SCOPUS 정보 검색 플랫폼

Bioorganic and Medicinal Chemistry Letters

Volumn 22, Issue 12, 2012, Pages 3873-3878

Identification, optimisation and in vivo evaluation of oxadiazole DGAT-1 inhibitors for the treatment of obesity and diabetes

(29) McCoull, William a Addie, Matthew S a Birch, Alan M a Birtles, Susan a Buckett, Linda K a Butlin, Roger J a Bowker, Suzanne S a Boyd, Scott a Chapman, Stephen a Davies, Robert D M a Donald, Craig S a Green, Clive P a Jenner, Chloe a Kemmitt, Paul D a Leach, Andrew G a Moody, Graeme C a Morentin Gutierrez, Pablo a Newcombe, Nicholas J a Nowak, Thorsten a Packer, Martin J a more..

a ASTRAZENECA (United Kingdom)

Author keywords

DGAT; LLE; Obesity; Oxadiazole; PK PD

Indexed keywords

ACYLTRANSFERASE INHIBITOR; ANTIDIABETIC AGENT; ANTIOBESITY AGENT; AZD 3988; UNCLASSIFIED DRUG;

ADIPOSE TISSUE; ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; CONTROLLED STUDY; DIABETES MELLITUS; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG EFFICACY; DRUG HALF LIFE; DRUG POTENCY; DRUG SCREENING; EXPERIMENTAL DOG; HUMAN; HUMAN CELL; IN VIVO STUDY; LIPOPHILICITY; MAXIMUM PLASMA CONCENTRATION; MICROSOME; MOUSE; NONHUMAN; OBESITY; PLASMA PROTEIN BINDING; RAT;

ANIMALS; DIABETES MELLITUS; DIACYLGLYCEROL O-ACYLTRANSFERASE; DOGS; DRUG DESIGN; DRUG EVALUATION, PRECLINICAL; ENZYME INHIBITORS; HALF-LIFE; HIGH-THROUGHPUT SCREENING ASSAYS; HUMANS; HYPOGLYCEMIC AGENTS; LIGANDS; MICE; OBESITY; OXADIAZOLES; QUANTITATIVE STRUCTURE-ACTIVITY RELATIONSHIP; RATS;

EID: 84861577181 PISSN: 0960894X EISSN: 14643405 Source Type: Journal
DOI: 10.1016/j.bmcl.2012.04.117 Document Type: Article

Times cited : (42)

References (26)

1
- 44649128516
- V.A. Zammit, L.K. Buckett, A.V. Turnbull, H. Wure, and A. Proven Pharmacol. Ther. 118 2008 295
- (2008) Pharmacol. Ther. , vol.118 , pp. 295
- Zammit, V.A.¹ Buckett, L.K.² Turnbull, A.V.³ Wure, H.⁴ Proven, A.⁵

2
- 36549079637
- B.K. Hubbard, I. Enyedy, T.A. Gilmore, and M. Serrano-Wu Expert Opin. Ther. Pat. 17 2007 1331
- (2007) Expert Opin. Ther. Pat. , vol.17 , pp. 1331
- Hubbard, B.K.¹ Enyedy, I.² Gilmore, T.A.³ Serrano-Wu, M.⁴

3
- 34848834771
- D. Matsuda, and H. Tomoda Curr. Opin. Invest. Drugs (Thomson Sci.) 8 2007 836
- (2007) Curr. Opin. Invest. Drugs (Thomson Sci.) , vol.8 , pp. 836
- Matsuda, D.¹ Tomoda, H.²

4
- 14744304497
- H.C. Chen, and R.V. Farese Arterioscler., Thromb., Vasc. Biol. 25 2005 482
- (2005) Arterioscler., Thromb., Vasc. Biol. , vol.25 , pp. 482
- Chen, H.C.¹ Farese, R.V.²

