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Volumn 19, Issue 17, 2009, Pages 5214-5217

Thiazole analog as stearoyl-CoA desaturase 1 inhibitor

Author keywords

MF 152; Obesity; SCD1; Stearoyl CoA desaturase 1 inhibitor; Thiazole; Type 2 diabetes

Indexed keywords

1 (2,4 DICHLOROPHENYL) 5 (4 IODOPHENYL) 4 METHYL N (1 PIPERIDYL) 1H PYRAZOLE 3 CARBOXAMIDE; ACYL COENZYME A DESATURASE; ACYL COENZYME A DESATURASE INHIBITOR; MF 152; THIAZOLE DERIVATIVE; UNCLASSIFIED DRUG;

EID: 68349157394     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2009.07.015     Document Type: Article
Times cited : (36)

References (23)
  • 13
    • 68349147654 scopus 로고    scopus 로고
    • note
    • The study of a small molecule of SCD inhibitor was reported recently, Ref. 6b.
  • 14
    • 68349124827 scopus 로고    scopus 로고
    • note
    • Five applications from Xenon (WO2005/011653 to WO 2005/011657) were published on February 10, 2005. Representative one: Abreo, M.; Chafeev, M.; Chakka, N.; Chowdhury, S.; Fu, J.-M.; Gschwend, H. W.; Holladay, M. W.; Hou, D.; Kamboj, R.; Kodumuru, V.; Li, W.; Liu, S.; Raina, V.; Sun, S.; Sun, S.; Sviridov, S.; Winther, M. D.; Zhang, Z. WO2005/011655.
  • 18
    • 68349129793 scopus 로고    scopus 로고
    • There was a patent application on five-membered heterocycles during the course of this work. However, examples disclosed are very limited in scope. Kamboj, R.; Zhang, Z.; Fu, J.-M.; Kodumuru, V.; Liu, S.; Sun, S.; Chakka, N. WO2006/034315.
    • There was a patent application on five-membered heterocycles during the course of this work. However, examples disclosed are very limited in scope. Kamboj, R.; Zhang, Z.; Fu, J.-M.; Kodumuru, V.; Liu, S.; Sun, S.; Chakka, N. WO2006/034315.
  • 19
    • 68349140937 scopus 로고    scopus 로고
    • Rat microsomal assay conditions: Li, C, S.; Ramtohul, Y.; Huang, Z.; Zhang, L.; Lachance, N. WO2006/130986.
    • Rat microsomal assay conditions: Li, C, S.; Ramtohul, Y.; Huang, Z.; Zhang, L.; Lachance, N. WO2006/130986.
  • 21
    • 68349126666 scopus 로고    scopus 로고
    • note
    • 2 atmosphere. However, compound 1 has a total of 10 metabolites with the hydroxylation metabolite 2 as major product whereas compound 13 has only three metabolites with the acid 16 as the major metabolite. Some of these metabolites from both compounds were confirmed with synthetic standard and not all metabolites were fully characterized.
  • 22
    • 68349129795 scopus 로고    scopus 로고
    • note
    • Food consumption was not vigorously measured for this exploratory experiment. There were ∼5% less food consumptions for both compound 13 and AM251, but they were not statistically significant in this study. Subsequent studies showed that compound 13 does not appear to have effect on food consumption (unpublished results).


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.