71933-93-2Relevant academic research and scientific papers
Synthesis and pharmacological evaluation of benzamide derivatives as selective 5-HT4 receptor agonists
Sonda, Shuji,Kawahara, Toshio,Katayama, Kenichi,Sato, Noriko,Asano, Kiyoshi
, p. 3295 - 3308 (2007/10/03)
It is thought that selective 5-HT4 receptor agonists-such as 4-amino-5-chloro-2-methoxy-N-[1-(6-oxo-6-phenylhexyl)piperidin-4-ylmethyl] benzamide (2)-have the ability to enhance both upper and lower gastrointestinal motility without any significant adverse effects. Modification of 2 was performed. Variation of the piperidin-4-ylmethyl moiety of 2 led to a decrease in the binding affinity for the 5-HT4 receptor. Following conversion of the carbonyl group on the benzoyl part to a hydroxyl or sulfoxide group, the binding affinity for the 5-HT4 receptor was retained although the effect on defecation was reduced. Many of the 4-amino-5-chloro-2-methoxy-N- (piperidin-4-ylmethyl)benzamides that had a ether or sulfide moiety in the side-chain part at the 1-position of the piperidine exhibited high affinity for the 5-HT4 receptor. Among these, phenylthio 41c and benzylthio derivative 44 were selective 5-HT4 receptor agonists, and had a similar effect on defecation to compound 2.
Homologs of idoxifene: Variation of estrogen receptor binding and calmodulin antagonism with chain length
Hardcastle, Ian R.,Rowlands, Martin G.,Grimshaw, Rachel M.,Houghton, John,Jarman, Michael,Sharff, Andrew,Neidle, Stephen
, p. 999 - 1004 (2007/10/03)
A series of homologs of idoxifene [1a, (E)-1-[4-(N- pyrrolidinoethoxy)phenyl]-1-(4-iodophenyl)-2-phenyl-1-butene] and selected homologs of 4-iodotamoxifen [2a, (E)-1-[4-[(N-dimethylamino)ethoxy]phenyl]- 1-(4-iodophenyl)-2-phenyl-1-butene] with the side ch
