1364683-70-4Relevant articles and documents
Chain branching approach in structure modification of TRPV1 receptor antagonist MK056 and its analogs
Jang, Mijung,Ryu, Chong Hyun,Park, Young-Ho,Kim, Hee-Doo
experimental part, p. 321 - 326 (2012/08/29)
A series of chain branched 1,3-dibenzylthiourea derivatives were designed, synthesized, and evaluated for their antagonist activity against TRPV1. The synthesized chain branched 1,3dibenzylthioureas 9a-g were tested for their antagonist activities against TRPV1 by 45 Ca 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 μM, but all of the chain branched analogs were less potent than the parent compounds MK-056 and SC0030, 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.