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Your search keyword '"B. Hermans"' showing total 2 results
Start Over Author "B. Hermans" Publisher elsevier science ltd
2 results on '"B. Hermans"'

1. Synthesis and structure-activity relationship of benzetimide derivatives as human CXCR3 antagonists.

Author

Bongartz JP, Buntinx M, Coesemans E, Hermans B, Lommen GV, and Wauwe JV

Subjects
Dexetimide chemistry, Humans, Structure-Activity Relationship, Dexetimide pharmacology, Receptors, CXCR3 antagonists & inhibitors
Abstract

The synthesis and evaluation of benzetimide derivatives showing potent CXCR3 antagonism are described. Optimization of the screening hits led to the identification of more potent CXCR3 antagonists devoid of anti-cholinergic activity and identification of the key pharmacophore moieties of the series.

Published
2008
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2. 2-Mercaptoimidazoles, a new class of potent CCR2 antagonists.

Author

Van Lomen G, Doyon J, Coesemans E, Boeckx S, Cools M, Buntinx M, Hermans B, and Van Wauwe J

Subjects
Calcium Signaling drug effects, Cell Line, Chemokine CCL2 pharmacology, Humans, Imidazoles chemical synthesis, Imidazoles pharmacology, Inhibitory Concentration 50, Receptors, CCR2, Structure-Activity Relationship, Ethylenethiourea analogs & derivatives, Ethylenethiourea chemical synthesis, Ethylenethiourea pharmacology, Receptors, Chemokine antagonists & inhibitors
Abstract

We describe the synthesis and SAR of a new class of CCR2 antagonists based on 2-mercaptoimidazole scaffold. The initial lead 1a was optimized to the 3,4-disubstituted analogues 1p-(S) and 1q-(S), which have IC(50) values in the MCP-1 induced Ca-flux below 0.01 microM.

Published
2005
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