123154-60-9Relevant 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.
Sydnone derivatives. Part VII: Synthesis of some novel thiazoles and their pharmacological properties
Kalluraya, Balakrishna,Rahiman, M. Abdul,Banji, David
, p. 263 - 268 (2007/10/03)
The synthesis of some 4-(arylsydnonyl)-2- (4-arylhydrazono-3-methyl-5-oxo-2-pyrazolin-1-yl)-thiazoles by reacting 1-thiocarboxamido-3-methyl-4-(arylhydrazono)-2-pyrazolin-5-ones with different 4-bromoacetyl-3-arylsydnones is described. A few compounds from this series were screened for their anti-inflammatory, analgesic, and CNS depressant activities. Among the tested compounds 6s, 6d, 6n, and 6u showed significant anti-inflammatory activity comparable with that of standard drug Ibuprofen. Compounds containing chlorine and carboxylic substituents are more active. 6f, 6r, and 6u showed marked analgesic activity and most of the compounds tested showed promising CNS depressant activity comparable with that of standard drug pentobarbitone.
Synthesis, characterization and antimicrobial studies of some novel 3- arylazo-7-hydroxy-4-methylcoumarins
Sharma, Pratibha,Pritmani, Shreeya
, p. 1139 - 1142 (2007/10/03)
A series of 3-arylazo-7-hydroxy-4-methylcoumarins have been synthesized in excellent yields (80-90%) and their structures established on the basis of IR, 1H NMR, mass spectral data and elemental analyses. Their purity has been ascertained by ch
High-Resolution 1H and 13C NMR Spectroscopy of Some Hydrazo Compounds
Al-Rawi, J. M. A.,Khayat, M. A. R.
, p. 112 - 116 (2007/10/02)
o-Benzenediazonium carboxylates couple with methylene-active compounds to yield hydrazo derivatives with high purity.The 1H and 13C NMR data of eleven such products are presented and analysed.The predominance of the hydrazo over the azo form is consistent with accepted criteria.Furthermore, evidence for the preference of the carbethoxy group over the acetyl group for intramolecular hydrogen bonding is suggested.KEY WORDS 1H NMR 13C NMR o-Benzenediazonium carboxylates Hydrazo compounds
