Sulfonamides with the N-alkyl-N'-dialkylguanidine moiety as 5-HT7 receptor ligands.
A series of arylsulfonamides containing guanidine incorporated in the structure of secondary amines (piperidine, piperazine) was synthesized on SynPhase Lanterns and evaluated for 5-HT(1A), 5-HT(2A), and 5-HT(7) receptors. The results demonstrated that N-alkyl-N'-dialkylguanidines displayed good 5-HT(7)/5-HT(1A) selectivity and may be regarded as promising structural core for development of 5-HT(7) ligands.
Zajdel
Paweł
P
Department of Medicinal Chemistry, Jagiellonian University Medical College, 30-688 Kraków, Poland. mfzajdel@cyf-kr.edu.pl
Subra
Gilles
G
Verdie
Pascal
P
Gabzdyl
Ewa
E
Bojarski
Andrzej J
AJ
Duszyńska
Beata
B
Martinez
Jean
J
Pawłowski
Maciej
M
D000818:Animals; D006146:Guanidines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D006801:Humans; D008024:Ligands; D051381:Rats; D044282:Receptor, Serotonin, 5-HT1A / Q000378:metabolism; D044402:Receptor, Serotonin, 5-HT2A / Q000378:metabolism; D011985:Receptors, Serotonin / Q000737:chemistry* / Q000378:metabolism; D058829:Serotonin 5-HT1 Receptor Antagonists; D058830:Serotonin 5-HT2 Receptor Antagonists; D012702:Serotonin Antagonists / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology
D006146:Guanidines; D008024:Ligands; D044402:Receptor, Serotonin, 5-HT2A; D011985:Receptors, Serotonin; D058829:Serotonin 5-HT1 Receptor Antagonists; D058830:Serotonin 5-HT2 Receptor Antagonists; D012702:Serotonin Antagonists; D013449:Sulfonamides; C104425:serotonin 7 receptor; D044282:Receptor, Serotonin, 5-HT1A