- Pyrazolone incorporating amino acid metallointercalators as effective DNA targets: Synthesis and in vitro biocidal evaluation
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Three novel mixed-ligand complexes using pyrazolone derivative (4-chloro-benzylidene-4-aminoantipyrine) as primary ligand and l-methionine as co-ligand, were synthesized and characterized by physico-chemical analytical techniques. The DNA interaction of t
- Raman, Natarajan,Selvaganapathy, Muthusamy
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- Spectroscopic, electrochemical DNA binding and in vivo anti-inflammatory studies on newly synthesized Schiff bases of 4-aminophenazone
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4-Aminophenazone (Ap-1) Schiff bases i.e., 4-{(3,4,5-trimethoxybenzylidine) amino}phenazone (Ap-2), 4-{(2-chlorobenzylidine) amino}phenazone (Ap-3) and 4-{(4-chlorobenzylidine)amino} phenazone (Ap-4) were synthesized and characterized by different spectro
- Arshad, Nasima,Ahmad, Mukhtar,Ashraf, Muhammad Zaman,Nadeem, Humaira
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- Antipyrine cationic surfactants capping silver nanoparticles as potent antimicrobial agents against pathogenic bacteria and fungi
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Development of effective anti-microbial agents has been hindered by the emergence of bacterial strains with multi-drug resistance. In this article, we report an efficient synthesis of silver nanoparticle (AgNP) by capping with a synthetic cationic surfact
- Aiad,Marzouk, Magda I.,Shaker, Soheir A.,Ebrahim, Nagwa E.,Abd-Elaal, Ali A.,Tawfik, Salah M.
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- Synthesis and biological evaluation of new pyrazolone Schiff bases as monoamine oxidase and cholinesterase inhibitors
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In the current work, Schiff base derivatives of antipyrine were synthesized. The chemical characterization of the compounds was confirmed using IR, 1H NMR, 13C NMR and mass spectroscopies. The inhibitory potency of synthesized compounds was investigated towards acetylcholinesterase (AChE), butyrylcholinesterase (BuChE), and monoamine oxidases A and B (MAO-A and MAO-B) enzymes. Some of the compounds displayed significant inhibitory activity against AChE and MAO-B enzymes, respectively. According to AChE enzyme inhibition assay, compounds 3e and 3g were found as the most potent derivatives with IC50 values of 0.285 μM and 0.057 μM, respectively. Also, compounds 3a (IC50 = 0.114 μM), 3h (IC50 = 0.049 μM), and 3i (IC50 = 0.054 μM) were the most active derivatives against MAO-B enzyme activity. So as to understand inhibition type, enzyme kinetics studies were carried out. Furthermore, molecular docking studies were performed to define and evaluate the interaction mechanism between compounds 3g and 3h and related enzymes. ADME (Absorption, Distribution, Metabolism, and Excretion) and BBB (Blood, Brain, Barier) permeability predictions were applied to estimate pharmacokinetic profiles of synthesized compounds.
- Tok, Fatih,Ko?yi?it-Kaymak??o?lu, Bedia,Sa?l?k, Begüm Nurpelin,Levent, Serkan,?zkay, Yusuf,Kaplanc?kl?, Zafer As?m
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- Preparation of a simple biocompatible magnetite@citric acid: An efficient reusable solid acid catalyst for the rapid synthesis of antipyrine Schiff’s bases and study of their radical scavenging potential
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Citric acid immobilized magnetic nanoparticles (MNPs@CA) have been synthesized and used for the preparation of bio-important antipyrine (1,5-dimethyl-2-phenyl-1,2-dihydro-3H-pyrazol-3-one) derived Schiff’s bases (3a–k) in lesser reaction time with very hi
- Kumari, Mitlesh,Gupta, Ragini,Jain, Yachana
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supporting information
p. 529 - 538
(2019/02/01)
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- Supramolecular coordination and antimicrobial activities of constructed mixed ligand complexes
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A novel series of copper(II) and palladium(II) with 4-derivatives benzaldehyde pyrazolone (Ln) were synthesized. The mixed ligand complexes were prepared by using 1,10-phenanthroline (Phen) as second ligand. The structure of these complexes was
- El-Sonbati,Diab,El-Bindary,Abou-Dobara,Seyam
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p. 213 - 221
(2013/04/10)
