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首页> 外文期刊>Medicinal chemistry research: an international journal for rapid communications on design and mechanisms of action of biologically active agents >^d>Department of Chemistry, Maharashtra Udayagiri Mahavidyalaya, Udgir, India
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^d>Department of Chemistry, Maharashtra Udayagiri Mahavidyalaya, Udgir, India

机译：^ d>化学系，马哈拉施特拉邦Udayagiri Mahavidyalaya，乌吉尔，印度

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摘要

A series of novel 3-hydroxy-2-(2,4,5-trimethoxy-phenyl)-4H-chromen-4-one (flavonol) derivatives (2a-u) of biological interest have been prepared via CLAISEN-SCHMIDT condensation followed by ALGAR-FLYNN-OYAMADA reaction and to search for the potent nonste-roidal anti-inflammatory agents from this novel series. All the synthesized compounds have been screened for their in vitro proinfiammatory cytokines tumor necrosis factor (TNF-a) and interleukin-6 (IL-6) inhibitory activity along with antimicrobial activity. As many as three compounds viz. 2h, 21, and 2q from this novel series were found to be potent TNF-alpha and IL-6 inhibitor (up to 72-81 % TNF-alpha and 86-92 % IL-6 inhibitory activity) but at 10 uM concentration as compared with the standard dexamethasone (71 % TNF-a and 84 % IL-6 inhibitory activities at 1 uM concentration). While the compounds 2d, 2m, 2n, and 2s were found to be potent antimicrobial agent showing even 2-2.5-fold more potency than that of standard ciprofloxacin and miconazole at the same MIC value of 10 mug/mL.
机译：通过CLAISEN-SCHMIDT缩合反应，制备了一系列具有生物学意义的新型3-羟基-2-（2,4,5-三甲氧基-苯基）-4H-铬-4-酮（黄酮醇）衍生物（2a-u）通过ALGAR-FLYNN-OYAMADA反应，并从该新系列中寻找有效的非甾体类抗炎药。筛选了所有合成的化合物的体外促炎性细胞因子肿瘤坏死因子（TNF-a）和白介素6（IL-6）抑制活性以及抗菌活性。多达三种化合物。发现该新系列的2h，21和2q是有效的TNF-α和IL-6抑制剂（高达72-81％的TNF-alpha和86-92％的IL-6抑制活性），但浓度为10uM与标准地塞米松相比（1 uM浓度下71％TNF-a和84％IL-6抑制活性）。虽然发现化合物2d，2m，2n和2s是有效的抗菌剂，但在相同的MIC值为10杯/毫升的情况下，其效力甚至比标准环丙沙星和咪康唑高出2-2.5倍。

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