Li FN, Kim NJ, Nam YH, Kim SH, Seo SY, Jeong YS, Kim SY, Park YH, Suh YG
Design, synthesis, and biological evaluation of phenylpropanamides as novel transient receptor potential valnilloid 1 antagonists. [Journal Article]
Arch Pharm Res 2009 Sep; 32(9):1201-10.
Synthesis and structure-activity relationship of N-benzyl-3-phenylpropanamides as transient receptor potential vanilloid 1 (TRPV1) antagonists are described. A variety of substituents such as halide, ester, nitro, and alkyl groups at 2 or 3-position of 4-(methylsulfonylamino) benzyl unit were examined. These compounds exhibited potent (45)Ca(2+) uptake inhibition in rat DRG neuron via TRPV1 blockade. Especially compound 28c, has been identified as a potent antagonist with IC(50) of 38 nM.
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