Synthesis, characterization and effect of bis-1,3,4-oxadiazole rings containing glycine moiety on the activity of some transferase enzymes

Abstract

We described herein the synthesis of bis-1,3,4-oxadiazole containing glycine moiety. N-{5-[5-(4-Methoxyphenyl)-1,3,4-oxadiazole-2-yl-sulfanyl]-1,3,4-oxadiazole-2-yl-methyl}-4-methoxybenzamide was fully characterized by elemental analysis, FT-IR and 1 H NMR spectroscopy. Also this study was designed to show the effects of bis-oxadiazole compound on the activities of some transferase enzymes such as: GOT, GPT and c-GT in sera. This compound demonstrated activation on GOT and GPT activities, inhibitory effects on the c-GT activity. These effects increased with increasing the concentration of the compound. The causes of the increases and decreases in the enzymes activities are discussed.

Synthesis, in silico studies and cytotoxicity evaluation of novel 1,3,4-oxadiazole derivatives designed as potential mPGES-1 inhibitors

“…Spectroscopic data also supported that 1,3,4-oxadiazole derivatives may exist in thione form rather than thiole form [52]. The N-H proton of compound 3 was detected at 14.69 ppm in accordance with literature [53] while the S-H proton was reported at 1.6-2.0 ppm [54]. The most important proof of the formation of ketone structure, the C=O stretching bands of compounds 3a-f which were detected at 1685-1658 cm -1 .…”

Synthetic Approaches and Pharmacological Activity of 1,3,4-Oxadiazoles: A Review of the Literature from 2000–2012

“…Tomi and co-workers [ 124 ] reported a study with the bis-1,3,4-oxadiazole compound 176 that contains a glycine unit on the transferase activity of enzymes such as: GOT, GPT and γ-GT in serum. Compound 176 showed activation for GOT and GPT and inhibitory effects on the activity of γ-GT, ( Figure 15 ).…”

Synthesis and Antimicrobial Studies of New [Tetrakis (1, 2, 4-Triazole / 1, 3, 4-Oxadiazole / 1, 3, 4-Thiadiazole] [Bis-(Benzene-1, 3, 5-Triyl)] Dioxymethylene Compounds

“…Moreover, some new derivatives of 5-phenyl-1,3,4-oxadiazole were yielded by reaction of an acid hydrazine and different benzoic acid derivatives in the presence of phosphorous oxychloride [20]. Furthermore, by ring closure mechanism, bis-1,3,4-oxadiazole compounds were prepared from an acid hydrazide which was resulted from the reaction of an aromatic ester and hydrazine hydrate [21]. Recently, 4-amino-5-(3,5-dimethoxyphenyl)-4H- [1,2,4]triazole-3-thiol compound was prepared from the reaction 3,5-dimethoxy benzoic acid and thiocarbohydrazide in presence of sodium bicarbonate [22].…”