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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >One-pot synthesis and molecular docking of some new spiropyranindol-2-one derivatives as immunomodulatory agents and in vitro antimicrobial potential with DNA gyrase inhibitor
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One-pot synthesis and molecular docking of some new spiropyranindol-2-one derivatives as immunomodulatory agents and in vitro antimicrobial potential with DNA gyrase inhibitor

机译：一些新的螺吡喃吲哚-2-衍生物作为免疫调节剂和DNA乙酶抑制剂的体外抗微生物电位的一锅合成及分子对接

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摘要

a series of 2-oxospiro[indoline-3,4'-pyran]derivatives 4 and 7 were obtained in good yield under mild conditions from the one-pot reaction of indole-2,3-dione derivatives 1, appropriate methylene active nitriles 2 and beta-dicarbonyl compound 3 or 6. The newly synthesized compounds were characterized and evaluated for their in vitro antibacterial, antifungal as well as immunomodulatory activity. According to MIC values, the most potent compounds 4f, 4h, 7a, 7c, 7e, 7f, 7g, 8a, and 8c were evaluated for MBC and displayed high activity to killing pathogens with a good MBC value against norfloxacin as well as investigated against an extended panel of multidrug resistance bacteria (MDRB) and exhibited promising to moderate multidrug resistance activities, compounds 7f showed the much better than norfloxacin with higher potency results. Furthermore, the most potent compounds showed an increase in the intracellular killing activity of neutrophils which confirmed the immunostimulatory power. Eight of the nine active compounds exhibited inhibitory activities with IC50 ranged between (18.07 +/- 0.18) to (27.03 +/- 0.24) mu M stronger than ciprofloxacin (26.43 +/- 0.64 mu M) for S. aureus DNA gyrase. Molecular docking was performed inside the active site of S. aureus DNA gyrase to predict the binding mode. (C) 2019 Elsevier Masson SAS. All rights reserved.
机译：一系列2-氧化氢[吲哚-3,4'-吡喃]衍生物4和7在温和的条件下，从吲哚-2,3-二酮衍生物1的单罐反应，适当的亚甲基活性腈2获得良好的产率。和β-二羰基化合物3或6.对新合成的化合物进行了表征和评价其体外抗菌，抗真菌以及免疫调节活性。根据MIC值，对MBC评估最有效的化合物4F，4H，7A，7C，7E，7F，7G，8A和8C，并显示出高活性，以杀死具有良好的MBC值对诺氟沙星以及研究的良好MBC值。多药耐药细菌（MDRB）的扩展面板，并表现出适度的多药耐药活性，化合物7F比诺氟沙星更好，具有较高的效力结果。此外，最有效的化合物显示出嗜中性粒细胞的细胞内杀伤活性增加，所述中性粒细胞确认免疫刺激性。九个活性化合物中的八个表现出与IC50的抑制活性（18.07 +/- 0.18）至（27.03 +/- 0.24），比西普洛西氟苯胺（26.43 +/-0.64μm）为S.UUREUS DNA乙酸酯的um m。在S.UUREUS DNA丙糖酶的活性位点内进行分子对接以预测结合模式。 （c）2019年Elsevier Masson SAS。版权所有。

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