Recent Developments on Pharmacological Potential of 1,3,4-Oxadiazole Scaffold

Design, synthesis, in silico, and in vitro evaluation of benzylbenzimidazolone derivatives as potential drugs on α-glucosidase and glucokinase as pharmacological targets

“…13,27 Therefore, in silico evaluation play a critical role in identifying novel molecules that can control blood glucose levels, using molecular docking to show the interactions with biological relevance amino acids in the union site, which helps to predict the possible biological activity. 28 The molecular docking analysis suggests good affinity energy (values < −5 Kcal mol −1 ); these values could be explained in the amino acid residues interaction, where the evaluated compounds present hydrogen, electrostatic and hydrophobic bond with catalytic or biological important residues of the Fig. 2 Interaction of 2r in the active (a-glu) or allosteric site (gk) of therapeutic targets.…”

Synthesis of S-(5-aryl-1,3,4-oxadiazol-2-yl) O-alkyl carbonothioate and alkyl 2-((5-aryl-1,3,4-oxadiazol-2-yl)thio) acetate, and their antimicrobial properties

“…Oxadiazolthione (2) with one Cl at position 2 showed intermediate result (10-12 mm). It should be noted that the introduction of propyl and isobutyloxycarbonyl fragments into 5-(2,4dichlorophenyl)-1,3,4-oxadiazole-2-thione led to a loss of activity of the observed in unsubstituted oxadiazolthione (3). At the same time, these compounds exhibit minimal (6-8 mm) fungicidal activity against C. albicans.…”

“…A wide interest in the chemistry of derivatives of 5-substituted-1,3,4-oxadiazole-2-thiones is associated with a broad variety of biological and physiological activities exhibited by their derivatives. Recently, numerous works on synthesis and biological activities such as antibacterial, antifungal, antiviral, anticonvulsant, anti-inflammatory, antitumor of 5-substituted-1,3,4-oxadiazole-2-thione derivatives were reported (1)(2)(3)(4)(5)(6)(7)(8)(9)(10). A distinctive structural feature of 5-aryl-1,3,4-oxadiazol-2thiones is the presence of an ambident thioamide group NH-C=S in their molecule, therefore, depending on the nature of the attacking electrophilic agent, derivatives can be obtained at the exocyclic sulfur atom, and on the endocyclic nitrogen atom or simultaneously on both reaction centers (S-or N-).…”

Tuneable access to indole, indolone, and cinnoline derivatives from a common 1,4-diketone Michael acceptor

“…Introduction Nitrogen-containing heterocycles are widespread in plenty of molecules of interest, either in materials science, optics, electronics, or biology [1][2][3][4]. They are also very useful building blocks to create more sophisticated organic molecules.…”