Design, synthesis, antimicrobial activity and anti-HIV activity evaluation of novel hybrid quinazoline–triazine derivatives

Rahul P. Modh; Erik De Clercq; Christophe Pannecouque; Kishor H. Chikhalia

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Design, synthesis, antimicrobial activity and anti-HIV activity evaluation of novel hybrid quinazoline–triazine derivatives

机译：新型杂合喹唑啉-三嗪衍生物的设计，合成，抗菌活性和抗HIV活性评估

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A series of novel hybrid quinazoline–triazine derivatives was designed and synthesized from cyanuric chloride and anthranilic acid through sequential reactions, which contain different pharmacophores like quinazoline and substituted diaryl triazine (DATA) linked with ethylene diamine. All the newly synthesized compounds were characterized by infrared, 1H-NMR, 13C-NMR, MS and elemental analysis. Further, we evaluated the in vitro anti-HIV activity of the newly synthesized compounds against HIV-1 (III_B) and HIV-2 (ROD) viral strains and as well as in vitro antimicrobial activity against four bacteria (Staphylococcus aureus, Bacillus cereus, Pseudomonas aeruginosa, Klebsiella pneumoniae) and two fungi (Aspergillus clavatus, Candida albicans) using the paper agar streak dilution method. The bioassay results indicate that four compounds namely 7d, 7n, 7r and 7s could be considered as possible potential agents.

机译：通过顺序反应，从氰尿酰氯和邻氨基苯甲酸设计并合成了一系列新颖的喹唑啉-三嗪杂化衍生物，其中包含不同的药效团，如喹唑啉和与乙二胺连接的取代的二芳基三嗪（DATA）。通过红外光谱， 1 H-NMR， 13 C-NMR，MS和元素分析对所有新合成的化合物进行表征。此外，我们评估了新合成的化合物对HIV-1（III _{B ）和HIV-2（ROD）病毒株的体外抗HIV活性，以及对4种化合物的体外抗微生物活性。使用纸琼脂条纹稀释法测定细菌（金黄色葡萄球菌，蜡状芽孢杆菌，铜绿假单胞菌，肺炎克雷伯菌）和两种真菌（曲霉，白色念珠菌）。生物测定结果表明，可以将四种化合物即7d，7n，7r和7s视为可能的潜在药物。}

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《Journal of enzyme inhibition and medicinal chemistry.》 |2014年第1期|共9页
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Rahul P. Modh; Erik De Clercq; Christophe Pannecouque; Kishor H. Chikhalia;
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机译：新型杂合喹唑啉-三嗪衍生物的设计，合成，抗菌活性和抗HIV活性评价
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Design, synthesis, antimicrobial activity and anti-HIV activity evaluation of novel hybrid quinazoline–triazine derivatives

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