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Chain Branching Approach in Structure Modification of TRPV1 Receptor Antagonist MK056 and its Analogs

Authors
Jang, MijungRyu, Chong HyunPark, Young-HoKim, Hee-Doo
Issue Date
Feb-2012
Publisher
PHARMACEUTICAL SOC KOREA
Keywords
Chain branching; TRPV1; 1,3-Dibenzylthioureas; Antagonist; Ca-45(2+)-influx assay
Citation
ARCHIVES OF PHARMACAL RESEARCH, v.35, no.2, pp.321 - 326
Journal Title
ARCHIVES OF PHARMACAL RESEARCH
Volume
35
Number
2
Start Page
321
End Page
326
URI
https://scholarworks.sookmyung.ac.kr/handle/2020.sw.sookmyung/11985
DOI
10.1007/s12272-012-0212-x
ISSN
0253-6269
Abstract
A series of chain branched 1,3-dibenzylthiourea derivatives were designed, synthesized, and evaluated for their antagonist activity against TRPV1. The synthesized chain branched 1,3-dibenzylthioureas 9a-g were tested for their antagonist activities against TRPV1 by Ca-45(2+)-influx assay using neonatal rat cultured spinal sensory neurons. Fluorinated ethyl-branched analog 9g showed the most potent antagonist activity with an IC50 value of 0.41 mu M, but all of the chain branched analogs were less potent than the parent compounds MK-056 and SC-0030, indicating that chain branching on the benzylic position of B-ring is detrimental to potency. Optimized receptor binding seems to be interfered by chain branching, and resulted in decrease in potency.
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