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International Journal of Medicinal Chemistry
Volume 2011 (2011), Article ID 424535, 8 pages
http://dx.doi.org/10.1155/2011/424535
Review Article

The Discovery of Novel Selective D1 Dopaminergic Agonists: A-68930, A-77636, A-86929, and ABT-413

Global Pharmaceutical Research and Development, Martin Consulting, Waukegan, IL 60064, USA

Received 4 December 2010; Accepted 17 February 2011

Academic Editor: Hussein El-Subbagh

Copyright © 2011 Yvonne Connolly Martin. This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

Abstract

The novel selective D1 dopaminergic full agonists A-68930, A-77636 were discovered by the synthesis of molecules to probe the bioactive conformation of the partial agonist SKF-38393, by the use of this information to add D1 affinity and selectivity to a screening hit, and by traditional medicinal chemistry exploration of structure-activity relationships. The subsequent design of A-86929 and ABT-413 capitalized on these results, recently disclosed agonists, and traditional medicinal chemistry.