- Synthesis of benzenepropanamine analogues as non-detergent spermicides with antitrichomonas and anticandida activities
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Fifteen analogues of benzenepropanamine were synthesized and evaluated for their spermicidal as well as microbicidal activities against Trichomonas vaginalis and Candida spp. Several compounds showed appreciable dual activities. Compound 12 exhibited good
- Kiran Kumar,Sharma, Vishnu Lal,Kumar, Manish,Shukla, Praveen Kumar,Tiwari, Pratibha,Jain, Rajeev Kumar,Maikhuri, Jagdamba Prasad,Singh, Divya,Gupta, Gopal,Singh, Man Mohan
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p. 6593 - 6600
(2007/10/03)
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- New 1-aryl-3-(4-arylpiperazin-1-yl)propane derivatives, with dual action at 5-HT1A serotonin receptors and serotonin transporter, as a new class of antidepressants
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In a search toward new and efficient antidepressants, 1-aryl-3-(4-arylpiperazin-1-yl)propane derivatives were designed, synthesized, and evaluated for 5-HT reuptake inhibition and 5-HT1A receptor antagonism. This dual pharmacological profile should lead, in principle, to a rapid and pronounced enhancement in serotoninergic neurotransmission and consequently to a more efficacious treatment of depression. The design was based on coupling structural moieties related to inhibition of serotonin reuptake, such as γ-phenoxypropylamines, to arylpiperazines, typical 5-HT1A ligands. In binding studies, several compounds showed affinity at the 5-HT transporter and 5-HT1A receptors. Antidepressant-like activity was initially assayed in the forced swimming test with those compounds with Ki 1A receptor. Furthermore, the antidepressant-like properties of 12f, 28a, and 28b, which exhibited 5-HT1A receptor antagonistic property in the latter study, were also evaluated in the learned helplessness test in rats. Among these three compounds, 28b (1-benzo[b]thiophene-3-yl)-3-[4-(2-methoxyphenyl)-1-ylpropan-1-ol) showed the higher affinity at both the 5-HT transporter and 5-HT1A receptors (Ki = 20 nM in both cases) and was also active in the other pharmacological tests. Such a pharmacological profile could lead to a new class of antidepressants with a dual mechanism of action and a faster onset of action.
- Martínez-Esparza,Oficialdegui,Pérez-Silanes,Heras,Orús,Palop,Lasheras,Roca,Mourelle,Bosch,Del Castillo,Tordera,Del Río,Monge
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p. 418 - 428
(2007/10/03)
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