Solid-phase synthesis of new Trp(Nps)-containing dipeptide derivatives as TRPV1 channel blockers.
Trp(Nps)-Lys-NH(2) derivatives, bearing alkyl or guanidine groups either at the N-terminus or on the Lys side-chain or at both positions were conveniently prepared on solid-phase and evaluated as TRPV1 channel antagonists.
Pérez de Vega
Ma Jesús
MJ
Instituto de Química Médica, CSIC, Juan de la Cierva, 3, 28006 Madrid, Spain.
García-López
Ma Teresa
MT
Zaccaro
Laura
L
Royo
Miriam
M
Albericio
Fernando
F
Fernández-Carvajal
Asia
A
Ferrer-Montiel
Antonio
A
González-Muñiz
Rosario
R
D000473:Alkanes; D004151:Dipeptides / Q000138:chemical synthesis* / Q000494:pharmacology*; D019791:Guanidine; D008239:Lysine; D013329:Structure-Activity Relationship; D050916:TRPV Cation Channels / Q000037:antagonists & inhibitors*; D014364:Tryptophan
D000473:Alkanes; D004151:Dipeptides; D050916:TRPV Cation Channels; C494482:TRPV1 protein, human; D014364:Tryptophan; D019791:Guanidine; D008239:Lysine