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Items: 1 to 20 of 113

1.

Synthesis and evaluation of cyclohexane carboxylic acid head group containing isoxazole and thiazole analogs as DGAT1 inhibitors.

Kandre S, Bhagat PR, Reddy MM, Dalal R, Dixit A, Deshmukh NJ, Anthony J, Bose J, Anupindi R, Sharma R, Gupte A.

Eur J Med Chem. 2014 May 22;79:203-15. doi: 10.1016/j.ejmech.2014.03.077. Epub 2014 Mar 28.

PMID:
24735646
2.

Evaluation of thiazole containing biaryl analogs as diacylglycerol acyltransferase 1 (DGAT1) inhibitors.

Kadam KS, Jadhav RD, Kandre S, Guha T, Reddy MM, Brahma MK, Deshmukh NJ, Dixit A, Doshi L, Srinivasan S, Devle J, Damre A, Nemmani KV, Gupte A, Sharma R.

Eur J Med Chem. 2013 Jul;65:337-47. doi: 10.1016/j.ejmech.2013.05.006. Epub 2013 May 14.

PMID:
23735282
3.

Discovery of novel quinoline carboxylic acid series as DGAT1 inhibitors.

Zhou G, Ting PC, Wishart G, Zorn N, Aslanian RG, Lin M, Smith M, Walker SS, Cook J, Van Heek M, Lachowicz J.

Bioorg Med Chem Lett. 2014 Apr 1;24(7):1790-4. doi: 10.1016/j.bmcl.2014.02.028. Epub 2014 Feb 19.

PMID:
24618302
4.

Synthesis and biological evaluation of isoxazole, oxazole, and oxadiazole containing heteroaryl analogs of biaryl ureas as DGAT1 inhibitors.

Jadhav RD, Kadam KS, Kandre S, Guha T, Reddy MM, Brahma MK, Deshmukh NJ, Dixit A, Doshi L, Potdar N, Enose AA, Vishwakarma RA, Sivaramakrishnan H, Srinivasan S, Nemmani KV, Gupte A, Gangopadhyay AK, Sharma R.

Eur J Med Chem. 2012 Aug;54:324-42. doi: 10.1016/j.ejmech.2012.05.016. Epub 2012 May 22.

PMID:
22683241
5.

Exploration of pyridine containing heteroaryl analogs of biaryl ureas as DGAT1 inhibitors.

Motiwala H, Kandre S, Birar V, Kadam KS, Rodge A, Jadhav RD, Mahesh Kumar Reddy M, Brahma MK, Deshmukh NJ, Dixit A, Doshi L, Gupte A, Gangopadhyay AK, Vishwakarma RA, Srinivasan S, Sharma M, Nemmani KV, Sharma R.

Bioorg Med Chem Lett. 2011 Oct 1;21(19):5812-7. doi: 10.1016/j.bmcl.2011.07.109. Epub 2011 Aug 4.

PMID:
21868220
6.

Discovery and optimization of adamantane carboxylic acid derivatives as potent diacylglycerol acyltransferase 1 inhibitors for the potential treatment of obesity and diabetes.

Pagire SH, Pagire HS, Lee GB, Han SJ, Kwak HJ, Kim JY, Kim KY, Rhee SD, Ryu JI, Song JS, Bae MA, Park MJ, Kim D, Lee DH, Ahn JH.

Eur J Med Chem. 2015 Aug 28;101:716-35. doi: 10.1016/j.ejmech.2015.06.043. Epub 2015 Jun 27.

PMID:
26218650
7.

Targeting Acyl-CoA:diacylglycerol acyltransferase 1 (DGAT1) with small molecule inhibitors for the treatment of metabolic diseases.

Cao J, Zhou Y, Peng H, Huang X, Stahler S, Suri V, Qadri A, Gareski T, Jones J, Hahm S, Perreault M, McKew J, Shi M, Xu X, Tobin JF, Gimeno RE.

J Biol Chem. 2011 Dec 2;286(48):41838-51. doi: 10.1074/jbc.M111.245456. Epub 2011 Oct 11.

9.

Discovery of orally active carboxylic acid derivatives of 2-phenyl-5-trifluoromethyloxazole-4-carboxamide as potent diacylglycerol acyltransferase-1 inhibitors for the potential treatment of obesity and diabetes.

Qian Y, Wertheimer SJ, Ahmad M, Cheung AW, Firooznia F, Hamilton MM, Hayden S, Li S, Marcopulos N, McDermott L, Tan J, Yun W, Guo L, Pamidimukkala A, Chen Y, Huang KS, Ramsey GB, Whittard T, Conde-Knape K, Taub R, Rondinone CM, Tilley J, Bolin D.

J Med Chem. 2011 Apr 14;54(7):2433-46. doi: 10.1021/jm101580m. Epub 2011 Mar 17.

PMID:
21413799
10.

Current status of the research and development of diacylglycerol O-acyltransferase 1 (DGAT1) inhibitors.

