Synthesis and Antimicrobial Activity of Tricyclic Quinazolinethiones

被引:6
作者
Nasrullaev, A. O. [1 ]
Islamova, Zh. I. [1 ]
Elmuradov, B. Zh. [1 ]
Bektemirov, A. M. [2 ]
Osipova, S. O. [1 ]
Khushbaktova, Z. A. [1 ]
Syrov, V. N. [1 ]
Shakhidoyatov, Kh. M. [1 ]
机构
[1] Acad Sci Uzbek, S Yu Yunusov Inst Chem Plant Subst, Tashkent, Uzbekistan
[2] Minist Publ Hlth Republ Uzbekistan, Res Inst Epidemiol Microbiol & Infect Dis, Tashkent, Uzbekistan
关键词
Deoxyvasicine thione; mackinazoline thione; condensation with aldehydes; Vilsmeier-Haack reagent; nucleophilic substitution; 6-hydroxy-; -hydroseleno-; -chloro-; -anilinomethylidene derivatives; antimicrobial activity;
D O I
10.1007/s11094-017-1614-3
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Deoxyvasicine thione (III) and mackinazoline thione (6,7,8,9-tetrahydro-11H-pyrido[2,1-b]quinazoline-11-thione, IV) were synthesized and condensed with aromatic and heterocyclic aldehydes at the alpha-methylene [CH2-3 (III) or CH2-6 (IV)]. Either 3- and 6-arylidene derivatives (V - XIII) or 6-hydroxymethylaryl derivatives (XIV) were formed depending on the reaction conditions. Formylation of IV synthesized the 6-hydroxymethylidene derivative (XV). 6-Chloro-, -hydroseleno-, and -anilinomethylidenemackinazoline thiones (XVI - XIX) were also synthesized. The antimicrobial activity of the synthesized compounds against S. aureus, E. coli, Bacillus cereus, Candida albicans, and Pseudomonas aeruginosa was studied.
引用
收藏
页码:355 / 360
页数:6
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