An efficient synthesis and biological study of novel indolyl-1,3,4-oxadiazoles as potent anticancer agents

A facile procedure for the one-pot synthesis of unsymmetrical 2,5-disubstituted 1,3,4-oxadiazoles

Synthesis and antimycobacterial activity of 4-(5-substituted-1,3,4-oxadiazol-2-yl)pyridines

Microwave assisted one pot synthesis of some novel 2,5-disubstituted 1,3,4-oxadiazoles as antifungal agents.

1,3,4-oxadiazole, a privileged structure, endows its derivatives with broad and potent biological functions, especially in antiviral activities, including anti-HIV, anti-HCV, anti-HBV, anti-HSV activities, etc. Molecular modeling and pharmacokinetic studies have demonstrated that the introduction of 1,3,4-oxadiazole ring to the inhibitors can change their polarity, flexibility as well as metabolic stability, and 1,3,4-oxadiazole scaffold can also act as acceptors of hydrogen bonds formation, which make it possible to be used as a isosteric substituent for amide or ester groups. This review focuses on the recent advances in the synthesis of 1,3,4-oxadiazole ring and mainly the discovery, biological activities investigations and structural modifications of several distinct classes of 1,3,4-oxadiazoles as potent antiviral agents. In addition, the binding models of some representative 1,3,4-oxadiazoles were also discussed, which provide rational explanation for their interesting antiviral activities, and also pave the way for further optimization of 1,3,4- oxadiazole based antiviral agents.

1,3,4-Oxadiazole: A Privileged Structure in Antiviral Agents

Synthesis and spectral data of 4,5-bis[5-aryl-1,3,4-oxadiazol-2-yl]-1-benzyl-1,2,3-triazoles

Generation and dienophilic properties of 1-benzyl-1H-1,2,3-triazolo[4,5-d]pyridazine-4,7-dione

The synthesis of the title compounds 3 upon cyclodehydration with thionyl chloride of the corresponding bis-aroylhydrazides 2 is described and their spectral properties are examined.

Synthesis and Spectral Data of 4,5-Bis(5-aryl-1,3,4-oxadiazol-2-yl)-1- benzyl-1,2,3-triazoles.

1-Benzyl-5,6-dihydro-1H-1,2,3-triazolo[4,5-d]pyridazine-4,7-dione by oxidation with lead tetraacetate afforded the corresponding triazolopyridazine-4,7-dione dehydrogenated at position 5 and 6 as the intermediate, which was trapped with several dienes giving the hetero-Diels-Alder adducts corresponding in good yields. The structure of the cycloadduct was determined by X-ray analysis.

A. B. Theocharis

Papers

Synthesis and spectral data of 4,5-bis[5-aryl-1,3,4-oxadiazol-2-yl]-1-benzyl-1,2,3-triazoles

Generation and dienophilic properties of 1-benzyl-1H-1,2,3-triazolo[4,5-d]pyridazine-4,7-dione

Synthesis and Spectral Data of 4,5-Bis(5-aryl-1,3,4-oxadiazol-2-yl)-1- benzyl-1,2,3-triazoles.

Generation and Dienophilic Properties of 1‐Benzyl‐1H‐1,2,3‐triazolo(4, 5‐d)pyridazine‐4,7‐dione.