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001-es BibID:	BIBFORM005639
Első szerző:	Ryu, HyungChul
Cím:	Stereospecific high-affinity TRPV1 antagonists : chiral N-(2-benzyl-3-pivaloyloxypropyl) 2-[4-(methylsulfonylamino)phenyl]propionamide analogues / Ryu, H., Jin, M. K., Kim, S. Y., Choi, H. K., Kang, S. U., Kang, D. W., Lee, J., Pearce, L. V., Pavlyukovets, V. A., Morgan, M. A., Tran, R., Toth, A., Lundberg, D. J., Blumberg, P. M.
Dátum:	2008
ISSN:	0022-2623 (Print)
Megjegyzések:	Previously, we reported the thiourea antagonists 2a and 2b as potent and high affinity TRPV1 antagonists. For further optimization of the lead compounds, a series of their amide and alpha-substituted amide surrogates were investigated and novel chiral N-(2-benzyl-3-pivaloyloxypropyl) 2-[4-(methylsulfonylamino)phenyl]propionamide analogues were characterized as potent and stereospecific rTRPV1 antagonists. In particular, compounds 72 and 73 displayed high binding affinities, with K i values of 4.12 and 1.83 nM and potent antagonism with K i values of 0.58 and 5.2 nM, respectively, in rTRPV1/CHO cells. These values are comparable or more potent than those of 5-iodoRTX under the same assay conditions. A distinctive binding model that includes two hydrophobic pockets is proposed for this series of compounds based on docking studies of 57 and 72 with a homology model of the TM3/4 region of TRPV1.
Tárgyszavak:	Orvostudományok Elméleti orvostudományok idegen nyelvű folyóiratközlemény külföldi lapban Animals Benzeneacetamides Binding Sites Binding, Competitive CHO Cells Calcium/metabolism Cricetinae Cricetulus Hydrophobicity Mesylates Models, Molecular Radioligand Assay Rats Stereoisomerism Structure-Activity Relationship TRPV Cation Channels
Megjelenés:	Journal of Medicinal Chemistry. - 51 : 1 (2008), p. 57-67. -
További szerzők:	Jin, Mi-Kyoung Kim, Su Yeon Choi, Hyun-Kyung Kang, Sang-Uk Kang, Dong Wook Lee, Jeewoo Pearce, Larry V. Pavlyukovets, Vladimir A. Morgan, Matthew A. Tran, Richard Tóth Attila (1971-) (biológus) Lundberg, Daniel J. Blumberg, Peter M.
Internet cím:	elektronikus változat
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