Paper Information

Journal:   JOURNAL OF THE IRANIAN CHEMICAL SOCIETY(JICS)   APRIL 2014 , Volume 11 , Number 2; Page(s) 369 To 378.
 
Paper: 

SYNTHESIS, IN VITRO LIPOXYGENASE INHIBITION, DOCKING STUDY AND THERMAL STABILITY ANALYSES OF NOVEL INDOLE DERIVATIVES

 
 
Author(s):  YAR MUHAMMAD*, SIDRA LALA RUKH, PONTIKI ELENI, MUSHTAQ NAFEESA, ASHRAF MUHAMMAD, NASAR RUMANA, KHAN ISLAM ULLAH, MAHMOOD NASIR, NAQVI SYED ALI RAZA, KHAN ZULFIQAR ALI, SHAHZAD SOHAIL ANJUM
 
* INTERDISCIPLINARY RESEARCH CENTER IN BIOMEDICAL MATERIALS, COMSATS INSTITUTE OF INFORMATION TECHNOLOGY, LAHORE, 54000, PAKISTAN
 
Abstract: 

A series of indole derivatives has been synthesized and biologically evaluated to identify potent new lipoxygenase (LOX) inhibitors. All selected indole derivatives were screened for their LOX inhibition studies. Most of compounds showed good in vitro LOX inhibition properties exhibiting IC50 values in the range of 53.61±0.14 to 198.61±0.11 mM (mean±SEM), as compared to the standard inhibitor baicalein with IC50 value 22.4±1.3 mM. Structure activity relationship has been discussed and docking stimulation of most active compound 4f has also performed. Thermal stability and melting point of indole derivatives have been performed by thermal gravimetric analysis and differential scanning calorimetry analysis under nitrogen atmosphere at heating rate of 20 °C min-1. Compound 4f bearing bis-phenyl moiety has been found to be the most potent (IC50 53.61±0.14 mM) and thermally most stable among the tested compounds. Imine (C=N) was found to be the key moiety for increasing the thermal stabilities of indole derivatives. FT-IR, NMR and elemental analysis techniques were performed for structural characterization.

 
Keyword(s): DIFFERENTIAL SCANNING CALORIMETRY, THERMAL GRAVIMETRIC ANALYSIS, LIPOXYGENASE INHIBITOR, IMINE, INDOLE-3-ACETIC ACID
 
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