5
- 64349101065
- A.M. Birch, S. Birtles, L.K. Buckett, P.D. Kemmitt, G.J. Smith, T.J.D. Smith, A.V. Turnbull, and S.J.Y. Wang J. Med. Chem. 52 2009 1558
- (2009) J. Med. Chem. , vol.52 , pp. 1558
- Birch, A.M.¹ Birtles, S.² Buckett, L.K.³ Kemmitt, P.D.⁴ Smith, G.J.⁵ Smith, T.J.D.⁶ Turnbull, A.V.⁷ Wang, S.J.Y.⁸

6
- 39149122218
- G. Zhao, A.J. Souers, M. Voorbach, H.D. Falls, B. Droz, S. Brodjian, Y.Y. Lau, R.R. Iyengar, J. Gao, A.S. Judd, S.H. Wagaw, M.M. Ravn, K.M. Engstrom, J.K. Lynch, M.M. Mulhern, J. Freeman, B.D. Dayton, X. Wang, N. Grihalde, D. Fry, D.W.A. Beno, K.C. Marsh, Z. Su, G.J. Diaz, C.A. Collins, H. Sham, R.M. Reilly, M.E. Brune, and P.R. Kym J. Med. Chem. 51 2008 380
- (2008) J. Med. Chem. , vol.51 , pp. 380
- Zhao, G.¹ Souers, A.J.² Voorbach, M.³ Falls, H.D.⁴ Droz, B.⁵ Brodjian, S.⁶ Lau, Y.Y.⁷ Iyengar, R.R.⁸ Gao, J.⁹ Judd, A.S.¹⁰ Wagaw, S.H.¹¹ Ravn, M.M.¹² Engstrom, K.M.¹³ Lynch, J.K.¹⁴ Mulhern, M.M.¹⁵ Freeman, J.¹⁶ Dayton, B.D.¹⁷ Wang, X.¹⁸ Grihalde, N.¹⁹ Fry, D.²⁰ more..

7
- 77950028319
- Y. Nakada, T.D. Aicher, Y.L. Huerou, T. Turner, S.A. Pratt, S.S. Gonzales, S.A. Boyd, H. Miki, T. Yamamoto, H. Yamaguchi, K. Kato, and S. Kitamura Bioorg. Med. Chem. 18 2010 2785
- (2010) Bioorg. Med. Chem. , vol.18 , pp. 2785
- Nakada, Y.¹ Aicher, T.D.² Huerou, Y.L.³ Turner, T.⁴ Pratt, S.A.⁵ Gonzales, S.S.⁶ Boyd, S.A.⁷ Miki, H.⁸ Yamamoto, T.⁹ Yamaguchi, H.¹⁰ Kato, K.¹¹ Kitamura, S.¹²

8
- 79953801433
- Y. Qian, S.J. Wertheimer, M. Ahmad, A.W. Cheung, F. Firooznia, M.M. Hamilton, S. Hayden, S. Li, N. Marcopulos, L. McDermott, J. Tan, W. Yun, L. Guo, A. Pamidimukkala, Y. Chen, K. Huang, G.B. Ramsey, T. Whittard, K. Conde-Knape, R. Taub, C.M. Rondinone, J. Tilley, and D. Bolin J. Med. Chem. 54 2011 2433
- (2011) J. Med. Chem. , vol.54 , pp. 2433
- Qian, Y.¹ Wertheimer, S.J.² Ahmad, M.³ Cheung, A.W.⁴ Firooznia, F.⁵ Hamilton, M.M.⁶ Hayden, S.⁷ Li, S.⁸ Marcopulos, N.⁹ McDermott, L.¹⁰ Tan, J.¹¹ Yun, W.¹² Guo, L.¹³ Pamidimukkala, A.¹⁴ Chen, Y.¹⁵ Huang, K.¹⁶ Ramsey, G.B.¹⁷ Whittard, T.¹⁸ Conde-Knape, K.¹⁹ Taub, R.²⁰ more..

