Sixteen Schiff bases of quinazolin‐4‐one‐linked 1,3,4‐oxadiazoles were synthesized by reaction with different aromatic aldehydes. Purity of newly synthesized derivatives was confirmed through thin‐layer chromatography, combustion analysis, and melting point. The structure of the derivatives was confirmed by determining infrared spectroscopy, nuclear magnetic resonance, and mass spectroscopy. All the synthesized derivatives were evaluated for their analgesic and anti‐inflammatory activities in mice and rats, respectively. In animal studies, the derivative (E)‐3‐(5‐(4‐(4‐methoxybenzylideneamino)phenyl)‐1,3,4‐oxadiazol‐2‐yl)‐2‐phenylquinazolin‐4(3H)‐one showed more potent analgesic activity and the derivative (Z)‐3‐(5‐(2‐(2‐hydroxybenzylideneamino)phenyl)‐1,3,4‐oxadiazol‐2‐yl)‐2‐phenylquinazolin‐4(3H)‐one showed more potent anti‐inflammatory activity as compared with other derivatives. The results of the present study indicate that reactions of 3‐(5‐(4‐aminophenyl)‐1,3,4‐oxadiazol‐2‐yl)‐2‐phenylquinazolin‐4(3H)‐one and 3‐(5‐(2‐aminophenyl)‐1,3,4‐oxadiazol‐2‐yl)‐2‐phenylquinazolin‐4(3H)‐one with different aromatic aldehydes produce Schiff bases of quinazolin‐4‐one‐linked 1,3,4‐oxadiazoles with potent analgesic and anti‐inflammatory activities.
in Wiley Online Library (wileyonlinelibrary.com).Novel hybrid molecules were synthesized through the amalgamation of quinoxaline residue with 1,3,4oxadiazole molecule. The purity of obtained 1,3,4-oxadiazoles derivatives containing quinoxaline residue (total 11) was confirmed through thin-layer chromatography, combustion analysis, and melting point, whereas their structures were confirmed by infrared spectroscopy, nuclear magnetic resonance, and mass spectroscopy. In animal studies, the derivatives 4-(5-(4-(3-methylquinoxalin-2-yl)phenyl)-1,3,4-oxadiazol-2-yl)benzenamine and 2-(5-(4-(3-methylquinoxalin-2-yl)phenyl)-1,3,4-oxadiazol-2-yl)benzenamine showed excellent analgesic and anti-inflammatory activities, respectively, as compared with other derivatives. In order to rationalize the biological results of the derivatives, molecular docking studies were performed using Argus lab. The compounds exhibited good docking scores between À12.987 and À9.92 kcal/mol against cyclooxygenase-II (5IKQ) protein fragment.
Pyrazole is a five membered heterocyclic ring which is a versatile lead compound for designing potent bioactive agents. This interesting group of compound has diverse biological activities such as antimicrobial, antiinflammatory, analgesic, anticonvulsant, anticancer, antihelmintic, antioxidant, and herbicidal. Given data represents that pyrazole being heterocyclic planar five membered ring systems have various pharmacological actions. Results of various derivatives of different pyrazole and their substitutions are reviewed in present article. Various methods for synthesizing pyrazole are discussed with their pharmacological actions. These derivatives of pyrazole are analysed here for varying pharmacological activities.
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