Synthesis and in vitro evaluation of antimycobacterial and cytotoxic activity of new α,β-unsaturated amide, oxazoline and oxazole derivatives from L-serine

被引：14

作者：

Aguirre-Renteria, Saul A. ^{[1
]}

Carrizales-Castillo, Juan J. J. ^{[1
]}

Camacho Corona, Maria del Rayo ^{[1
]}

Hernandez-Fernandez, Eugenio ^{[1
]}

Garza-Gonzalez, Elvira ^{[2
]}

Rivas-Galindo, Veronica M. ^{[3
]}

Arredondo-Espinoza, Eder ^{[1
]}

Avalos-Alanis, Francisco G. ^{[1
]}

机构：

[1] Univ Autonoma Nuevo Leon, Fac Ciencias Quim, Pedro de Alba S-N,Ciudad Univ, San Nicolas De Los Garza 66455, Nuevo Leon, Mexico

[2] Univ Autonoma Nuevo Leon, Serv Gastroenterol, Hosp Univ Dr Jose Eleuterio Gonzalez, Av Gonzalitos y Madero S-N, Monterrey 64460, Nuevo Leon, Mexico

[3] Univ Autonoma Nuevo Leon, Fac Med, Av Madero S-N, Monterrey 64460, Nuevo Leon, Mexico

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2020年 / 30卷 / 09期

关键词：

Acrylamides; Antitubercular activity; Cytotoxicity; Oxazolines; Oxazoles; TUBERCULOSIS; AGENTS;

D O I：

10.1016/j.bmcl.2020.127074

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The synthesis of 19 compounds derived from L-serine and analogs of p-substituted cinnamic acid is reported. Oxazolines 9 and oxazoles 10 have high antitubercular activity with Minimum Inhibitory Concentration (MIC) of 0.7812-25.0 mu g/mL (3.21-100.3 mu M), against two strains of Mycobacterium tuberculosis sensitive to first-line drugs Isoniazid (INH), Rifampicin (RIF), Ethambutol (EMB), Pyrazinamide (PZE) (H37Rv) and a clinical isolate resistant to INH, RIF and EMB (G122). The cytotoxic evaluation shows that oxazoles have low activity, finding viability > 96% against the VERO cell line. The results show these compounds could be considered as future alternatives for antitubercular treatment.

引用

页数：5

共 17 条

[1] Synthesis, antimycobacterial and cytotoxic activity of α,β-unsaturated amides and 2,4-disubstituted oxazoline derivatives [J].