Synthesis, antiarrhythmic and anticoagulant activities of novel thiazolo derivatives from methyl 2-(thiazol-2-ylcarbamoyl)acetate.
A series of novel thiazolo derivatives were synthesized by initial condensation of methyl 2-(thiazol-2-ylcarbamoyl)acetate with phenyl isothiocyanate and further reactions using different organic reagents. The structures of newly synthesized compounds were confirmed by IR, 1H NMR, EIMS spectral data and elemental analysis. Initially the acute toxicity of the compounds was assayed via the determination of their LD(50). 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, LD(50) and pharmacological activities of the synthesized compounds were reported.
Amr
Abd El-Galil E
Ael-G
Applied Organic Chemistry Department, National Research Center, El-Tahrir Street, Dokki, Cairo, Egypt. aamr1963@yahoo.com
Sabrry
Nermien M
NM
Abdalla
Mohamed M
MM
Abdel-Wahab
Bakr F
BF
D000818:Animals; D000889:Anti-Arrhythmia Agents / Q000737:chemistry*; D000925:Anticoagulants / Q000737:chemistry*; D004353:Drug Evaluation, Preclinical; D064420:Drug-Related Side Effects and Adverse Reactions; D006801:Humans; D015394:Molecular Structure; D011817:Rabbits; D051381:Rats; D013057:Spectrum Analysis; D013844:Thiazoles / Q000138:chemical synthesis* / Q000494:pharmacology
D000889:Anti-Arrhythmia Agents; D000925:Anticoagulants; D013844:Thiazoles