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- Design, synthesis, antimicrobial, anticancer evaluation, and QSAR studies of 4-(substituted benzylidene-Amino)-1,5-dimethyl-2-phenyl-1,2-dihydropyrazol-3- ones
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A series of 4-(substituted benzylidene-Amino)-1,5-dimethyl-2-phenyl-1,2- dihydropyrazol-3-ones (1-17) was synthesized and tested in vitro for its antimicrobial and anticancer potentials. The biological screening results indicated that compounds having m-c
- Sigroha, Sumit,Narasimhan, Balasubramanian,Kumar, Pradeep,Khatkar, Anurag,Ramasamy, Kalavathy,Mani, Vasudevan,Mishra, Rakesh Kumar,Majeed, Abu Bakar Abdul
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p. 3863 - 3875
(2013/02/25)
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- Predictions and correlations of structure activity relationship of some aminoantipyrine derivatives on the basis of theoretical and experimental ground
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A series of 4-aminoantipyrine derivatives were produced by condensing aromatic primary amine, namely, 4-aminoantipyrine with different aryl carbonyls which occurred cleanly and efficiently without using any catalyst at room temperature. Their structures w
- Ali, Parvez,Meshram, Jyotsna,Sheikh, Javed,Tiwari, Vandana,Dongre, Rajendra,Hadda, Taibi B.
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experimental part
p. 157 - 164
(2012/07/28)
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- Synthesis of novel Schiff base analogues of 4-amino-1,5-dimethyl-2- phenylpyrazol-3-one and their evaluation for antioxidant and anti-inflammatory activity
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4-Aminoantipyrine (4-amino-1,5-dimethyl-2-phenylpyrazole-3-one) and its analogues have been found to be compounds of interest for their anti-inflammatory, analgesic, antiviral, antipyretic, antirheumatic and antimicrobial activities. In the present study,
- Alam, Mohammad Sayed,Choi, Jung-Hyun,Lee, Dong-Ung
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experimental part
p. 4103 - 4108
(2012/09/21)
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- Supramolecular and structural modification on conformational by mixed ligand
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A novel series of platinum(II) and palladium(II) complexes have been synthesized by template condensation of 4-methoxybenzaldehyde, benzaldehyde, 4-chlorobenzaldehyde and 4-nitrobenzaldehyde, with appropriate 4-aminoantipyrine (4-AAP) in the presence of K
- El-Sonbati,Diab,El-Bindary,Abd El-Kader
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p. 211 - 217
(2013/01/15)
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- Brand new quantitative solid-state synthesis of N-pyrazolyl azomethines
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Fifteen preparatively useful azomethines 3 and 5 have been quantitatively (100% yield at 100% conversion) obtained as hydrates by ball-milling together 4-aminoantipyrine 1 and 3-amino-4,6-dimethylpyrazolopyridine 4 with solid benzaldehydes 2 without passi
- Abdel-Latif, Ehab,Kaupp, Gerd,Metwally, Mohamed A.
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p. 187 - 189
(2007/10/03)
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- Synthesis and pharmacological screening of a new series of 3-(4-antipyryl)-2-arylthiazolidin-4-ones
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A series of 3-(4-antipyryl)-2-arylthiazolidin-4-one derivatives were synthesized and pharmacologically evaluated for antinociceptive, spasmolytic and cardiovascular activities.The presence of a methoxy-naphthyl or a substituted phenyl group in 2-position
- Al-Khamees, Hamad A.,Bayomi, Said M.,Kandil, Hesham A.,El-Tahir, Kamal E. H.
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p. 103 - 106
(2007/10/02)
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- REACTION OF SCHIFF BASES OBTAINED FROM 4-AMINOANTIPYRINE AND 4-AMINO-1,2,4-TRIAZOLE WITH KETONES
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With acetophenone and p-nitroacetophenone in alcohol and benzene media in the presence of acid N-arylidene-4-aminoantipyrines form α,β-unsaturated ketones, and with antipyrine the form aryldiantipyrylmethanes.With the same ketones N-arylidene-4-amino-1,2,4-triazoles form the products from addition at the azomethine bond.In both cases reaction with benzylideneacetone was not detected.
- Letunov, V. I.
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p. 145 - 149
(2007/10/02)
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