Active site directed docking studies: synthesis and pharmacological evaluation of cis-2,6-dimethyl piperidine sulfonamides as inhibitors of acetylcholinesterase.

Girisha HR; Narendra Sharath Chandra JN; Boppana S

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Active site directed docking studies: synthesis and pharmacological evaluation of cis-2,6-dimethyl piperidine sulfonamides as inhibitors of acetylcholinesterase.

机译：活性部位定向对接研究：顺式-2,6-二甲基哌啶磺酰胺作为乙酰胆碱酯酶抑制剂的合成和药理评价。

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Hypocholinergic function associated with Alzheimer's disease (AD) is well-accepted hypothesis, in this regard, many research attempts have been made to elevate the reduced cholinergic neurotransmission, among them two main treatment strategies were widely explored, namely stimulation of muscarinic receptor 1 and/or reversible inhibition of acetylcholinesterase (AChE) enzyme. In an attempt to improve the efficacy and to minimize general side effects of these AChE inhibitors, many lead molecules are developed in research; one among them is piperidine derivative. Donazepil is a widely prescribed AChE inhibitor which displays a piperidine ring in its structure. In the present study, we have docked cis-2,6-dimethyl piperidine sulfonamides (3a-i) on AChE enzyme and synthesized by nucleophilic substitution reaction between cis-2,6-dimethyl piperidine and alkyl/aryl sulfonyl chlorides in the presence of triethylamine. These piperidine sulfonamides were subjected to in vitro AChE enzyme inhibition studies and in vivo antiamnesic study to reverse scopolamine induced memory loss in rats. Two derivatives (3a and f) in this class of piperidines (3a-i) showed considerable inhibition against different sources of AChE in vitro and reduced average number of mistakes done by wistar rats as compared to scopolamine treated group in vivo (rodent memory evaluation).

机译：与阿尔茨海默氏病（AD）相关的低胆碱能功能是公认的假设，在这一方面，已经进行了许多研究来提高胆碱能神经传递的降低，其中广泛探索了两种主要的治疗策略，即刺激毒蕈碱受体1和/或对乙酰胆碱酯酶（AChE）酶的可逆抑制。为了提高这些AChE抑制剂的功效并最大程度地减少其副作用，许多铅分子正在研究中。其中之一是哌啶衍生物。 Donazepil是一种广泛使用的AChE抑制剂，在其结构中具有哌啶环。在本研究中，我们将顺式2,6-二甲基哌啶磺酰胺（3a-i）停在AChE酶上，并通过在顺式2,6-二甲基哌啶与烷基/芳基磺酰氯之间的亲核取代反应合成三乙胺。对这些哌啶磺酰胺进行了体外AChE酶抑制研究和体内抗记忆删除研究，以逆转东pol碱诱导的大鼠记忆丧失。与东pol碱治疗的体内组相比，此类哌啶（3a-i）中的两种衍生物（3a和f）在体外对AChE的不同来源显示出显着的抑制作用，并且wistar大鼠的平均失误次数减少（啮齿动物记忆评估）。

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《European Journal of Medicinal Chemistry: Chimie Therapeutique》 |2009年第10期|共6页
作者
Girisha HR; Narendra Sharath Chandra JN; Boppana S;
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中图分类医药、卫生;劳动卫生;
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1. Active site directed docking studies: synthesis and pharmacological evaluation of cis-2,6-dimethyl piperidine sulfonamides as inhibitors of acetylcholinesterase. [J] . Girisha HR, Narendra Sharath Chandra JN, Boppana S European Journal of Medicinal Chemistry: Chimie Therapeutique . 2009,第10期

机译：活性部位定向对接研究：顺式-2,6-二甲基哌啶磺酰胺作为乙酰胆碱酯酶抑制剂的合成和药理评价。
2. Design, synthesis, biological evaluation and molecular docking study of arylcarboxamido piperidine and piperazine-based hydroxamates as potential HDAC8 inhibitors with promising anticancer activity [J] . Trivedi Prakruti, Adhikari Nilanjan, Amin Sk Abdul, European journal of pharmaceutical sciences . 2019,第期

机译：芳基甲基甲醛哌啶和哌嗪基羟肟酸盐作为潜在HDAC8抑制剂的设计，合成，生物学评价及分子对接研究抗癌活性
3. Design, synthesis, biological evaluation and molecular docking study of arylcarboxamido piperidine and piperazine-based hydroxamates as potential HDAC8 inhibitors with promising anticancer activity [J] . Trivedi Prakruti, Adhikari Nilanjan, Amin Sk Abdul, European journal of pharmaceutical sciences . 2019,第期

机译：芳基甲基甲醛哌啶和哌嗪基羟肟酸盐作为潜在HDAC8抑制剂的设计，合成，生物学评价及分子对接研究抗癌活性
4. Mapping the Binding Site of a Large Set of Quinazoline Type EGF-R Inhibitors Using Molecular Field Analyses and Molecular Docking Studies [C] . 北京大学中医药现代研究中心2003年年会论文集 . 2004

机译：使用分子场分析和分子对接研究定位一大套喹唑啉型EGF-R抑制剂的结合位点
5. Part One. Synthesis of optically active tryptophan derivatives with potential activity as indoleamine 2,3-dioxygenase inhibitors: An approach via asymmetric catalytic hydrogenation. Part Two. Design, synthesis and pharmacology of selective ligands for alpha1-containing GABA(A)/benzodiazepine receptor subtypes: SAR studies of beta-carbolines at positions -3 and -6 and their corresponding bivalent ligands. Part Three. First enantiospecific total synthesis of the important biogenetic intermediates, (+)-polyneuridine and (+)-polyneuridine aldehyde, as well as 16-epi-vellosimine and macusine A. [D] . Yin, Wenyuan. 2007

机译：第一部分。具有吲哚胺2,3-二加氧酶抑制剂潜在活性的旋光色氨酸衍生物的合成：一种通过不对称催化氢化的方法。第二部分。含α1的GABA（A）/苯并二氮杂receptor受体亚型的选择性配体的设计，合成和药理作用：位于-3和-6位的β-咔啉及其相应的二价配体的SAR研究。第三部分。重要生物遗传中间体，（+）-聚神经氨酸和（+）-聚神经氨酸醛，以及16-表-维西辛和Macusine A的首次对映体全合成。
6. Synthesis Pharmacological Profile and Docking Studies of New Sulfonamides Designed as Phosphodiesterase-4 Inhibitors [O] . Isabelle Karine da Costa Nunes, Everton Tenório de Souza, Suzana Vanessa S. Cardozo, -1

机译：被设计为磷酸二酯酶4抑制剂的新型磺酰胺的合成药理作用和对接研究
7. Synthesis, Pharmacological Profile and Docking Studies of New Sulfonamides Designed as Phosphodiesterase-4 Inhibitors. [O] . Isabelle Karine da Costa Nunes, Everton Tenório de Souza, Suzana Vanessa S Cardozo, 2016

机译：新型磺胺类药物的合成，药理学特征和对接研究设计为磷酸二酯酶-4抑制剂。

Active site directed docking studies: synthesis and pharmacological evaluation of cis-2,6-dimethyl piperidine sulfonamides as inhibitors of acetylcholinesterase.

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