DeVita RJ, Pinto S.

J Med Chem. 2013 Dec 27;56(24):9820-5. doi: 10.1021/jm4007033. Epub 2013 Sep 3. Review.

PMID:
23919406
11.

Design and synthesis of potent carboxylic acid DGAT1 inhibitors with high cell permeability.

Bali U, Barba O, Dawson G, Gattrell WT, Horswill JG, Pan DA, Procter MJ, Rasamison CM, Sambrook Smith CP, Taylor-Warne A, Wong-Kai-In P.

Bioorg Med Chem Lett. 2012 Jan 15;22(2):824-8. doi: 10.1016/j.bmcl.2011.12.050. Epub 2011 Dec 17.

PMID:
22217874
12.

Discovery of a low-systemic-exposure DGAT-1 inhibitor with a picolinoylpyrrolidine-2-carboxylic acid moiety.

Yan J, Wang G, Dang X, Guo B, Chen W, Wang T, Zeng L, Wang H, Hu Y.

Bioorg Med Chem. 2017 Sep 1;25(17):4701-4714. doi: 10.1016/j.bmc.2017.07.007. Epub 2017 Jul 14.

PMID:
28739155
13.

Triazolo compounds useful as diacylglycerol acyltransferase1 inhibitor - WO2009126624.

Matsuda D, Tomoda H.

Expert Opin Ther Pat. 2010 Aug;20(8):1097-102. doi: 10.1517/13543776.2010.493877.

PMID:
20509774
14.

Identification of 2-aminooxazole amides as acyl-CoA: diacylglycerol acyltransferase 1 (DGAT1) inhibitors through scaffold hopping strategy.

Kim HM, Smith MD, Kim JH, Caplen MA, Chan TY, McKittrick BA, Cook JA, van Heek M, Lachowicz J.

Bioorg Med Chem Lett. 2013 Dec 1;23(23):6410-4. doi: 10.1016/j.bmcl.2013.09.048. Epub 2013 Sep 25.

PMID:
24120540
15.

Pharmacological inhibition to examine the role of DGAT1 in dietary lipid absorption in rodents and humans.

Maciejewski BS, LaPerle JL, Chen D, Ghosh A, Zavadoski WJ, McDonald TS, Manion TB, Mather D, Patterson TA, Hanna M, Watkins S, Gibbs EM, Calle RA, Steppan CM.

Am J Physiol Gastrointest Liver Physiol. 2013 Jun 1;304(11):G958-69. doi: 10.1152/ajpgi.00384.2012. Epub 2013 Apr 4.

PMID:
23558010
16.

Discovery of pyrrolopyridazines as novel DGAT1 inhibitors.

Fox BM, Iio K, Li K, Choi R, Inaba T, Jackson S, Sagawa S, Shan B, Tanaka M, Yoshida A, Kayser F.

Bioorg Med Chem Lett. 2010 Oct 15;20(20):6030-3. doi: 10.1016/j.bmcl.2010.08.066. Epub 2010 Aug 18.

PMID:
20833038
17.

A novel coenzyme A:diacylglycerol acyltransferase 1 inhibitor stimulates lipid metabolism in muscle and lowers weight in animal models of obesity.

Yamamoto T, Yamaguchi H, Miki H, Kitamura S, Nakada Y, Aicher TD, Pratt SA, Kato K.

Eur J Pharmacol. 2011 Jan 15;650(2-3):663-72. doi: 10.1016/j.ejphar.2010.10.040. Epub 2010 Oct 29.

PMID:
21034741
18.

Discovery of diamide compounds as diacylglycerol acyltransferase 1 (DGAT1) inhibitors.

Nakajima K, April M, Brewer JT, Daniels T, Forster CJ, Gilmore TA, Jain M, Kanter A, Kwak Y, Li J, McQuire L, Serrano-Wu MH, Streeper R, Szklennik P, Thompson J, Wang B.

Bioorg Med Chem Lett. 2016 Feb 15;26(4):1245-8. doi: 10.1016/j.bmcl.2016.01.025. Epub 2016 Jan 11.

PMID:
26804232
19.

Intestine-targeted DGAT1 inhibition improves obesity and insulin resistance without skin aberrations in mice.

Tsuda N, Kumadaki S, Higashi C, Ozawa M, Shinozaki M, Kato Y, Hoshida K, Kikuchi S, Nakano Y, Ogawa Y, Furusako S.

PLoS One. 2014 Nov 18;9(11):e112027. doi: 10.1371/journal.pone.0112027. eCollection 2014.

20.

Synthesis of some 5-phenylisoxazole-3-carboxylic acid derivatives as potent xanthine oxidase inhibitors.

Wang S, Yan J, Wang J, Chen J, Zhang T, Zhao Y, Xue M.

Eur J Med Chem. 2010 Jun;45(6):2663-70. doi: 10.1016/j.ejmech.2010.02.013. Epub 2010 Feb 10.

PMID:
20189693

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