Synthesis, Evaluation and Pharmacological action of Oxadiazole derivatives

Abstract

Impacted numerous drug discovery programs including-muscarinic antagonists, benzodiazepine receptor partial agonists, Dopamine transporters, antirhinovirals, growth hormone secretagogues, 5-HT antagonists, antispasmodics. Heterocyclic compounds possess diverse biological properties that have led to intense study and research of these compounds. One of these compounds is Oxadiazole which has been found to exhibit various pharmacological activities. 1, 3, 4-oxadiazole having heterocyclic nucleus is a novel molecule which attract the chemist to search for a new therapeutic molecule. 1,3,4-oxadizole exhibited a wide range of biological activities which includes antibacterial, anti-tubercular, anticonvulsant, hypoglycemic, anti-allergic, enzyme inhibitor, vasodialatory, antifungal, cytotoxic, antiinflammatory, analgesic, hypolipidemic, anticancer, insecticidal, ulcerogenic activities etc. Out of the various derivative 2, 5-Disubstituted-1, 3, 4-oxadiazole is a widely exploited for various application. A large number of drugs used clinically have oxadiazole ring as a structural building block. The capacity of 1,3,4-oxadiazole nucleus to undergo variety of chemical reactions including electrophilic substitution, nucleophilic substitution, thermal and photochemical which make it medicinal backbone on which a number of potential molecules can be constructed. This review has basic information about 2, 5disubstituted-1, 3, 4-oxadiazole derivatives published in various journals for further development in the field. Oxadiazole derivatives are a class of heterocyclic compounds. The titled compounds were synthesized according to the procedures as given in the methodology. The reactions were monitored by TLC. The physical constants like melting point and solubility were determined for all the intermediates and final products. The compounds were further characterized by IR and 1H NMR and mass spectra. All the titled compounds were evaluated for their Anticonvulsant, Anti-inflammatory, Antibacterial, Antitubercular and Antioxidant activity.

Design, Synthesis, Characterization and Computational Studies of Mannich Bases Oxadiazole Derivatives as New Class of Jack Bean Urease Inhibitors

“…The bacterial ureases can also be inhibited by the five‐membered heterocycles like 1,2,4 triazoles and 1,3,4 oxadiazoles [30–35] . It is documented that some of the 1,3,4 oxadiazoles derived Mannich bases decrease inflammation and prevent fungal growth and they also possess analgesic, antiulcer, antibacterial, anti‐HIV, anti‐convulsant, anti‐tuberculosis and anticancer activities and as inhibitors of various other enzymes and are used in many other applications [36–39] . The broad therapeutic applications of oxadiazoles and Mannich bases have prompted us to synthesize Mannich bases of 1,3,4‐oxadiazole‐2‐thiones and evaluate their antiurease activity.…”

“…[30][31][32][33][34][35] It is documented that some of the 1,3,4 oxadiazoles derived Mannich bases decrease inflammation and prevent fungal growth and they also possess analgesic, antiulcer, antibacterial, anti-HIV, anti-convulsant, anti-tuberculosis and anticancer activities and as inhibitors of various other enzymes and are used in many other applications. [36][37][38][39] The broad therapeutic applications of oxadiazoles and Mannich bases have prompted us to synthesize Mannich bases of 1,3,4-oxadiazole-2-thiones and evaluate their antiurease activity. The data shows that Mannich bases of 1,3,4-oxadiazole-2-thiones are strong inhibitors of the urease enzyme and suggest further studies on more derivatives.…”