Synthesis and the biological activity of bis-mefenamidocalixarene

Authors

DOI:

https://doi.org/10.24959/175951

Keywords:

calixarenes, conjugates, diaminocalix[4]arene, bis-mefenamidocalixarene, mefenamic acid, non-steroidal anti-inflammatory drugs, anti-exudative activity

Abstract

Aim. To develop the method for the synthesis of the conjugate of diaminocalix[4]arene with 2-(2,3-dimethylphenyl)aminobenzoic acid (mefenamic acid) – bis-mefenamidocalixarene, determine its structure and physicochemical properties and assess its anti-exudative activity (AeA).
Results and discussion. The conjugate of diaminocalixarene with mefenamic acid – bis-mefenamidocalixarene was synthesized at one step by the reaction of reactants in equimolar amounts in the presence of 1-ethyl-3-(3-dimethylaminopropyl) carbodiimide. The structure of the compound obtained was determined by spectral methods. AeA of bis-mefenamidocalixarene was studied in rats using the model of formalin edema. The results of the experimental studies showed that bis-mefenamidocalixarene exhibited the anti-exudative activity, which was equal to the reference drug – sodium diclofenac.
Experimental part. The reaction of diaminocalixaren with 2- (2,3-dimethylphenyl)aminobenzoic acid (mefenamic acid) led to bis-mefenamidocalixarene with 40 % yield. The screening of AeA was carried out using modern digital plethysmometer (IITC Life Science (USA)).
Conclusions. The effective one-stage method for the synthesis of the conjugate of diaminocalix[4]arene with 2-(2,3-dimethylphenyl)aminobenzoic acid – bis-mefenamidocalixarene has been developed. Its structure has been proven, and AeA has been studied. AeA is equal to the reference drug. It has been found that bis-mefenamidokalixaren synthesized is a promising compound for further profound studies.

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Published

2019-08-20

How to Cite

(1)
Chalenko, N. M.; Rodik, R. V.; Syrova, G. O. Synthesis and the Biological Activity of Bis-Mefenamidocalixarene. J. Org. Pharm. Chem. 2019, 17, 21-25.

Issue

Vol. 17 No. 3(67) (2019)

Section

Original Researches

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