Design, synthesis, pharmacological evaluation and computational studies of 1-(biphenyl-4-yl)-2-[4-(substituted phenyl)-piperazin-1-yl]ethanones as potential antipsychotics

BhosaleS.H.; KanhedA.M.; DashR.C.; SuryawanshiM.R.; MahadikK.R.

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Design, synthesis, pharmacological evaluation and computational studies of 1-(biphenyl-4-yl)-2-[4-(substituted phenyl)-piperazin-1-yl]ethanones as potential antipsychotics

机译：1-（联苯-4-基）-2- [4-（取代苯基）-哌嗪-1-基]乙酮作为潜在抗精神病药的设计，合成，药理学评估和计算研究

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This article describes the design of biphenyl moiety linked with aryl piperazine and syntheses of fourteen 1-(biphenyl-4-yl)-2-[4-(substituted phenyl)-piperazin-1-yl]ethanone derivatives along with their pharmacological evaluation for antipsychotic activity and computational studies including quantitative structure activity relationship (QSAR) and descriptor based similarity study. All compounds were found to exhibit considerable anti-dopaminergic and anti-serotonergic activity in behavioural models. Among all derivatives, compound 1-(biphenyl-4-yl)-2-[4-(2-methoxyphenyl)-piperazin-1- yl]ethanone (3c) and 1-(biphenyl-4-yl)-2-[4-(2,3-dichlorophenyl)-piperazin-1-yl] ethanone (3k) showed impressive antipsychotic profile with lower potency for catalepsy induction. These results were found to be sturdily matching with docking study in designing of compounds with homology model of human dopamine D2 receptor. Also the QSAR study strongly supports the obtained results.

机译：本文介绍了与芳基哌嗪连接的联苯部分的设计以及十四种1-（联苯基-4-基）-2- [4-（取代苯基）-哌嗪-1-基]乙酮衍生物的合成及其药理学评价。抗精神病活性和计算研究，包括定量结构活性关系（QSAR）和基于描述符的相似性研究。发现所有化合物在行为模型中均表现出相当大的抗多巴胺能和抗5-羟色胺能活性。在所有衍生物中，化合物1-（联苯基-4-基）-2- [4-（2-甲氧基苯基）-哌嗪-1-基]乙酮（3c）和1-（联苯基-4-基）-2- [ 4-（2,3-二氯苯基）-哌嗪-1-基]乙酮（3k）表现出令人印象深刻的抗精神病药物特性，并具有较低的诱导僵尸症的功效。发现这些结果与设计与人多巴胺D2受体同源性模型的化合物的对接研究牢固地匹配。 QSAR研究也强烈支持所获得的结果。

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来源
《European Journal of Medicinal Chemistry: Chimie Therapeutique》 |2014年第null期|共8页
作者
BhosaleS.H.; KanhedA.M.; DashR.C.; SuryawanshiM.R.; MahadikK.R.;
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正文语种 eng
中图分类药学;
关键词
1-(Biphenyl-4-yl)-2-4-(substituted phenyl)-piperazin-1-yl ethanones; Antipsychotic; Descriptor based similarity study; Pharmacological evaluation; QSAR;

机译：1-（Biphenyl-4-yl）-2- [4-（取代苯基）-哌嗪-1-基]乙酮;抗精神病药物;基于描述符的相似性研究;药理学评估;QSAR;

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1. Design, synthesis, pharmacological evaluation and computational studies of 1-(biphenyl-4-yl)-2-[4-(substituted phenyl)-piperazin-1-yl]ethanones as potential antipsychotics [J] . BhosaleS.H., KanhedA.M., DashR.C., European Journal of Medicinal Chemistry: Chimie Therapeutique . 2014,第Null期

机译：1-（联苯-4-基）-2- [4-（取代苯基）-哌嗪-1-基]乙酮作为潜在抗精神病药的设计，合成，药理学评估和计算研究
2. Synthesis, computational studies and preliminary pharmacological evaluation of 2-(4-(aryl substituted) piperazin-1-yl) N, N-diphenylacetamides as potential antipsychotics. [J] . Kumar S, Wahi AK, Singh R European Journal of Medicinal Chemistry: Chimie Therapeutique . 2011,第9期

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3. Design, synthesis, pharmacological evaluation and descriptor based similarities study of N,N-diphenyl-2-[4-(substituted phenyl)piperazin-1-yl] acetamides as potential antipsychotics [J] . DashR.C., BhosaleS.H., ShelkeS.M., Medicinal chemistry . 2012,第6期

机译：N，N-二苯基-2- [4-（取代的苯基）哌嗪-1-基]乙酰胺作为潜在的抗精神病药的设计，合成，药理评价和基于描述符的相似性研究
4. Synthesis and Properties of a New Unsymmetrical Diarylethene 1-{2-methyl-5-(4-trifluoromethyl)phenyl-3-thienyl}-2-{2-methyl-5-(3-chlorine)phenyl-3-thienyl} Perfluorocyclopentene [C] . Shuying Li, Ruiming Lu, Daobin Zhang, International Conference on Materials chemistry and environmental protection . 2015

机译：新的非对称二芳基乙烯1- {2-甲基 - 5-（4-三氟甲基）苯基-3-噻吩基} - 2 - {2-甲基-5-（3-氯）苯基 -3的合成及性质-thienyl}全氟环戊烯
5. STUDY OF THE KINETICS OF THE (1,5)-SIGMATROPIC PHENYL REARRANGEMENT IN 1-(PARA-SUBSTITUTED PHENYL)-2, 3, 4, 5-TETRAPHENYL-2, 4-CYCLOPENTADIEN-1-OLS [D] . OLDAKER, GUY BROOKLYN, III. 1979

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7. Synthesis, computational studies and preliminary pharmacological evaluation of 2-[4-(aryl substituted) piperazin-1-yl]-N-benzylacetamides as potential antipsychotics [O] . Sushil Kumar, A.K. Wahi, Ranjit Singh 2016

机译：2- [4-（芳基取代）哌嗪-1-基] -N-苄基乙酰胺作为潜在抗精神病药的合成，计算研究和初步药理学评价

Design, synthesis, pharmacological evaluation and computational studies of 1-(biphenyl-4-yl)-2-[4-(substituted phenyl)-piperazin-1-yl]ethanones as potential antipsychotics

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