Synthesis, antitumor and antimicrobial activity of novel 1-substituted phenyl-3-[3-alkylamino(methyl)-2-thioxo-1,3,4-oxadiazol-5-yl] β-carboline derivatives

Journal of the Brazilian Chemical Society

Duarte, Marta C. T.¹  Foglio, Mary Ann¹  Dias Filho, Benedito P.¹  Universidade Estadual de Campinas, Campinas, Brazil¹  Universidade Estadual de Maringá, Maringá, Brazil¹  Formagio, Anelise S. N.¹  Barbosa, Valéria A.¹  Carvalho, João E. de¹  Sarragiotto, Maria Helena¹  Savariz, Franciele C.¹ 

关键词: 1;    3-disubstituted β-carboline derivatives;    1;    3;    4-oxadiazole;    Mannich bases;    antitumor activity;    antimicrobial activity;   

DOI  :  10.1590/S0103-50532010000200014

学科分类：化学（综合）

来源: SciELO

【 摘 要 】

With the purpose of activity enhancement of 1-substituted phenyl-3-(2-thioxo-1,3,4-oxadiazol-5-yl) β-carbolines 1a-c, reported as potential antitumor agents in our previous study, herein we report the synthesis and antitumor activity evaluation of several novel Mannich bases 2-7(a-c), by the introduction of different alkylamino(methyl) groups in the 1,3,4-oxadiazole unity of 1a-c. The antimicrobial activities of 1a-c and of 2-7(a-c) were also evaluated. Additionally, an in silico study of the ADME properties of novel synthesized β-carboline derivatives 2-7(a-c) was performed by evaluation of their Lipinski's parameters and topological polar surface area (TPSA) and percentage of absorption (% ABS) data.

【 授权许可】

Unknown