期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 48, 期 6, 页码 1857-1872出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm0495071
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High throughput screening using the recombinant human TRPV1 receptor was used to identify a series of pyridinylpiperazine ureas (3) as TRPV1 vanilloid receptor ligands. Exploration of the structure-activity relationships by parallel synthesis identified the essential pharmacophoric elements for antagonism that permitted further optimization via targeted synthesis to provide a potent orally bioavailable and selective TRPV1 modulator 41 active in several in vivo models.
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