9
- 80255140429
- W. Yun, M. Ahmad, Y. Chen, P. Gillespie, K. Conde-Knape, S. Kazmer, S. Li, Y. Qian, R. Taub, S.J. Wertheimer, T. Whittard, and D. Bolin Bioorg. Med. Chem. Lett. 21 2011 7205
- (2011) Bioorg. Med. Chem. Lett. , vol.21 , pp. 7205
- Yun, W.¹ Ahmad, M.² Chen, Y.³ Gillespie, P.⁴ Conde-Knape, K.⁵ Kazmer, S.⁶ Li, S.⁷ Qian, Y.⁸ Taub, R.⁹ Wertheimer, S.J.¹⁰ Whittard, T.¹¹ Bolin, D.¹²

10
- 77956914790
- B.M. Fox, K. Iio, K. Li, R. Choi, T. Inaba, S. Jackson, S. Sagawa, B. Shan, M. Tanaka, A. Yoshida, and F. Kayser Bioorg. Med. Chem. Lett. 20 2010 6030
- (2010) Bioorg. Med. Chem. Lett. , vol.20 , pp. 6030
- Fox, B.M.¹ Iio, K.² Li, K.³ Choi, R.⁴ Inaba, T.⁵ Jackson, S.⁶ Sagawa, S.⁷ Shan, B.⁸ Tanaka, M.⁹ Yoshida, A.¹⁰ Kayser, F.¹¹

11
- 84860410307
- H. Motiwala, S. Kandre, V. Birar, K.S. Kadam, A. Rodge, R.D. Jadhav, M. Mahesh Kumar Reddy, M.K. Brahma, N.J. Deshmukh, A. Dixit, L. Doshi, A. Gupte, A.K. Gangopadhyay, R.A. Vishwakarma, S. Srinivasan, M. Sharma, K.V.S. Nemmani, and R. Sharma Bioorg. Med. Chem. Lett. 21 2011 5812
- (2011) Bioorg. Med. Chem. Lett. , vol.21 , pp. 5812
- Motiwala, H.¹ Kandre, S.² Birar, V.³ Kadam, K.S.⁴ Rodge, A.⁵ Jadhav, R.D.⁶ Mahesh Kumar Reddy, M.⁷ Brahma, M.K.⁸ Deshmukh, N.J.⁹ Dixit, A.¹⁰ Doshi, L.¹¹ Gupte, A.¹² Gangopadhyay, A.K.¹³ Vishwakarma, R.A.¹⁴ Srinivasan, S.¹⁵ Sharma, M.¹⁶ Nemmani, K.V.S.¹⁷ Sharma, R.¹⁸

12
- 79956071958
- R.L. Dow, J. Li, M.P. Pence, E.M. Gibbs, J.L. LaPerle, J. Litchfield, D.W. Piotrowski, M.J. Munchhof, T.B. Manion, W.J. Zavadoski, G.S. Walker, R.K. McPherson, S. Tapley, E. Sugarman, A. Guzman-Perez, and P. DaSilva-Jardine ACS Med. Chem. Lett. 2 2011 407
- (2011) ACS Med. Chem. Lett. , vol.2 , pp. 407
- Dow, R.L.¹ Li, J.² Pence, M.P.³ Gibbs, E.M.⁴ Laperle, J.L.⁵ Litchfield, J.⁶ Piotrowski, D.W.⁷ Munchhof, M.J.⁸ Manion, T.B.⁹ Zavadoski, W.J.¹⁰ Walker, G.S.¹¹ McPherson, R.K.¹² Tapley, S.¹³ Sugarman, E.¹⁴ Guzman-Perez, A.¹⁵ Dasilva-Jardine, P.¹⁶

