16296-90-5Relevant academic research and scientific papers
Novel inhibitors of chymase
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Page/Page column 54, (2008/06/13)
The present invention is directed to a compound of formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof, and methods for treating inflammatory and serine protease mediated disorders.
New 3-[4-(aryl)piperazin-1-yl]-1-(benzo[b]thiophen-3-yl)propane derivatives with dual action at 5-HT1A serotonin receptors and serotonin transporter as a new class of antidepressants
Martinez, Javier,Perez, Silvia,Oficialdegui, Ana M,Heras, Begona,Orus, Lara,Villanueva, Helena,Palop, Juan A,Roca, Joan,Mourelle, Marisa,Bosch, Ana,Del Castillo, Juan-C,Lasheras, Berta,Tordera, Rosa,Del Rio, Joaquin,Monge, Antonio
, p. 55 - 61 (2007/10/03)
A series of new 3-[4-(aryl)piperazin-1-yl]-1-(benzo[b]thiophen-3-yl)propane derivatives were synthesized in an attempt to find a new class of antidepressant drugs with dual activity at 5-HT1A serotonin receptors and serotonin transporter. Title compounds were evaluated for in vitro activity on 5-HT1A receptor and 5-HT transporter. They show high nanomolar affinity for both activities, and in particular, compounds 1-(5-chlorobenzo[b]thiophen-3-yl)-3-[4-(2-methoxyphenyl)piperazin-1-yl] propan-1-ol (7) and 1-(5-fluorobenzo[b]thiophen-3-yl)-3-[4-(2-methoxyphenyl)piperazin-1-yl] propan-1-ol (8) show values (nM) of Ki = 30 and 2.3 for 5-HT1A receptors and Ki = 30 and 12 for serotonin transporters, respectively. In GTPγS binding assays, compound 8 revealed antagonist properties to 5-HT1A receptors. Such a pharmacological profile could lead to potent antidepressant agents with new dual mechanism of action.
Condensed thiazole derivatives, having 5-HT receptor affinity
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, (2008/06/13)
Compounds of formula I STR1 in which A is S(O) p or O;p is 0, 1 or 2;g is 0, 1, 2, 3, or 4;n is 2 or 3; andR 1, R 2, R 3, R 4 and R 5 are optional substituents have utility in the treatment of central nervous system disorders, for example depression, anxiety, psychoses (for example schizophrenia), tardive dyskinesia, obesity, drug addiction, drug abuse, cognitive disorders, Alzheimer''s disease, senile dementia, cerebral ischemia, obsessive-compulsive behavior, panic attacks, social phobias, eating disorders and anorexia, non-insulin dependent diabetes mellitus, hyperglycemia, and stress.
