Solid phase synthesis of sulphonamides: novel ligands of 5-HT6 receptors.
Using solid phase synthesis techniques, we have rapidly obtained a series of eight aryl sulphonamides derived from putrescine. These conjugates with various aryl groups were evaluated for their affinity towards 5-HT6 receptors in man. This evaluation revealed the interest of two compounds which present the same activity level, in the submicromolar range, as two reference derivatives. The most potent will be considered as a new lead for further investigations.
Renault
J
J
UPRES Synthèse et extraction de molécules à visée thérapeutique, Université de Rennes I, Faculté des Sciences Biologiques et Médicales, France.
Fabis
F
F
Dauphin
F
F
Lebranchu
M
M
Le Roch
M
M
Butt
S
S
Uriac
P
P
Rault
S
S
D006801:Humans; D008024:Ligands; D008238:Lysergic Acid Diethylamide / Q000378:metabolism; D011700:Putrescine / Q000031:analogs & derivatives / Q000138:chemical synthesis; D011985:Receptors, Serotonin / Q000378:metabolism*; D012702:Serotonin Antagonists / Q000378:metabolism; D013449:Sulfonamides / Q000138:chemical synthesis* / Q000378:metabolism*
D008024:Ligands; D011985:Receptors, Serotonin; D012702:Serotonin Antagonists; D013449:Sulfonamides; C097216:serotonin 6 receptor; D008238:Lysergic Acid Diethylamide; D011700:Putrescine