13
- 80052924403
- R.L. Dow, M. Andrews, G.E. Aspnes, G. Balan, E. Michael Gibbs, A. Guzman-Perez, K. Karki, J.L. LaPerle, J. Li, J. Litchfield, M.J. Munchhof, C. Perreault, and L. Patel Bioorg. Med. Chem. Lett. 21 2011 6122
- (2011) Bioorg. Med. Chem. Lett. , vol.21 , pp. 6122
- Dow, R.L.¹ Andrews, M.² Aspnes, G.E.³ Balan, G.⁴ Michael Gibbs, E.⁵ Guzman-Perez, A.⁶ Karki, K.⁷ Laperle, J.L.⁸ Li, J.⁹ Litchfield, J.¹⁰ Munchhof, M.J.¹¹ Perreault, C.¹² Patel, L.¹³

14
- 84855650314
- U. Bali, O. Barba, G. Dawson, W.T. Gattrell, J.G. Horswill, D.A. Pan, M.J. Procter, C.M. Rasamison, C.P. Sambrook Smith, A. Taylor-Warne, and P. Wong-Kai-In Bioorg. Med. Chem. Lett. 22 2012 824
- (2012) Bioorg. Med. Chem. Lett. , vol.22 , pp. 824
- Bali, U.¹ Barba, O.² Dawson, G.³ Gattrell, W.T.⁴ Horswill, J.G.⁵ Pan, D.A.⁶ Procter, M.J.⁷ Rasamison, C.M.⁸ Sambrook Smith, C.P.⁹ Taylor-Warne, A.¹⁰ Wong-Kai-In, P.¹¹

15
- 77954647349
- A.M. Birch, L.K. Buckett, and A.V. Turnbull Curr. Opin. Drug Discov. Devel. 13 2010 489
- (2010) Curr. Opin. Drug Discov. Devel. , vol.13 , pp. 489
- Birch, A.M.¹ Buckett, L.K.² Turnbull, A.V.³

16
- 73649126531
- A.J. King, A.S. Judd, and A.J. Souers Expert Opin. Ther. Pat. 20 2010 19
- (2010) Expert Opin. Ther. Pat. , vol.20 , pp. 19
- King, A.J.¹ Judd, A.S.² Souers, A.J.³

17
- 82355171896
- J. Cao, Y. Zhou, H. Peng, X. Huang, S. Stahler, V. Suri, A. Qadri, T. Gareski, J. Jones, S. Hahm, M. Perreault, J. McKew, M. Shi, X. Xu, J.F. Tobin, and R.E. Gimeno J. Biol. Chem. 286 2011 41838
- (2011) J. Biol. Chem. , vol.286 , pp. 41838
- Cao, J.¹ Zhou, Y.² Peng, H.³ Huang, X.⁴ Stahler, S.⁵ Suri, V.⁶ Qadri, A.⁷ Gareski, T.⁸ Jones, J.⁹ Hahm, S.¹⁰ Perreault, M.¹¹ McKew, J.¹² Shi, M.¹³ Xu, X.¹⁴ Tobin, J.F.¹⁵ Gimeno, R.E.¹⁶

18
- 84873064822
- Assay protocols can be found in Ref. 5
- Assay protocols can be found in Ref. 5

19
- 0035914412
- K.D. Lardizabal, J.T. Mai, N.W. Wagner, A. Wyrick, T. Voelker, and D.J. Hawkins J. Biol. Chem. 276 2001 38862
- (2001) J. Biol. Chem. , vol.276 , pp. 38862
- Lardizabal, K.D.¹ Mai, J.T.² Wagner, N.W.³ Wyrick, A.⁴ Voelker, T.⁵ Hawkins, D.J.⁶

20
- 77958021757
- D. Buttar, N. Colclough, S. Gerhardt, P.A. MacFaul, S.D. Phillips, A. Plowright, P. Whittamore, K. Tam, K. Maskos, S. Steinbacher, and H. Steuber Bioorg. Med. Chem. 18 2010 7486
- (2010) Bioorg. Med. Chem. , vol.18 , pp. 7486
- Buttar, D.¹ Colclough, N.² Gerhardt, S.³ MacFaul, P.A.⁴ Phillips, S.D.⁵ Plowright, A.⁶ Whittamore, P.⁷ Tam, K.⁸ Maskos, K.⁹ Steinbacher, S.¹⁰ Steuber, H.¹¹

