These tools will no longer be maintained as of December 31, 2024. Archived website can be found here. PubMed4Hh GitHub repository can be found here. Contact NLM Customer Service if you have questions.


Pubmed for Handhelds

PUBMED FOR HANDHELDS

Search MEDLINE/PubMed

  • Title: Spiroindane based amides as potent and selective MC4R agonists for the treatment of obesity.
    Author: He S, Ye Z, Dobbelaar PH, Sebhat IK, Guo L, Liu J, Jian T, Lai Y, Franklin CL, Bakshi RK, Dellureficio JP, Hong Q, Weinberg DH, Macneil T, Tang R, Strack AM, Tamvakopoulos C, Peng Q, Miller RR, Stearns RA, Chen HY, Chen AS, Fong TM, Wyvratt MJ, Nargund RP.
    Journal: Bioorg Med Chem Lett; 2010 Aug 01; 20(15):4399-405. PubMed ID: 20598882.
    Abstract:
    We report a series of potent and selective MC4R agonists based on spiroindane amide privileged structures for potential treatments of obesity. Among the synthetic methods used, Method C allows rapid synthesis of the analogs. The series of compounds can afford high potency on MC4R as well as good rodent pharmacokinetic profiles. Compound 1r (MK-0489) demonstrates MC4R mediated reduction of food intake and body weight in mouse models. Compound 1r is efficacious in 14-day diet-induced obese (DIO) rat models.
    [Abstract] [Full Text] [Related] [New Search]