Design, synthesis, and evaluation of a new class of noncyclic 1,3-dicarbonyl compounds as PPARα selective activators

Bioorganic and Medicinal Chemistry Letters

Volumn 14, Issue 13, 2004, Pages 3507-3511

  Li, Zhibin ^a   Liao, Chenzhong ^a,b   Ko, Ben C B ^c,d   Shan, Song ^a   Tong, Edith H Y ^c,d   Yin, Zihui ^a   Pan, Desi ^a   Wong, Vincent K W ^c   Shi, Leming ^a   Ning, Zhi Qiang ^a   Hu, Weiming ^a   Zhou, Jiaju ^b   Chung, Stephen S M ^c   Lu, Xian Ping ^a  

^a TSINGHUA UNIVERSITY   (China)

^b INSTITUTE OF PROCESS ENGINEERING   (China)

^c UNIVERSITY OF HONG KONG   (Hong Kong)

^d UNIVERSITY OF HONG KONG   (Hong Kong)

Author keywords

Metabolic diseases; Noncyclic 1,3 dicarbonyl compounds; PPAR activators; Type 2 diabetes

Indexed keywords

BENZENE DERIVATIVE; CYCLOHEXANE DERIVATIVE; PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR AGONIST;

ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; CONTROLLED STUDY; DRUG DESIGN; DRUG EFFICACY; DRUG POTENCY; DRUG SYNTHESIS; EVALUATION; MOUSE; NON INSULIN DEPENDENT DIABETES MELLITUS; NONHUMAN; STRUCTURE ACTIVITY RELATION;

ADIPOSE TISSUE; ADMINISTRATION, ORAL; ALDEHYDES; ANIMALS; ANTILIPEMIC AGENTS; BLOOD GLUCOSE; DIABETES MELLITUS, TYPE 2; DISEASE MODELS, ANIMAL; DRUG DESIGN; KETONES; LIPID METABOLISM; MICE; PPAR ALPHA; PPAR DELTA; PPAR GAMMA; STRUCTURE-ACTIVITY RELATIONSHIP;

ANIMALIA;

EID: 2942525791     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2004.04.053     Document Type: Article

References (21)

1. Kelly D.E., Goodpaster B.H. Diabetes Care. 24:2001;933
2. Issemann I., Green S. Nature. 347:1990;645
3. Willson T.M., Brown P.J., Sternbach D.D., Henke B.R. J. Med. Chem. 43:2000;527
4. Lehmann J.M., Moore L.B., Smith-Oliver T.A., Wilkison W.O., Willson T.M., Kliewer S.A. J. Biol. Chem. 270:1995;12953
5. Oliver W.R., Shenk J.L., Snaith M.R., Russell C.S., Plunket K.D., Bodkin N.L., Lewis M.C., Winegar D.A., Sznaidman M.L., Lambert M.H., Xu H.E., Sternbach D.D., Kliewer S.A., Hansen B.C., Willson T.M. PNAS. 98:2001;5306
6. Bastie C., Luquet S., Holst D., Jehl-Pietri C., Grimaldi P.A. J. Biol. Chem. 275:2000;38768
7. Son C., Hosoda K., Matsuda J., Fujikura J., Yonemitsu S., Iwakura H., Masuzaki H., Ogawa Y., Hayashi T., Itoh H., Nishimura H., Inoue G., Yoshimasa Y., Yamori Y., Nakao K. Endocrinology. 142:2001;4189
8. Larsen T.M., Toubro S., Astrup A. Int. J. Obesity. 27:2003;147
9. Wang Y.X., Lee C.H., Tiep S., Yu R.T., Ham J., Kang H., Evans R.M. Cell. 113:2003;159
10. Etgen G.J., Mantlo N. Curr. Topics Med. Chem. 3:2003;1649
11. Shibata T., Matsui K., Nagao K., Shinkai H., Yonemori F., Wakitani K. Eur. J. Pharmacol. 364:1999;211
12. Shinkai H., Onogi S., Tanaka M., Shibata T., Wao M., Wakitani K., Uchida I. J. Med. Chem. 41:1998;1927
13. Brown P.J., Winegar D.A., Plunket K.D., Moore L.B., Lewis M.C., Wilson J.G., Sundseth S.S., Koble C.S., Wu Z., Chapman J.M., Lehmann J.M., Kliever S.A., Willson T.M. J. Med. Chem. 42:1999;3785
14. Goodsell D.S., Olson A.J. Proteins. 8:1990;195
15. Goodsell D.S., Morris G.M., Olson A.J. J. Mol. Recognition. 9:1996;1
16. Morris G.M., Goodsell D.S., Huey R., Olson A.J. J. Comput. Aided Mol. Des. 10:1996;293
17. Morris G.M., Goodsell D.S., Halliday R.S., Huey R., Hart W.E., Belew R.K., Olson A.J. J. Comput. Chem. 19:1998;1639
18. Cronet P., Petersen J.F.W., Folmer R., Blomberg N., Sjoblom K., Karlsson U., Lindstedt E.-L. Structure. 9:2001;699
19. Gampe R.T. Jr., Montana V.G., Lambert M.H., Miller A.B., Bledsoe R.K., Milburn M.V., Kliewer S.A., Willson T.M., Xu H.E. Mol. Cell. 5:2000;545
20. Xu H.E., Lambert M., Montana V.G., Parks D.J., Blanchard S.G., Brown P.J., Sternbach D.D., Lehmann J.M., Wisely G.B., Willson T.M., Kliewer S.A., Milburn M.V. Mol. Cell. 3:1999;397
21. SYBYL® 6.81. Tripos Inc., 1699 Hanley Road, St. Louis, MO 63144, USA