1081819-52-4Relevant articles and documents
Synthesis and pharmacological evaluation of pyridinyl-1,3,4-oxadiazolyl-ethanone derivatives as antimicrobial, antifungal and antitubercular agents
Mansoori, Mohammad Hashim,Khatik, Gopal L.,Mishra, Vijay
, p. 744 - 755 (2017/10/30)
Abstract: Nicotinic acid was converted into different substituted acetylated nicotinic acid derivatives by sequential transformation involving formation of hydrazide, Schiff’s base and finally acylated oxadiazole derivatives. The synthesized compounds were characterized by spectroscopic techniques and evaluated in vitro for the antimicrobial, antifungal, as well as antitubercular activity. Among all the synthesized derivatives, compounds 6b, 6d, 6e, 6g, and 6j demonstrated excellent antimicrobial activity on Bacillus subtilis. The compounds 6d, 6j and compounds 6b, 6f, 6h, and 6i exhibited maximum zone of inhibition against fungi Candida albicans as well as Aspergillus niger, respectively at the concentration of 500 μg/mL. The antitubercular activity exhibited by 6f, 6g, and 6d with minimum inhibitory concentration (MIC) values of 1.2, 3.1, and 7.8 μg/mL, respectively. The synthesized compounds were studied by molecular docking through Autodock Vina to evaluate their interaction at respective proteins. Further the effect of synthesized derivatives on surface morphology of human erythrocytes as well as hemolysis was also evaluated. The results demonstrated lesser extent of hemolytic toxicity.
An efficient alkynylation of 4-thiazolidinone with terminal alkyne under C-H functionalisation
Shaikh, Mohammed Umar M.,Mudaliar, Sulochana S.,Chikhalia, Kishor H.
, p. 50780 - 50785 (2016/06/09)
A method of palladium catalysed efficient alkynylation through the cross coupling reaction of terminal alkynes with the slightly more acidic C-H bonds of 4-thiazolidinone has been developed. This method allows the direct introduction of an ethynyl group into the 4-thiazolidinone moiety. Mild reaction conditions involving aerial oxidation and one pot synthesis make this reaction more efficient for the formation of sp3(C)-sp(C) bond.
Metal-Free Synthesis of 1,3,4-Oxadiazoles from N′-(Arylmethyl)hydrazides or 1-(Arylmethyl)-2-(arylmethylene)hydrazines
Shang, Zhenhua,Chu, Qianqian,Tan, Sheng
, p. 1032 - 1040 (2015/03/30)
An efficient and versatile metal-free synthesis of 1,3,4-oxadiazoles from N′-(arylmethyl)hydrazides or 1-(arylmethyl)-2-(arylmethylene)hydrazines through oxidative dehydrogenation is reported. A range of 2,5-disubstituted 1,3,4-oxadiazoles were prepared by treating N′-(arylmethyl)hydrazides with (diacetoxyiodo)benzene in acetonitrile or by treating 1-(arylmethyl)-2-(arylmethylene)hydrazines with [bis(trifluoroacetoxy)iodo]benzene in methyl tert-butyl ether. Aldehyde N-acylhydrazones and aldazines were initially generated in situ as intermediates.
