phillips M, Lloyd J, Abell LM, Lu H, Locke G, Adam LP, Taylor DS, Yin X, Behnia K, Zhao L, Yang R, Basso M, Caporuscio C, Chen AY, Liu E, Kirshgessner T, Onorato JM, Ryan C, Traeger SC, Gordon D, Wexler RR, Finlay HJ. Tora G, et al. Among authors: liu e. J Med Chem. 2020 Feb 27;63(4):1660-1670. doi: 10.1021/acs.jmedchem.9b01831. Epub 2020 Feb 11. J Med Chem. 2020. PMID: 31990537
Identification of substituted benzothiazole sulfones as potent and selective inhibitors of endothelial lipase.
Kim SH, Johnson JA, Jiang J, Parkhurst B, Phillips M, Pi Z, Qiao JX, Tora G, Ye Chen A, Liu E, Yin X, Yang R, Zhao L, Taylor DS, Basso M, Behnia K, Onorato J, Chen XQ, Abell LM, Lu H, Locke G, Caporuscio C, Adam LP, Gordon D, Wexler RR, Finlay HJ. Kim SH, et al. Among authors: liu e. Bioorg Med Chem Lett. 2019 Aug 1;29(15):1918-1921. doi: 10.1016/j.bmcl.2019.05.048. Epub 2019 May 25. Bioorg Med Chem Lett. 2019. PMID: 31176700
Corrigendum to "Identification of substituted benzothiazole sulfones as potent and selective inhibitors of endothelial lipase" [Bioorg. Med. Chem. Lett. 29 (2019) 1918-1921].
Kim SH, Johnson JA, Jiang J, Parkhurst B, Phillips M, Pi Z, Qiao JX, Tora G, Ye Chen A, Liu E, Yin X, Yang R, Zhao L, Taylor DS, Basso M, Behnia K, Onorato J, Chen XQ, Abell LM, Lu H, Locke G, Caporuscio C, Adam LP, Gordon D, Wexler RR, Finlay HJ. Kim SH, et al. Among authors: liu e. Bioorg Med Chem Lett. 2019 Sep 1;29(17):2525. doi: 10.1016/j.bmcl.2019.07.032. Epub 2019 Jul 25. Bioorg Med Chem Lett. 2019. PMID: 31353296 No abstract available.
Conformationally constrained ortho-anilino diaryl ureas: discovery of 1-(2-(1'-neopentylspiro[indoline-3,4'-piperidine]-1-yl)phenyl)-3-(4-(trifluoromethoxy)phenyl)urea, a potent, selective, and bioavailable P2Y1 antagonist.
Qiao JX, Wang TC, Ruel R, Thibeault C, L'Heureux A, Schumacher WA, Spronk SA, Hiebert S, Bouthillier G, Lloyd J, Pi Z, Schnur DM, Abell LM, Hua J, Price LA, Liu E, Wu Q, Steinbacher TE, Bostwick JS, Chang M, Zheng J, Gao Q, Ma B, McDonnell PA, Huang CS, Rehfuss R, Wexler RR, Lam PY. Qiao JX, et al. Among authors: liu e. J Med Chem. 2013 Nov 27;56(22):9275-95. doi: 10.1021/jm4013906. Epub 2013 Nov 12. J Med Chem. 2013. PMID: 24164581
Discovery of nonbenzamidine factor VIIa inhibitors using a biaryl acid scaffold.
Bolton SA, Sutton JC, Anumula R, Bisacchi GS, Jacobson B, Slusarchyk WA, Treuner UD, Wu SC, Zhao G, Pi Z, Sheriff S, Smirk RA, Bisaha S, Cheney DL, Wei A, Schumacher WA, Hartl KS, Liu E, Zahler R, Seiler SM. Bolton SA, et al. Among authors: liu e. Bioorg Med Chem Lett. 2013 Sep 15;23(18):5239-43. doi: 10.1016/j.bmcl.2013.06.028. Epub 2013 Jun 20. Bioorg Med Chem Lett. 2013. PMID: 23927973
Biphenylsulfonamide 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, et al. Murugesan N, et al. Among authors: liu ec. J Med Chem. 1998 Dec 17;41(26):5198-218. doi: 10.1021/jm970872k. J Med Chem. 1998. PMID: 9857090
Design, structure-activity relationships, X-ray crystal structure, and energetic contributions of a critical P1 pharmacophore: 3-chloroindole-7-yl-based factor Xa inhibitors.
Shi Y, Sitkoff D, Zhang J, Klei HE, Kish K, Liu EC, Hartl KS, Seiler SM, Chang M, Huang C, Youssef S, Steinbacher TE, Schumacher WA, Grazier N, Pudzianowski A, Apedo A, Discenza L, Yanchunas J, Stein PD, Atwal KS. Shi Y, et al. Among authors: liu ec. J Med Chem. 2008 Dec 11;51(23):7541-51. doi: 10.1021/jm800855x. J Med Chem. 2008. PMID: 18998662
Biphenylsulfonamide endothelin receptor antagonists. 4. Discovery of N-[[2'-[[(4,5-dimethyl-3-isoxazolyl)amino]sulfonyl]-4-(2-oxazolyl)[1,1'-biphenyl]- 2-yl]methyl]-N,3,3-trimethylbutanamide (BMS-207940), a highly potent and orally active ET(A) selective antagonist.
Murugesan N, Gu Z, Spergel S, Young M, Chen P, Mathur A, Leith L, Hermsmeier M, Liu EC, Zhang R, Bird E, Waldron T, Marino A, Koplowitz B, Humphreys WG, Chong S, Morrison RA, Webb ML, Moreland S, Trippodo N, Barrish JC. Murugesan N, et al. Among authors: liu ec. J Med Chem. 2003 Jan 2;46(1):125-37. doi: 10.1021/jm020289q. J Med Chem. 2003. PMID: 12502366
4,301 results