Synthesis, antiarrhythmic and anticoagulant activities of novel thiazolo derivatives from methyl 2-(thiazol-2-ylcarbamoyl)acetate

被引：56

作者：

Amr, Abd El-Galil E. ^{[1
]}

Sabrry, Nermien M. ^{[1
]}

Abdalla, Mohamed M. ^{[2
]}

Abdel-Wahab, Bakr F. ^{[1
]}

机构：

[1] Natl Res Ctr, Appl Organ Chem Dept, Cairo, Egypt

[2] Hicare Pharmaceut Co, Res Units, Cairo, Egypt

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2009年 / 44卷 / 02期

关键词：

Thiazoles; Thiadiazoles; Bis-imides; Antiarrhythmic; Anticoagulant activities; ANTIMICROBIAL AGENTS; PYRIDINE; 2-AMINOTHIAZOLE; ANTICONVULSANT; INHIBITOR; ANTITUMOR; PLASMA; RATS;

D O I：

10.1016/j.ejmech.2008.05.004

中图分类号：

R914 [药物化学];

学科分类号：

100705 [微生物与生化药学];

摘要：

A series of novel thiazolo derivatives 2-17 were synthesized by initial condensation of methyl 2-(thiazol-2-ylcarbamoyl)acetate 1 with phenyl isothiocyanate and further reactions using different organic reagents. The structures of newly synthesized compounds were confirmed by IR, H-1 NMR, EIMS spectral data and elemental analysis. Initially the acute toxicity of the compounds was assayed via the determination of their LD50. All the compounds were screened for their antiarrhythmic and anticoagulant activities and they showed high antiarrhythmic activity compared with procaine amide and lidocaine as positive controls. The detailed synthesis, spectroscopic data, LD50 and pharmacological activities of the synthesized compounds were reported. (c) 2008 Published by Elsevier Masson SAS.

引用

页码：725 / 735

页数：11

共 37 条

[1]

Synthesis and investigation of a new cyclo (Nα-dipicolinoyl) pentapeptide of a breast and CNS cytotoxic activity and an ionophoric specificity [J].