26406-97-3Relevant academic research and scientific papers
N-4-t-Butylbenzyl 2-(4-methylsulfonylaminophenyl) propanamide TRPV1 antagonists: Structure-activity relationships in the A-region
Kim, Yong Soo,Kil, Min-Jung,Kang, Sang-Uk,Ryu, Hyungchul,Kim, Myeong Seop,Cho, Yongsung,Bhondwe, Rahul S.,Thorat, Shivaji A.,Sun, Wei,Liu, Keliang,Lee, Jin Hee,Choi, Sun,Pearce, Larry V.,Pavlyukovets, Vladimir A.,Morgan, Matthew A.,Tran, Richard,Lazar, Jozsef,Blumberg, Peter M.,Lee, Jeewoo
, p. 215 - 224 (2012/02/16)
Structure-activity relationships for the A-region in a series of N-4-t-butylbenzyl 2-(4-methylsulfonylaminophenyl) propanamides as TRPV1 antagonists have been investigated. Among them, the 3-fluoro analogue 54 showed high binding affinity and potent antagonism for both rTRPV1 and hTRPV1 in CHO cells. Its stereospecific activity was demonstrated with marked selectivity for the (S)-configuration (54S versus 54R). A docking study of 54S with our hTRPV1 homology model highlighted crucial hydrogen bonds between the ligand and the receptor contributing to its potency.
Stereospecific high-affinity TRPV1 antagonists: Chiral N-(2-benzyl-3- pivaloyloxypropyl) 2-[4-(methylsulfonylamino)phenyl]propionamide analogues
Ryu, Hyungchul,Jin, Mi-Kyoung,Su, Yeon Kim,Choi, Hyun-Kyung,Kang, Sang-Uk,Dong, Wook Kang,Lee, Jeewoo,Pearce, Larry V.,Pavlyukovets, Vladimir A.,Morgan, Matthew A.,Tran, Richard,Toth, Attila,Lundberg, Daniel J.,Blumberg, Peter M.
, p. 57 - 67 (2008/09/18)
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 α-substituted amide surrogates were investigated and novel chiral N-(2-be
Tertiary aminoacids
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, (2008/06/13)
New α-(cyclic tert. aminophenyl)-aliphatic acids, e.g. those of the formula STR1 AND FUNCTIONAL DERIVATIVES THEREOF, ARE ANTI-INFLAMMATORY AGENTS.
