Synthesis of Some Novel 2,6-Disubstituted Pyridazin-3(2H)-one Derivatives as Analgesic, Anti-Inflammatory, and Non-Ulcerogenic Agents

Ibrahim Tamer H.; Loksha Yasser M.; Elshihawy Hosam A.; Khodeer Dina M.; Said Mohamed M.

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Synthesis of Some Novel 2,6-Disubstituted Pyridazin-3(2H)-one Derivatives as Analgesic, Anti-Inflammatory, and Non-Ulcerogenic Agents

机译：一些新型2,6-二取代的哒嗪-3（2H） - 酮衍生物作为镇痛，抗炎和非溃疡性剂的合成

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Some novel 2,6-disubstituted pyridazine-3(2H)-one derivatives were synthesized and evaluated for in vitro cyclooxygenase-2 (COX-2) inhibitory efficacy. Compounds 2-{[3-(2-methylphenoxy)-6-oxopyridazin-1(6H)-yl]methyl}-1H-isoindole-1,3(2H)-dione (5a), 2-propyl-6-(o-tolyloxy)pyridazin-3(2H)-one (6a), and 2-benzyl-6-(3,5-dimethyl-1H-pyrazol-1-yl)pyridazin-3(2H)-one (16a) showed the most potent COX-2 inhibitory activity with IC50 values of 0.19, 0.11, and 0.24M, respectively. The synthesized compounds with the highest COX-2 selectivity indices were evaluated for their anti-inflammatory, analgesic, and ulcerogenic activities. Compounds 6a and 16a demonstrated the most potent and consistent anti-inflammatory activity over the synthesized compounds, which was significantly higher than that of celecoxib in the carrageenin rat paw edema model and with milder ulcer scoring than that of indomethacin in the ulcerogenicity screening.

机译：一些新的2,6-二取代的哒嗪-3（2H）-ONE衍生物被合成并评价体外环氧化酶-2（COX-2）抑制效力。化合物2 - {[3-（2-甲基苯氧基）-6-氧气吡啶嗪-1（6h） - 甲基]甲基} -1H-异吲哚-1,3（2h） - 二硫醚（5a），2-丙基-6-（甲苯甲酰基-3（2H） - ONE（6A）和2-苄基-6-（3,5-二甲基-1H-吡唑-1-基）Pyridazin-3（2H） - One（16A）显示出来最有效的COX-2抑制活性，IC 50值分别为0.19,0.11和0.24米。评价具有最高COX-2选择性指数的合成化合物，用于其抗炎，镇痛和溃疡性活性。化合物6a和16a证明了合成化合物上最有效和一致的抗炎活性，其显着高于角叉菜胶爪水肿模型中的塞克西布含量，并且具有比溃疡性筛选中的吲哚美辛含量更高的溃疡率。

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来源
《Archiv der Pharmazie》 |2017年第9期|共13页
作者
Ibrahim Tamer H.; Loksha Yasser M.; Elshihawy Hosam A.; Khodeer Dina M.; Said Mohamed M.;
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作者单位

Sinai Univ Fac Pharm &

Pharmaceut Ind Dept Pharmaceut Chem Al Arish 31751 North Sinai Egypt;

Sinai Univ Fac Pharm &

Pharmaceut Ind Dept Pharmaceut Chem Al Arish 31751 North Sinai Egypt;

Suez Canal Univ Fac Pharm Dept Organ Pharmaceut Chem Ismailia Egypt;

Suez Canal Univ Fac Pharm Dept Pharmacol &

Toxicol Ismailia Egypt;

Suez Canal Univ Fac Pharm Dept Organ Pharmaceut Chem Ismailia Egypt;

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原文格式 PDF
正文语种 ger
中图分类药学;
关键词
Analgesic activity; Anti-inflammatory; COX-1; COX-2; Pyridazinone;

机译：镇痛活动;抗炎;COX-1;COX-2;哒嗪酮;

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1. Synthesis of Some Novel 2,6-Disubstituted Pyridazin-3(2H)-one Derivatives as Analgesic, Anti-Inflammatory, and Non-Ulcerogenic Agents [J] . Ibrahim Tamer H., Loksha Yasser M., Elshihawy Hosam A., Archiv der Pharmazie . 2017,第9期

机译：一些新型2,6-二取代的哒嗪-3（2H） - 酮衍生物作为镇痛，抗炎和非溃疡性剂的合成
2. Synthesis and Pharmacological Evaluation of Novel 1-(2-(Benzoyl-Substituted-2-phenyl-1H-Indol-5-Carbony) Hydrazinyloxy) Vinyl Nitrate Derivatives as Potent Non-Ulcerogenic, Analgesic and Anti-Inflammatory Agents [J] . Vinod J. Mokale Mayuresh K. Raut Prashant J. Burange Navneet S. Dhoot Shashikant V. Bhandari Kailash G. Bothara Jitendra B. Naik Medicinal Chemistry . 2010,第4期

机译：新型1-（2-（苯甲酰基取代的-2-苯基-1H-吲哚-5-碳）肼氧基酰氧基）硝酸乙烯酯衍生物的合成和药理学评价为有效的非致溃疡性，镇痛和消炎药
3. Synthesis and pharmacological evaluation of novel 1-(2-(benzoyl-substituted-2-phenyl-1H-indol-5-carbony) hydrazinyloxy) vinyl nitrate derivatives as potent non-ulcerogenic, analgesic and anti-inflammatory agents. [J] . Mokale VJ, Raut MK, Burange PJ, Medicinal chemistry . 2010,第4期

机译：新型的1-（2-（苯甲酰基取代的-2-苯基-1H-吲哚-5-碳原子）肼基氧基）乙烯基硝酸酯衍生物的合成和药理学评估，这些衍生物具有有效的无溃疡作用，镇痛作用和抗炎作用。
4. Enantioselective Photodimerization of a 2,6-Disubstituted Anthracene Derivative Assisted by a One-Handed Homo-Double Helix Formation [C] . Akio Urushima, Makoto Tanaka, Naomichi Horimoto 日本化学会春季年会講演予稿集 . 2018

机译：通过单手同源双螺旋形成辅助2,6二二偶蒽衍生物的映选择性光电二聚体
5. Antiviral Agents: 3,5-Disubstituted 1,2,4-Oxadiazole Derivatives and Novel Peptidomimetics Containing Hydroxyethyl Isostere and Imidazolidinone Structures. [D] . Krake, Susann H. 2013

机译：抗病毒剂：3,5-二取代的1,2,4-恶二唑衍生物和新型的模拟拟肽，其中含有羟乙基等排酮和咪唑烷酮结构。
6. Synthesis comparative docking and pharmacological activity of naproxen amino acid derivatives as possible anti-inflammatory and analgesic agents [O] . Ahmed A Elhenawy, LM Al-Harbi, Gaber O Moustafa, 2019

机译：萘普生氨基酸衍生物作为抗炎和镇痛药的合成比较对接和药理活性
7. Design, synthesis, and evaluation of anti-inflammatory, analgesic, ulcerogenicity, and nitric oxide releasing studies of novel indomethacin analogs as non-ulcerogenic derivatives [O] . Shashikant V. Bhandari, Jignesh K. Parikh, Kailash G. Bothara, 2010

机译：抗炎，镇痛，溃疡性和一氧化氮释放研究的设计，合成和评价，作为非溃疡性衍生物的新型吲哚美嗪类似物

Synthesis of Some Novel 2,6-Disubstituted Pyridazin-3(2H)-one Derivatives as Analgesic, Anti-Inflammatory, and Non-Ulcerogenic Agents

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