Ureas with histamine H3-antagonist receptor activity--a new scaffold discovered by lead-hopping from cinnamic acid amides.

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Lau JF, Jeppesen CB, Rimvall K, Hohlweg R

Ureas with histamine H3-antagonist receptor activity--a new scaffold discovered by lead-hopping from cinnamic acid amides.

Bioorg Med Chem Lett. 2006 Oct 15;16(20):5303-8.

PubMed ID

16908150 [ View in PubMed

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Abstract

A group of tri and tetrasubstituted urea derivatives have been found to be hH(3)-antagonists. The most potent compounds were found in the class of (piperazine-1-yl)-(piperidine-1-yl)-methanones which in addition showed negligible hERG inhibition.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Bepridil	Potassium voltage-gated channel subfamily H member 2	Ki (nM)	444	N/A	N/A	Details
Thioridazine	Potassium voltage-gated channel subfamily H member 2	Ki (nM)	869	N/A	N/A	Details