2-(Aminomethyl)-benzamide-based glycine transporter type-2 inhibitors

Koc-Kan Ho; Kenneth C Appell; John J Baldwin; Adolph C Bohnstedt; Guizhen Dong; Tao Guo; Robert Horlick; Khondaker R Islam; Steven G Kultgen; Christopher M Masterson; Edward McDonald; Kirk McMillan; J Richard Morphy; Zoran Rankovic; Hardy Sundaram; Maria Webb

doi:10.1016/j.bmcl.2003.09.080

2-(Aminomethyl)-benzamide-based glycine transporter type-2 inhibitors

Bioorg Med Chem Lett. 2004 Jan 19;14(2):545-8. doi: 10.1016/j.bmcl.2003.09.080.

Authors

Koc-Kan Ho¹, Kenneth C Appell, John J Baldwin, Adolph C Bohnstedt, Guizhen Dong, Tao Guo, Robert Horlick, Khondaker R Islam, Steven G Kultgen, Christopher M Masterson, Edward McDonald, Kirk McMillan, J Richard Morphy, Zoran Rankovic, Hardy Sundaram, Maria Webb

Affiliation

¹ Pharmacopeia, Inc., PO Box 5350, Princeton, NJ 08543-5350, USA. kanho@pharmacorp.com

PMID: 14698200
DOI: 10.1016/j.bmcl.2003.09.080

Abstract

Structure-activity studies on benzamide 1 obtained from library screening led to the discovery of a novel series of potent and selective glycine transporter type-2 inhibitors.

MeSH terms

Amino Acid Transport Systems, Neutral / antagonists & inhibitors*
Amino Acid Transport Systems, Neutral / metabolism
Animals
Benzamides / chemistry*
Benzamides / metabolism
Benzamides / pharmacology
CHO Cells
Cricetinae
Glycine / antagonists & inhibitors
Glycine / metabolism*
Glycine Plasma Membrane Transport Proteins
Humans

Substances

Amino Acid Transport Systems, Neutral
Benzamides
Glycine Plasma Membrane Transport Proteins
Glycine