Abacavir prodrugs: microwave-assisted synthesis and their evaluation of anti-HIV activities.

Sriram D; Yogeeswari P; Myneedu NS; Saraswat V

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Abacavir prodrugs: microwave-assisted synthesis and their evaluation of anti-HIV activities.

机译：阿巴卡韦前药：微波辅助合成及其抗HIV活性的评估。

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The synthesis of a new series of abacavir prodrugs involving N2-substitution with various substituted benzaldehyde and ketone derivatives is described. The in vitro anti-HIV activities indicated that compound (3-(2-(4-methylaminobenzylideneamino)-6-(cyclopropylamino)-9H-purin-9-yl)c yclopentyl)methanol (3) was found to be most potent compound with EC50 of 0.05 microM and CC50 of >100 microM with selectivity index of >2000. Compound 3 was found to be 32 times more potent than the parent drug (EC50 of 1.6 microM). At pH 7.4, 37 degrees C, the hydrolytic t1/2 ranged between 120 and 240 min.

机译：描述了涉及各种取代苯甲醛和酮衍生物的N2-取代的一系列新的阿巴卡韦前药的合成。体外抗HIV活性表明，发现化合物（3-（2-（4-（甲基甲氨基苄叉基氨基）-6-（环丙基氨基）-9H-嘌呤-9-基）环戊基）甲醇（3）是最有效的化合物EC50为0.05 microM，CC50> 100 microM，选择性指数> 2000。发现化合物3的效力是母体药物的32倍（EC50为1.6 microM）。在pH 7.4（37摄氏度）下，水解t1 / 2介于120和240分钟之间。

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《Bioorganic and Medicinal Chemistry Letters》 |2006年第8期|共3页
作者
Sriram D; Yogeeswari P; Myneedu NS; Saraswat V;
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原文格式 PDF
正文语种 eng
中图分类药学;生物化学;
关键词
Anti-HIV Agents; Dideoxynucleosides; Microwaves; Prodrugs; 抗HIV药; 双去氧核苷类; 微波; 药物前体;

机译：Anti-HIV Agents;Dideoxynucleosides;Microwaves;Prodrugs;抗HIV药;双去氧核苷类;微波;药物前体;

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1. Abacavir prodrugs: microwave-assisted synthesis and their evaluation of anti-HIV activities. [J] . Sriram D, Yogeeswari P, Myneedu NS, Bioorganic and Medicinal Chemistry Letters . 2006,第8期

机译：阿巴卡韦前药：微波辅助合成及其抗HIV活性的评估。
2. A novel and efficient one-pot synthesis of symmetrical diamide (bis-amidate) prodrugs of acyclic nucleoside phosphonates and evaluation of their biological activities. [J] . Jansa P, Baszczynski O, Dracinsky M, European Journal of Medicinal Chemistry: Chimie Therapeutique . 2011,第9期

机译：一种新型高效的一锅法合成无环核苷膦酸酯的对称二酰胺（双酰胺）前体药物及其生物学活性。
3. Synthesis and biological evaluation of phosphoramidate prodrugs of two analogues of 2-deoxy-D-ribose-1-phosphate directed to the discovery of two carbasugars as new potential anti-HIV leads [J] . Hamon Nadege, Slusarczyk Magdalena, Serpi Michaela, Bioorganic and medicinal chemistry . 2015,第4期

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4. The Synthesis and Biological Evaluation of Prodrug Amide Derivatives Based on Phenylene Dioxy Di Acetic Acid [C] . Jalal Hassan Mohammed, Saadon Abdulla Aowda International Conference on Materials Engineering and Science . 2020

机译：基于亚苯基二氧化亚乙酸的前药酰胺衍生物的合成与生物学评价
5. Synthesis of potential anti-HIV agents and prodrugs: Part I synthesis of L-3'-hydroxymethylnucleosides. Part II synthesis and pharmacokinetics of 3'-azido-2',3'-dideoxyuridine (AZDU) as prodrugs . [D] . Cooperwood, John Steven. 1999

机译：潜在的抗HIV药物和前药的合成：第I部分L-3'-羟甲基核苷的合成。第二部分3'-叠氮基2'，3'-二脱氧尿苷（AZDU）作为前药的合成和药代动力学。
6. Synthesis and biological evaluation of phosphoramidate prodrugs of two analogues of 2-deoxy-d-ribose-1-phosphate directed to the discovery of two carbasugars as new potential anti-HIV leads [O] . Nadège Hamon, Magdalena Slusarczyk, Michaela Serpi, -1

机译：2-脱氧-d-核糖-1-磷酸的两个类似物的氨基磷酸酯前药的合成和生物学评估其目的是发现两个石竹作为新的潜在抗HIV药物
7. Bis-14-membered ring diketal diamines: Synthesis and evaluation of their anti-HIV and anti-tumoral activities. [O] . Affani, Radouane, Pélissier, Franck, Aubertin, Anne-Marie, 2009

机译：双14元环二缩酮二胺：合成和评估其抗HIV和抗肿瘤活性。

Abacavir prodrugs: microwave-assisted synthesis and their evaluation of anti-HIV activities.

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