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Synthesis and evaluation of potent pyrrolidine H(3) antagonists
Anil Vasudevan1, Scott E Conner, Robert G Gentles
1Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60031, USA. anil.vasudevan@abbott.com
Bioorganic & Medicinal Chemistry Letters
|October 10, 2002
Abstract:
The synthesis and biological evaluation of novel antagonists of the rat H(3) receptor are described. These compounds differ from prototypical H(3) antagonists in that they do not contain an imidazole moiety, but rather a substituted aminopyrrolidine moiety. A systematic modification of the substituents on the aminopyrrolidine ring was performed using pre-formatted precursor sets, where applicable, to afford several compounds with high affinity and selectivity for the H(3) receptor.