3-O-substituted benzyl pyridazinone derivatives as COX inhibitors.

Chintakunta VK; Akella V; Vedula MS; Mamnoor PK; Mishra P; Casturi SR; Vangoori A; Rajagopalan R

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3-O-substituted benzyl pyridazinone derivatives as COX inhibitors.

机译：3-O-取代的苄基哒嗪酮衍生物作为COX抑制剂。

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New 3-O-substituted benzyl pyridazinone compounds have been synthesised and evaluated for their cyclooxygenase inhibitory activity and COX-2 selectivity. Among the compounds synthesised, three compounds (11b-11d) have shown in vitro COX-2 selectivity. These compounds have been evaluated for their in vivo potential using carrageenan-induced rat paw edema assay. One compound (11b) showed 32% anti-inflammatory activity at 30 mgkg(-1) dose.

机译：已经合成了新的3-O-取代的苄基哒嗪酮化合物，并对其环加氧酶的抑制活性和COX-2选择性进行了评估。在合成的化合物中，三种化合物（11b-11d）具有体外COX-2选择性。已使用角叉菜胶诱导的大鼠爪水肿测定法评估了这些化合物的体内潜力。一种化合物（11b）在30 mgkg（-1）剂量下显示32％的抗炎活性。

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来源
《European Journal of Medicinal Chemistry: Chimie Therapeutique》 |2002年第4期|共9页
作者
Chintakunta VK; Akella V; Vedula MS; Mamnoor PK; Mishra P; Casturi SR; Vangoori A; Rajagopalan R;
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正文语种 eng
中图分类医药、卫生;
关键词
Cyclooxygenase Inhibitors; Pyridazines; 环加氧酶抑制药; 哒嗪类;

机译：Cyclooxygenase Inhibitors;Pyridazines;环加氧酶抑制药;哒嗪类;

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1. 3-O-substituted benzyl pyridazinone derivatives as COX inhibitors. [J] . Chintakunta VK, Akella V, Vedula MS, European Journal of Medicinal Chemistry: Chimie Therapeutique . 2002,第4期

机译：3-O-取代的苄基哒嗪酮衍生物作为COX抑制剂。
2. SAR studies of pyridazinone derivatives as novel glucan synthase inhibitors. [J] . Zhou G, Ting PC, Aslanian R, Bioorganic and Medicinal Chemistry Letters . 2011,第10期

机译：SAR研究哒嗪酮衍生物作为新型葡聚糖合成酶抑制剂。
3. Synthesis and biological evaluation of pyridazinone derivatives as selective COX-2 inhibitors and potential anti-inflammatory agents [J] . Ahmed Eman M., Kassab Asmaa E., El-Malah Afaf A., European Journal of Medicinal Chemistry: Chimie Therapeutique . 2019,第期

机译：哒嗪酮衍生物作为选择性Cox-2抑制剂和潜在抗炎剂的合成与生物学评价
4. Glassy 2-(1-benzyl-2-styryl-6-methylpyridin-4(1-H)-ylidene) fragment containing 1H-indene-1,3(2H)-dione and pyrimidine-2,4,6(1H,3H,5H)-trione derivatives with light-emitting and amplified spontaneous emission properties [C] . Elmars Zarins, Julija Pervenecka, Elina Misina, Conference on Fiber Lasers and Glass Photonics: Materials through Applications . 2020

机译：含1H-茚-1,3（2H）-二酮和嘧啶-2,4,6（1H）的玻璃状2-（1-苄基-2-苯乙烯基-6-甲基吡啶-4（1-H）-亚烷基）片段具有发光和放大的自发发射特性的3H，5H）-三酮衍生物
5. Synthesis, lipophilicity, and antifungal properties of 3(2H)-pyridazinone derivatives. [D] . Anwair, Massud Allag S. 2005

机译：3（2H）-哒嗪酮衍生物的合成，亲脂性和抗真菌特性。
6. Synthesis and biological evaluation of new 3(2H)-pyridazinone derivatives as non-toxic anti-proliferative compounds against human colon carcinoma HCT116 cells [O] . Zeynep Özdemir, Semra Utku, Bijo Mathew, 2020

机译：新的3（2H）-哒嗪酮衍生物作为抗人结肠癌HCT116细胞无毒抗增殖化合物的合成及生物学评价
7. Docking and quantitative structure-activity relationship of bi-cyclic heteroaromatic pyridazinone and pyrazolone derivatives as phosphodiesterase 3A (PDE3A) inhibitors. [O] . Camila Muñoz-Gutiérrez, Daniela Cáceres-Rojas, Francisco Adasme-Carreño, 2017

机译：双环杂芳基哒嗪酮和吡唑啉酮衍生物作为磷酸二酯酶3a（pDE3a）抑制剂的对接和定量构效关系。

3-O-substituted benzyl pyridazinone derivatives as COX inhibitors.

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