565448-36-4Relevant academic research and scientific papers
Asymmetric synthesis and receptor activity of chiral simplified resiniferatoxin (sRTX) analogues as transient receptor potential vanilloid 1 (TRPV1) ligands
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.
, p. 382 - 385 (2015/03/18)
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.
Asymmetric synthesis and receptor activity of chiral simplified resiniferatoxin (sRTX) analogues as transient receptor potential vanilloid 1 (TRPV1) ligands
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
, p. 382 - 385 (2015/08/19)
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.
TRPV1 ANTAGONISTS
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, (2014/02/15)
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
PROCESS OF SULFONATING 4-AMINOBENZONITRILES
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Page/Page column 26, (2008/06/13)
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
PENTAFLUOROSULPHANYL-SUBSTITUTED COMPOUND AND ITS USE FOR PRODUCING MEDICAMENTS
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Page/Page column 40; 41, (2008/06/13)
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.
NOVEL N-HYDROXY THIOUREA, UREA AND AMIDE COMPOUNDS AND THE PHARMACEUTICAL COMPOSITIONS COMPRISING THE SAME
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Page 37-38, (2010/02/06)
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
Novel non-vanilloid VR1 antagonist of high analgesic effects and its structural requirement for VR1 antagonistic effects
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
, p. 4389 - 4393 (2007/10/03)
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.
