Synthesis and anti-diabetic activity evaluation of new 1,2,3-triazole derivatives incorporating 2-pyrazoline ring

Abstract

In the present work, a new series of compounds containing 1,2,3-triazole and 2-pyrazoline moieties in the same matrix was synthesized via a multistep synthetic route. The synthesized compounds were characterized by FT-IR, 1HNMR and 13C NMR spectra. The target compounds and their precursors were screened in vitro for their α-amylases inhibitory activity. The preliminary activity results revealed that all the tested compounds displayed an inhibition activity ranged from moderate to high depending on their structures and concentrations compared to ascorbose as a standard drug.

Synthesis and Preliminary Anti-Inflammatory and Anti-Microbial Evaluation of New 4,5-Dihydro-1H-Pyrazole Derivatives

“…These heterocyclic molecules are widely distributed in nature and can be found as vitamins, alkaloids, pigments, and parts of the cells of both plants and animals (2,4) . Pyrazolines and their derivatives have been the focus of numerous activities, including : antimicrobial (10)(11)(12) , antiinflammatory (13)(14)(15)(16) , anti-cancer (17)(18)(19) , antibacterial (20)(21)(22) , antidiabetic (23,24) , Antioxidants (25,26 ) ,Anti-malarial (27), antivirals (28)(29)(30) .Based on the aforementioned biological and pharmacological profiles demonstrated by chalcone and pyrazoline, we designed our research which focuses on synthesis of different 3,5-di-phenyl-2pyrazolines linked to aniline and substituted aniline, and evaluate their anti-inflammatory, antibacterial and antifungal activities .…”

Synthesis and Molecular Docking Studies of New Pyrimidinone ring Containing 1,2,3-Triazole Derivatives

“…10,11 Thus, compounds contain 1,2,3-triazole ring system showing a broad range of pharmaceutical applications such as antioxidant, 12 anticancer, 13 antimicrobial, 14 antiviral, 15 antibacterial 16 and antidiabetic agents. 17,18 On the other hand, pyrimidine ring (1,3-diazine) is an aromatic six-membered heterocycle with two nitrogen atoms located at 1-and 3-positions and alloxan (5,5-dihydroxypyrimidine-2,4,6(1H,3H,5H)-trione) is the first pyrimidine derivative was isolated in 1818 via oxidizing of uric acid with nitric acid. 19 Characteristically, pyrimidine ring is a weak base (pKa 1.31) and has a high dipole moment that subtends π-π stacking interactions with dual hydrogen-bonding capacity that can be of importance in drug-target interactions and is normally stable towards ringopening reactions.…”