2-Heteroaryl Benzimidazole Derivatives as Melanin Concentrating Hormone Receptor 1 (MCH-R1) Antagonists 


Vol. 34,  No. 8, pp. 2305-2310, Aug.  2013
10.5012/bkcs.2013.34.8.2305


PDF
  Tumbnail

  Abstract

A novel series of 2-heteroaryl substituted benzimidazole derivatives, containing the piperidinylphenyl acetamide group at the 1-position, were synthesized and evaluated as MCH-R1 antagonists. Extensive SAR investigation probing the effects of C-2 heteroaryl group led to the identification of 2-[2-(pyridin-3-yl)ethyl] analog 3o, which exhibits highly potent MCH-R1 binding activity with an IC50 value of 1 nM. This substance 3o also has low hERG binding activity, good metabolic stability, and favorable pharmacokinetic properties.

  Statistics
Cumulative Counts from November, 2022
Multiple requests among the same browser session are counted as one view. If you mouse over a chart, the values of data points will be shown.


  Cite this article

[IEEE Style]

C. J. Lim, J. Y. Kim, B. H. Lee, K. Oh, K. Y. Yi, "2-Heteroaryl Benzimidazole Derivatives as Melanin Concentrating Hormone Receptor 1 (MCH-R1) Antagonists," Bulletin of the Korean Chemical Society, vol. 34, no. 8, pp. 2305-2310, 2013. DOI: 10.5012/bkcs.2013.34.8.2305.

[ACM Style]

Chae Jo Lim, Jeong Young Kim, Byung Ho Lee, Kwang-Seok Oh, and Kyu Yang Yi. 2013. 2-Heteroaryl Benzimidazole Derivatives as Melanin Concentrating Hormone Receptor 1 (MCH-R1) Antagonists. Bulletin of the Korean Chemical Society, 34, 8, (2013), 2305-2310. DOI: 10.5012/bkcs.2013.34.8.2305.

Search
(IN TITLE, AUTHOR, ABSTRACT,KEYWORDS)

Advanced Search ▼

POPULAR KEYWORDS
(TOP 10 KEYWORDS)

Recent Publications
(LAST 3 YEARS)

ISSN(Print) 0253-2964
ISSN(Online) 1229-5949