Title compds. I [wherein R1 = H; R2 = (un)substituted benzyl or 2-phenylethyl; R3 = H, halo or alkoxy; R4 = (CH2)nNH; n = 0-3; R5 = O or S; R6 = NHCH2; R7 = t-Bu or CF3] were prepd. as vanilloid TRPV1 receptor antagonists. For instance, thiourea II was synthesized in 42% yield by nucleophilic addn. of 4-tert-butylbenzyl isothiocyanate with the corresponding sulfamoylaniline (prepn. given). II was found to inhibit TRPV1-dependent responses with an affinity that was significantly greater than that of the classic TRPV1 receptor antagonist, capsazepine, in both in vitro and in vivo studies. Therefore, I can be used for the prepn. of medicaments for the treatment of inflammatory states.
Preparation of sulfamoylphenyl thiourea derivatives as vanilloid TRPV1 receptor antagonists for the treatment of inflammatory states.
BARALDI, Pier Giovanni;BOREA, Pier Andrea;
2006
Abstract
Title compds. I [wherein R1 = H; R2 = (un)substituted benzyl or 2-phenylethyl; R3 = H, halo or alkoxy; R4 = (CH2)nNH; n = 0-3; R5 = O or S; R6 = NHCH2; R7 = t-Bu or CF3] were prepd. as vanilloid TRPV1 receptor antagonists. For instance, thiourea II was synthesized in 42% yield by nucleophilic addn. of 4-tert-butylbenzyl isothiocyanate with the corresponding sulfamoylaniline (prepn. given). II was found to inhibit TRPV1-dependent responses with an affinity that was significantly greater than that of the classic TRPV1 receptor antagonist, capsazepine, in both in vitro and in vivo studies. Therefore, I can be used for the prepn. of medicaments for the treatment of inflammatory states.I documenti in SFERA sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
