Synthesis and Biological Activity of Some New 1,3,4-Thiadiazole and 1,2,4-Triazole Compounds Containing a Phenylalanine Moiety

Molecules

Mihaela Moise³  Valeriu Sunel³  Lenuta Profire¹  Marcel Popa²  Jacques Desbrieres⁴ 

[1] Department of Pharmaceutical Chemistry, Faculty of Pharmacy, “Gr. T. Popa” Medicine and Pharmacy University, 16 Universitatii Street, 700115, Romania;Department of Natural and Synthetic Polymers, Faculty of Chemical Engineering and Environmental Protection, “Gh. Asachi” Technical University, 71A B-dul Mangeron, Iasi, 700050, Romania; E-mail:;Department of Organic Chemistry and Biochemistry, Faculty of Chemistry, “Al. I. Cuza” University, Iasi, 11 B-dul Carol I, 700506, Romania; E-mails:;Pau et Pays de l’Adour University, Institut Pluridisciplinaire de Recherche sur l’Environnement et les Matériaux – Equipe de Physique et Chimie des Polymèrs (IPREM/EPCP), UMR 5254 CNRS, Hélioparc Pau Pyrénées 2, av. President Angot, 64053 Pau Cedex 09, France; E-mail:

关键词: phenylalanine;    thiosemicarbazide;    1;    3;    4-thiadiazole;    1;    2;    4-triazole;    anti-inflammatory activity;   

DOI  :  10.3390/molecules14072621

来源: mdpi

【 摘 要 】

New 1,3,4-thiadiazole, 6, 7 and 1,2,4-triazole derivatives, 8, 9 containing a phenylalanine moiety have been synthesized by intramolecular cyclization of 1,4-disubstituted thiosemicarbazides, 4, 5, in acid and alkaline media, respectively; the thiosemicarbazides were obtained by reaction of hydrazide 3 with appropriate aromatic isothiocyanates. The toxicity of the synthesized compounds was evaluated and the anti-inflammatory study of the triazole compound 9 established an appreciable anti-inflammatory activity that is comparable with that of other nonsteroidal anti-inflammatory agents.

【 授权许可】

CC BY   
© 2009 by the authors; licensee Molecular Diversity Preservation International, Basel, Switzerland.