Discovery of novel 1,4-dihydropyridine-based PDE4 inhibitors.

Autor: Poondra RR; Department of Medicinal Chemistry, Institute of Life Sciences, University of Hyderabad Campus, Gachibowli, Hyderabad 500 046, India. rajamohanreddyp@ilsresearch.org, Nallamelli RV, Meda CL, Srinivas BN, Grover A, Muttabathula J, Voleti SR, Sridhar B, Pal M, Parsa KV
Jazyk: angličtina
Zdroj: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2013 Feb 15; Vol. 23 (4), pp. 1104-9. Date of Electronic Publication: 2012 Dec 08.
DOI: 10.1016/j.bmcl.2012.11.121
Abstrakt: Substituted 1,4-dihydropyridines were discovered as a novel and potent series of phosphodiesterase 4 (PDE4) inhibitors. Structure-activity relationships within this series have been carried out and studies revealed that the dihydropyridine core, with indole moiety and 3,4-dimethoxybenzyl group, is a potent analogue for PDE4 inhibition. These novel series of compounds were prepared via a 3-component reaction in a single pot. In vitro biological activity, modeling studies and crystallography data are also reported.
(Copyright © 2012 Elsevier Ltd. All rights reserved.)
Databáze: MEDLINE