Operative conversions of 3-carboxy-4-quinolones into 3-nitro-4-quinolones via ipso-nitration: potential antifilarial agents as inhibitors of Brugia malayi thymidylate kinase

Azad Chandra S.; Balaramnavar Vishal M.; Khan Imran A.; Doharey Pawan K.; Saxena Jitendra K.; Saxena Anil K.

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Operative conversions of 3-carboxy-4-quinolones into 3-nitro-4-quinolones via ipso-nitration: potential antifilarial agents as inhibitors of Brugia malayi thymidylate kinase

机译：通过IPSO - 硝化剂将3-羧基-4-喹诺酮酮的手术转换成3硝基-4-喹啉酮：潜在的防污剂，作为Brugia Malayi胸苷酸氨酯激酶的抑制剂

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An efficient, cost effective and green methodology for ipso nitration in the synthesis of the 3-nitro derivative of 3-carboxy 4-quinolones has been developed by the quantitative use of copper acetate and silver nitrate in water. The observed regioselectivity of nitration is explained by the DFT calculations. Three of these compounds with IC50 values (2.9-3.4 mmol) against Brugia malayi thymidylate kinase may be good antifilarial agents as also evidenced by molecular docking studies.

机译：通过在水中定量使用乙酸盐和银硝酸银，开发了合成3-羧基4-喹诺酮网的3-碳乳酮衍生物的合成中的高效，成本效益和绿色的方法。观察到的硝化区域被DFT计算解释。这些化合物中的三种与IC50值（2.9-3.4mmol）对抗Brugia Malayi胸酰酸酯激酶可以是良好的防污剂，也可以通过分子对接研究所证明的。

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来源
《RSC Advances》 |2015年第100期|共7页
作者
Azad Chandra S.; Balaramnavar Vishal M.; Khan Imran A.; Doharey Pawan K.; Saxena Jitendra K.; Saxena Anil K.;
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CSIR Cent Drug Res Inst Div Med &

Proc Chem Lucknow 226031 Uttar Pradesh India;

Global Inst Pharmaceut Educ &

Res Kashipur 244713 Uttrakhand India;

CSIR Cent Drug Res Inst Div Med &

Proc Chem Lucknow 226031 Uttar Pradesh India;

CSIR Cent Drug Res Inst Div Biochem Lucknow 226031 Uttar Pradesh India;

CSIR Cent Drug Res Inst Div Biochem Lucknow 226031 Uttar Pradesh India;

CSIR Cent Drug Res Inst Div Med &

Proc Chem Lucknow 226031 Uttar Pradesh India;

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正文语种 eng
中图分类化学;
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1. Operative conversions of 3-carboxy-4-quinolones into 3-nitro-4-quinolones via ipso-nitration: potential antifilarial agents as inhibitors of Brugia malayi thymidylate kinase [J] . Azad Chandra S., Balaramnavar Vishal M., Khan Imran A., RSC Advances . 2015,第100期

机译：通过IPSO - 硝化剂将3-羧基-4-喹诺酮酮的手术转换成3硝基-4-喹啉酮：潜在的防污剂，作为Brugia Malayi胸苷酸氨酯激酶的抑制剂
2. An operational transformation of 3-carboxy-4-quinolones into 3-nitro-4-quinolones via ipso-nitration using polysaccharide supported copper nanoparticles: synthesis of 3-tetrazolyl bioisosteres of 3-carboxy-4-quinolones as antibacterial agents [J] . Chandra S. Azad, Anudeep K. Narula RSC Advances . 2016,第23期

机译：使用多糖负载的铜纳米粒子通过IPSO硝化将3-羧基-4-喹诺酮酮的操作转化为3-硝基-4-喹诺酮类：3-羧基-4-喹诺酮网的3-四唑克基生物蛋白剂作为抗菌剂的合成
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Operative conversions of 3-carboxy-4-quinolones into 3-nitro-4-quinolones via ipso-nitration: potential antifilarial agents as inhibitors of Brugia malayi thymidylate kinase

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