54970-80-8Relevant academic research and scientific papers
Design, synthesis, analgesic, anti-inflammatory activity of novel pyrazolones possessing aminosulfonyl pharmacophore as inhibitors of COX-2/5-LOX enzymes: Histopathological and docking studies
Abdelgawad, Mohamed A.,Labib, Madlen B.,Ali, Waleed A.M.,Kamel, Gehan,Azouz, Amany A.,EL-Nahass, EL-Shaymaa
, p. 103 - 114 (2018/03/21)
A series of newly synthesized 4-aryl-hydrazonopyrazolones were designed and their structures were confirmed by spectral and elemental analyses. All synthesized compounds were evaluated for their in vitro COXs, 5-LOX inhibition, in vivo analgesic and anti-
Synthesis, characterisation and biological screening of some 2-substituted benzimidazole derivatives as potential anticancer agents
Shaaban, Mohammed Abed-Elrahman,Kamal, Aliaa Mohammed,Teba, Heba El-Sayed
, p. 228 - 234 (2016/05/11)
Twenty two new polycyclic compounds containing a 2-substituted benzimidazole core were synthesised, characterised and evaluated in vitro against the three most widespread cancers. Seven compounds showed outstanding antitumor activity towards breast, lung
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 and antimicrobial activity of pyrazolinones and pyrazoles having benzothiazole moiety
Amir, Mohd.,Javed, Sadique A.,Hassan, Mohd. Zaheen
experimental part, p. 1261 - 1270 (2012/07/31)
A new class of 4-arylhydrazono-1-benzothiazolyl-3-methylpyrazolin-5-ones (3a-j) and 4-arylazo-1-benzothiazolyl-3,5-dimethylpyrazoles (4a-j) were designed as pharmacophore hybrids between pyrazolinone/pyrazole and benzothiazole moiety. The target molecules were efficiently synthesized by the cyclization of various oxobutyrates/pentane-2,4-dione derivatives with 6-chloro-2- hydrazinobenzothiazole in the presence of glacial acetic acid. The compounds were evaluated for their in vitro antimicrobial activity. Preliminary study of the structure-activity relationship revealed that electron-withdrawing groups in phenyl ring had a promising effect on the antimicrobial activity. Also, correlation study has been used to establish the relationships between the antibacterial activity and physicochemical parameter clogP. Springer Science+Business Media, LLC 2011.
