- Asymmetric synthesis and receptor activity of chiral simplified resiniferatoxin (sRTX) analogues as transient receptor potential vanilloid 1 (TRPV1) ligands
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The chiral isomers of the two potent simplified RTX-based vanilloids, compounds 2 and 3, were synthesized employing highly enantioselective PTC alkylation and evaluated as hTRPV1 ligands. The analysis indicated that the R-isomer was the eutomer in binding affinity and functional activity. The agonism of compound 2R was comparable to that of RTX. Docking analysis of the chiral isomers of 3 suggested the basis for its stereospecific activity and the binding mode of 3R.
- Kim, Myeong Seop,Ki, Yooran,Ahn, Song Yeon,Yoon, Suyoung,Kim, Sung-Eun,Park, Hyeung-Geun,Lee, Jeewoo,Sun, Wei,Son, Karam,Cui, Minghua,Choi, Sun,Pearce, Larry V.,Esch, Timothy E.,DeAndrea-Lazarus, Ian A.,Blumberg, Peter M.
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p. 382 - 385
(2015/03/18)
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- Asymmetric synthesis and receptor activity of chiral simplified resiniferatoxin (sRTX) analogues as transient receptor potential vanilloid 1 (TRPV1) ligands
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The chiral isomers of the two potent simplified RTX-based vanilloids, compounds 2 and 3, were synthesized employing highly enantioselective PTC alkylation and evaluated as hTRPV1 ligands. The analysis indicated that the R-isomer was the eutomer in binding affinity and functional activity. The agonism of compound 2R was comparable to that of RTX. Docking analysis of the chiral isomers of 3 suggested the basis for its stereospecific activity and the binding mode of 3R.
- Kim, Myeong Seop,Ki, Yooran,Ahn, Song Yeon,Yoon, Suyoung,Kim, Sung-Eun,Park, Hyeung-Geun,Sun, Wei,Son, Karam,Cui, Minghua,Choi, Sun,Pearce, Larry V.,Esch, Timothy E.,Deandrea-Lazarus, Ian A.,Blumberg, Peter M.,Lee, Jeewoo
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p. 382 - 385
(2015/08/19)
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- TRPV1 ANTAGONISTS
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Disclosed herein are compounds of formula (I) or pharmaceutically acceptable salts, prodrugs, or combinations thereof, wherein X1, L, Rx, Ry, Rz, R1, R2, A, m, n, p, q, and r are defined in
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- PROCESS OF SULFONATING 4-AMINOBENZONITRILES
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A process of producing a compound of formula (3), wherein R1 is a C1-5 alkyl group, R2 is a halogen atom, a C1-5 alkyl group, a C2-5 alkenyl group, a C2-5 alkynyl group, a C1-5 a
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Page/Page column 26
(2008/06/13)
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- PENTAFLUOROSULPHANYL-SUBSTITUTED COMPOUND AND ITS USE FOR PRODUCING MEDICAMENTS
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The present invention relates to pentafluorosulphanyl-substituted compounds, processes for preparing them, medicaments comprising these compounds, and the use of these compounds for producing medicaments.
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Page/Page column 40; 41
(2008/06/13)
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- NOVEL N-HYDROXY THIOUREA, UREA AND AMIDE COMPOUNDS AND THE PHARMACEUTICAL COMPOSITIONS COMPRISING THE SAME
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The present invention relates to novel n-hydroxythiourea, urea and amide compounds as a potent vanilloid receptor antagonist and the pharmaceutical compositions comprising the same. The inventive compound can be useful for analgesics to prevent, alleviate
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- Novel non-vanilloid VR1 antagonist of high analgesic effects and its structural requirement for VR1 antagonistic effects
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A novel non-vanilloid VR1 antagonist consisting of a new vanilloid equivalent exhibits excellent analgesic effects as well as highly potent antagonistic activities in both capsaicin single channel and calcium uptake assays. In addition, the structural requirement for the vanilloid equivalent of the potent VR1 antagonist has also been elucidated.
- Suh, Young-Ger,Lee, Yong-Sil,Min, Kyung-Hoon,Park, Ok-Hui,Seung, Ho-Sun,Kim, Hee-Doo,Park, Hyoung-Geun,Choi, Ji-Yeon,Lee, Jeewoo,Kang, Sang-Wook,Oh, Uh-Taek,Koo, Jae-Yeon,Joo, Yung-Hyup,Kim, Sun-Young,Kim, Jin Kwan,Park, Young-Ho
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p. 4389 - 4393
(2007/10/03)
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