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: Structure-activity relationships of N-acyl pyrroloquinolone PDE-5 inhibitors.
    Author: Lanter JC, Sui Z, Macielag MJ, Fiordeliso JJ, Jiang W, Qiu Y, Bhattacharjee S, Kraft P, John TM, Haynes-Johnson D, Craig E, Clancy J.
    Journal: J Med Chem; 2004 Jan 29; 47(3):656-62. PubMed ID: 14736245.
    Abstract:
    The discovery of the potent and selective PDE-5 inhibitory activity of a pyrroloquinolone scaffold prompted us to explore the SAR of its acyl derivatives. During the course of these studies, three structural series were found with K(i) values for PDE-5 in the subnanomolar range. Systematic modification of one of these leads produced a compound with excellent selectivity for PDE-5 over other phosphodiesterases and oral bioavailability of 15% in male rats. This compound also displayed in vivo efficacy in an anesthetized canine model of erection when dosed intravenously.
    [Abstract] [Full Text] [Related] [New Search]