18794-94-0Relevant academic research and scientific papers
Type II diabetes-related enzyme inhibition and molecular modeling study of a novel series of pyrazolone derivatives
Shetty, Shobhitha,Kalluraya, Balakrishna,Nithinchandra,Peethambar,Telkar, Sandeep B.
, p. 2834 - 2846 (2014/05/06)
Inhibitors of alpha-Amylase are targets for the development of novel drugs for the treatment of diabetes and obesity. Alpha amylase is an enzyme which increases the bio availability of glucose in the blood. Hence, the inhibition effects of alpha amylase of 2-[1-(4-isobutylphenyl)ethyl]-5-methyl-4-[2-(aryl- substituted)hydrazinylidene]-2,4-dihydro-3H-pyrazol-3-one (4a-l) were investigated, among them compounds 4d, 4f, 4a, and 4g have displayed good inhibitory activity. The compounds with significant results were further evaluated for their molecular modeling study using in silico method. The new series of compounds were synthesized by solvent-free microwave irradiation method and were characterized by spectral and analytical data.
Synthesis of 4-(2-phenylhydrazono)-1-(4-phenylthiazol-2-yl)-1H-pyrazol- 5(4H)-one compounds and characterization of their affinities to anti-apoptotic Bcl-2 family proteins
Shi, Shicheng,Han, Li,Zhou, Mi,Li, Yangfeng,Liu, Zhen,Yu, Biao,Wang, Renxiao
supporting information, p. 1133 - 1138 (2013/10/21)
Organic compounds containing the thiazol-2-yl-1H-pyrazol-5(4H)-one moiety are known to be associated with versatile pharmacological applications. In this study, we describe the methods for preparing 4-(2-phenylhydrazono)-1-(4- phenylthiazol-2-yl)-1H-pyrazol-5(4H)-one compounds. A set of 26 compounds were synthesized with overall yields ranging between 37% -92%. They were tested in a fluorescence polarization-based binding assay against three anti-apoptotic Bcl-2 family proteins, including Bcl-xL, Bcl-2, and Mcl-1. Our results indicate that this class of compounds are not effective inhibitors of these anti-apoptotic Bcl-2 family proteins. Their apoptosis-inducing effects are possibly due to BAX activation as suggested by Gavathiotis et al. in their recent study. However, other possibilities should not be ignored. In addition, a crystal structure obtained by us reveals that the exocyclic double bond in the molecular structure of this class of compounds is in the (Z)-configuration This class of compounds are not effective binders of anti-apoptotic Bcl-2 family proteins. Their apoptosis-inducing effects are possibly due to BAX activation rather than Bcl-2 inhibition as suggested by a recent study. Copyright
Synthesis, characterization and antibacterial screening of new pyrazole and pyrazoline-5-one derivatives
Nagaraju,Srinivasulu,Doraswamy,Venkata Ramana
experimental part, p. 293 - 298 (2012/03/11)
A series of N′-(p-toluene sulphonyl)-3-methyl-4-(substituted arylhydrazono)-2-pyrazoline-5-ones and N′-(2-hydroxybenzoyl)-3,5-dimethyl- 4-(substituted arylazo)pyrazoles have been synthesized and characterized by chemical analysis, IR and 1H NMR spectral data. The compounds have been screened for antibacterial activity against Staphylococcus aureus and Escherichia coli.
Synthesis of N′-(2-hydroxybenzoyl)-3-methyl-4-(substituted-phenylhydrazono)-2- pyrazolin-5-ones
Venkata Ramana,Ravindranath
, p. 112 - 113 (2007/10/03)
N′-(2-Hydroxybenzoyl)-3-methyl-4-(substituted-phenylhydrazono)-2- pyrazolin-5-ones have been synthesised by the reaction of 2-(substituted-phenylhydrazono)-ethyl-2,3-dioxobutyrate with salicylic acid hydrazine.