21
- 35748934487
- P.D. Leeson, and B. Springthorpe Nat. Rev. Drug Discov. 6 2007 881
- (2007) Nat. Rev. Drug Discov. , vol.6 , pp. 881
- Leeson, P.D.¹ Springthorpe, B.²

22
- 84861575058
- A.M. Birch, S.S. Bowker, R.J. Butlin, C.S. Donald, W. McCoull, T. Nowak, and A. Plowright PCT Int. Appl. 2006 418
- (2006) PCT Int. Appl. , pp. 418
- Birch, A.M.¹ Bowker, S.S.² Butlin, R.J.³ Donald, C.S.⁴ McCoull, W.⁵ Nowak, T.⁶ Plowright, A.⁷

23
- 84861580564
- R.J. Butlin, C.P. Green, and W. McCoull PCT Int. Appl. 2006 74
- (2006) PCT Int. Appl. , pp. 74
- Butlin, R.J.¹ Green, C.P.² McCoull, W.³

24
- 0010040681
- S. Wold, P. Geladi, K. Esbensen, and J. Oehman J. Chemom. 1 1987 41
- (1987) J. Chemom. , vol.1 , pp. 41
- Wold, S.¹ Geladi, P.² Esbensen, K.³ Oehman, J.⁴

25
- 84861571751
- B.M. Fox, N. Furukawa, X. Hao, K. Iio, T. Inaba, S.M. Jackson, F. Kayser, M. Labelle, K. Li, T. Matsui, D.L. McMinn, N. Ogawa, S.M. Rubenstein, S. Sagawa, K. Sugimoto, M. Suzuki, M. Tanaka, G. Ye, A. Yoshida, and J. Zhang PCT Int. Appl. 2004 176
- (2004) PCT Int. Appl. , pp. 176
- Fox, B.M.¹ Furukawa, N.² Hao, X.³ Iio, K.⁴ Inaba, T.⁵ Jackson, S.M.⁶ Kayser, F.⁷ Labelle, M.⁸ Li, K.⁹ Matsui, T.¹⁰ McMinn, D.L.¹¹ Ogawa, N.¹² Rubenstein, S.M.¹³ Sagawa, S.¹⁴ Sugimoto, K.¹⁵ Suzuki, M.¹⁶ Tanaka, M.¹⁷ Ye, G.¹⁸ Yoshida, A.¹⁹ Zhang, J.²⁰ more..

26
- 84863115587
- V.S.C. Yeh, D.W.A. Beno, S. Brodjian, M.E. Brune, S.C. Cullen, B.D. Dayton, M.K. Dhaon, H.D. Falls, J. Gao, N. Grihalde, P. Hajduk, T.M. Hansen, A.S. Judd, A.J. King, R.C. Klix, K.J. Larson, Y.Y. Lau, K.C. Marsh, S.W. Mittelstadt, D. Plata, M.J. Rozema, J.A. Segreti, E.J. Stoner, M.J. Voorbach, X. Wang, X. Xin, G. Zhao, C.A. Collins, B.F. Cox, R.M. Reilly, P.R. Kym, and A.J. Souers J. Med. Chem. 55 2012 1751
- (2012) J. Med. Chem. , vol.55 , pp. 1751
- Yeh, V.S.C.¹ Beno, D.W.A.² Brodjian, S.³ Brune, M.E.⁴ Cullen, S.C.⁵ Dayton, B.D.⁶ Dhaon, M.K.⁷ Falls, H.D.⁸ Gao, J.⁹ Grihalde, N.¹⁰ Hajduk, P.¹¹ Hansen, T.M.¹² Judd, A.S.¹³ King, A.J.¹⁴ Klix, R.C.¹⁵ Larson, K.J.¹⁶ Lau, Y.Y.¹⁷ Marsh, K.C.¹⁸ Mittelstadt, S.W.¹⁹ Plata, D.²⁰ more..

* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.