4-Aminoquinoline derived antimalarials: synthesis, antiplasmodial activity and heme polymerization inhibition studies.

Solomon VR; Haq W; Smilkstein M; Srivastava K; Puri SK; Katti SB

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4-Aminoquinoline derived antimalarials: synthesis, antiplasmodial activity and heme polymerization inhibition studies.

机译：4-氨基喹啉衍生的抗疟药：合成，抗血浆活性和血红素聚合抑制研究。

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A new series of 4-aminoquinoline derivatives have been synthesized and found to be active against both susceptible and resistant strains of Plasmodium falciparum in vitro. Compound 1-[3-(7-chloro-quinolin-4-ylamino)-propyl]-3-cyclopropyl-thiourea (7) exhibited superior in vitro activity against resistant strains of P. falciparum as compared to chloroquine (CQ). All the compounds showed resistance factor between 0.59 and 4.31 as against 5.05 for CQ. Spectroscopic studies suggested that this class of compounds act on heme polymerization target.

机译：已经合成了一种新的4-氨基喹啉衍生物，发现在体外反对敏感和抗性疟原虫腐蚀性和抗性抗性菌株。化合物1- [3-（7-氯 - 喹啉-4-酰基氨基） - 丙基] -3-环丙基 - 硫脲（7）与氯喹（CQ）相比，对抗性P. falciparum的抗性株的体外活性优异。所有化合物显示出0.59和4.31的电阻因子，为CQ的5.05。光谱研究表明，这类化合物对血红素聚合靶标作用。

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《European Journal of Medicinal Chemistry: Chimie Therapeutique》 |2010年第11期|共7页
作者
Solomon VR; Haq W; Smilkstein M; Srivastava K; Puri SK; Katti SB;
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Medicinal and Process Chemistry Division Central Drug Research Institute MG Road Lucknow 226 001 India.;

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正文语种 eng
中图分类药学;
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1. 4-Aminoquinoline derived antimalarials: synthesis, antiplasmodial activity and heme polymerization inhibition studies. [J] . Solomon VR, Haq W, Smilkstein M, European Journal of Medicinal Chemistry: Chimie Therapeutique . 2010,第11期

机译：4-氨基喹啉衍生的抗疟药：合成，抗血浆活性和血红素聚合抑制研究。
2. 4-Aminoquinoline derived antimalarials: synthesis, antiplasmodial activity and heme polymerization inhibition studies. [J] . Solomon VR, Haq W, Smilkstein M, European Journal of Medicinal Chemistry: Chimie Therapeutique . 2010,第11期

机译：4-氨基喹啉衍生的抗疟药：合成，抗血浆活性和血红素聚合抑制研究。
3. 4-Aminoquinoline derived antimalarials: synthesis, antiplasmodial activity and heme polymerization inhibition studies. [J] . Solomon VR, Haq W, Smilkstein M, European Journal of Medicinal Chemistry: Chimie Therapeutique . 2010,第11期

机译：4-氨基喹啉衍生的抗疟药：合成，抗血浆活性和血红素聚合抑制研究。
4. Heme Polymerization Inhibition Activity (HPIA) Assay of Synthesized Xanthone Derivative as Antimalarial Compound [C] . Dhina Fitriastuti, Jumina, Priatmoko International Conference on Chemistry, Chemical Process and Engineering . 2017

机译：血红素聚合抑制活性（HPIA）衍生物作为抗体化合物的合成X原酮衍生物测定
5. Implications for the role of the peroxoferric intermediate in the second step of nitric oxide synthase derived from the reactivity of P450-CAM with camphor-5-oxime and characterization of the heme iron coordination structures of tyrosine- and histidine-ligated heme enzymes using magnetic circular dichroism spectroscopy [D] . Bandara, D.M. Indika 2010

机译：P450-CAM与樟脑5-肟的反应性衍生的一氧化氮合酶第二步中的过氧铁中间体的作用以及使用磁性圆环表征酪氨酸和组氨酸连接的血红素酶的血红素铁配位结构的特征二向色光谱
6. Relationship between Antimalarial Drug Activity Accumulation and Inhibition of Heme Polymerization in Plasmodium falciparum In Vitro [O] . Shaun R. Hawley, Patrick G. Bray, Mathirut Mungthin, 1998

机译：体外恶性疟原虫抗疟药活性积累和抑制血红素聚合的关系
7. Design, synthesis of 4-aminoquinoline-derived thiazolidines and their antimalarial activity and heme polymerization inhibition studies [O] . V. Raja Solomon, W. Haq, Kumkum Srivastava, 2012

机译：4-氨基喹啉衍生的噻唑烷的设计，合成及其抗疟活性和血红素聚合抑制研究

4-Aminoquinoline derived antimalarials: synthesis, antiplasmodial activity and heme polymerization inhibition studies.

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