56353-00-5Relevant articles and documents
Synthesis of Pyridine Clubbed 2,5-Disubstituted-1,3,4-Oxadiazole Derivatives Shows Potent Antimicrobial Activity
Katiyar, Pratima,Singh, Manjul Pratap
, p. 822 - 829 (2022/03/01)
In the present study, a series of 2,5-disubstituted-1,3,4 oxadiazole analogues retaining pyridine moiety were synthesized (4a-j) by reacting various substituted aromatic acids and isonicotinohydrazide by using POCl3 as a cycling agent. The structure elucidation of all the synthesized compounds was done by chromatographic data and spectral data analysis. The synthesized compounds were evaluated for their in-vitro antimicrobial activity against various strains of ESKAPE pathogens. Antibacterial activity was performed against Bacillus subtilis, Escherichia coli, Staphylococcus aureus and Pseudomonas aeruginosa, while antifungal activity was assayed against Candida albicans and Aspergillus spp. The result of in-vitro antimicrobial studies of all the synthesized compounds revealed that compound 4d and 4f exhibited promising activity against selected microbial strains equally compared to Cefixime and Econazole used as reference drugs.
Facile synthesis of 1,3,4-oxadiazoles via iodine promoted oxidative annulation of methyl-azaheteroarenes and hydrazides
Shang, Zhi-Hao,Sun, Ji-Na,Guo, Jiang-Shan,Sun, Yuan-Yuan,Weng, Wei-Zhao,Zhang, Zhen-Xiao,Li, Zeng-Jing,Zhu, Yan-Ping
, (2020/01/08)
An oxidative sp3 C–H bond of methyl-azaheteroarenes protocol was reported for the synthesis of 1,3,4-oxadiazoles via [4 + 1] annulation with hydrazides. This protocol enables 1,3,4-oxadiazole and quinoline linked diheterocycles via selective oxidation of sp3 C–H bond of methyl-azaheteroarenes in the presence of I2-DMSO. The reaction has a broad substrate scope and good functional group tolerance for methyl-azaheteroarenes and hydrazides.
Iodine-promoted one-pot synthesis of 1,3,4-oxadiazole scaffolds: Via sp3 C-H functionalization of azaarenes
Mani, Geeta Sai,Donthiboina, Kavitha,Shankaraiah, Nagula,Kamal, Ahmed
, p. 15999 - 16006 (2019/10/28)
An efficient iodine-mediated one-pot synthetic protocol for the synthesis of 2,5-disubstituted 1,3,4-oxadiazole scaffolds has been developed via sp3 C-H functionalization. Gratifyingly, this method involves oxidative amination with concomitant base-mediated cyclization of methylhetarenes and acylhydrazines by employing iodine and Cs2CO3. The key features of the present method include good functional group tolerance, a clean protocol, metal-free conditions and high yields, making this protocol an attractive strategy towards the synthesis of bioactive molecules and their key building blocks.