- Promising Ag(I) complexes with N-acylhydrazones from aromatic aldehydes and isoniazid against multidrug resistance in tuberculosis
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In the present work, synthesis, characterization and antitubercular assays of N-acylhydrazones derivatives and their corresponding silver(I) complexes are described. The compounds were characterized by elemental analysis, IR and NMR spectroscopic measurem
- dos Santos, Paulo Victor P.,Ribeiro, Camila M.,Pavan, Fernando R.,Corbi, Pedro P.,Bergamini, Fernando R.G.,Carvalho, Marcos A.,D'Oliveria, Kaique A.,Cuin, Alexandre
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- Acylhydrazones as isoniazid derivatives with multi-target profiles for the treatment of Alzheimer's disease: Radical scavenging, myeloperoxidase/acetylcholinesterase inhibition and biometal chelation
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Acylhydrazones 1a-o, derived from isoniazid, were synthesized and evaluated for Myeloperoxidase (MPO) and Acetylcholinesterase (AChE) inhibition, as well as their antioxidant and metal chelating activities, with the purpose of investigating potential multi-target profiles for the treatment of Alzheimer's disease. Synthesized compounds were tested using the 2,2-diphenyl-2-picrylhydrazyl (DPPH) method and 1i, 1j and 1 m showed radical scavenging ability. Compounds 1b, 1 h, 1i, 1 m and 1o inhibited MPO activity (10 μM) at 96.1 ± 5.5%, 90 ± 2.1%, 100.3 ± 1.7%, 80.1 ± 9.4% and 82.2 ± 10.6%, respectively, and only compound 1 m was able to inhibit 54.2 ± 1.7% of AChE activity (100 μM). Docking studies of the most potent compound 1 m were carried out, and the computational results provided the theoretical basis of enzyme inhibition. Furthermore, compound 1 m was able to form complexes with Fe2+ and Zn2+ ions in a 2:1 ligand:metal ratio according to the Job Plot method.
- Henriques, Ruan Roberto,Junior, Marcos Antonio de Abreu Lopes,Nogueira, Thayssa Lisboa do Couto,Romeiro, Nelilma Correia,Silva, Leandro Louback da,Farias, André Borges,Quimas, Jo?o Victor Fernandes,Santos, Daniela Corrêa,Souza, Andréa Luzia Ferreira de
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- Antimicrobial activities of synthetic arylidine nicotinic and isonicotinic hydrazones
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Background: Despite availability of variety of antibacterial agents, re-emergance of pathogenic bacteria is still a serious medical concern. Identification of new, safer, and selective antibacterial agents is the key interest in the medicinal chemistry research. Methods: A library of synthetic arylidene nicotinic and isonicotinic hydrazones (1-63) were investigated for antimicrobial activities. Results: A number of derivatives showed significant to moderate antimicrobial activities against Gram positive and Gram negative bacterial cultures. Few compounds also showed antifungal activity against fungal cultures. Minimum Inhibitory Concentration (MIC) was calculated for the most active compounds 1, 7, 11, 19, 34, 46, 50, 51, and 55 against gram positive and gram negative cultures. Conclusion: Newly identified compounds may serve as lead for future research in order to get the more powerful antibacterial agents.
- Hayat, Muhammad,Khan, Khalid Mohammed,Saeed, Sumayya,Salar, Uzma,Khan, Momin,Baig, Taimoor,Ahmad, Aqeel,Parveen, Shahnaz,Taha, Muhammad
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p. 1057 - 1067
(2018/10/31)
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- Xanthine oxidase inhibitory activity of nicotino/isonicotinohydrazides: A systematic approach from in vitro, in silico to in vivo studies
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Change in life style and eating habits has led to an increased prevalence of hyperuricemia worldwide. The role of hyperuricemia is no more restricted to gout, but it has a central role in progression of CVD, hypertension, metabolic syndrome, and arthritis
- Zafar, Humaira,Hayat, Muhammad,Saied, Sumayya,Khan, Momin,Salar, Uzma,Malik, Rizwana,Choudhary, M. Iqbal,Khan, Khalid Mohammed
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p. 2351 - 2371
(2017/04/03)
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- From Dynamic Combinatorial Chemistry to in Vivo Evaluation of Reversible and Irreversible Myeloperoxidase Inhibitors
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The implementation of dynamic combinatorial libraries allowed the determination of highly active reversible and irreversible inhibitors of myeloperoxidase (MPO) at the nanomolar level. Docking experiments highlighted the interaction between the most activ
- Soubhye, Jalal,Gelbcke, Michel,Van Antwerpen, Pierre,Dufrasne, Fran?ois,Boufadi, Mokhtaria Yasmina,Nève, Jean,Furtmüller, Paul G.,Obinger, Christian,Zouaoui Boudjeltia, Karim,Meyer, Franck
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supporting information
p. 206 - 210
(2017/03/08)
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- Synthesis and biological screening of some pyridine derivatives as anti-malarial agents
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Two series of pyridine derivatives were synthesised and evaluated for their in vivo anti-malarial activity against Plasmodium berghei. The anti-malarial activity was determined in vivo by applying 4-day standard suppressive test using chloroquine (CQ)-sen
- Bekhit, Adnan A.,Hymete, Ariaya,Damtew, Ashenafi,Mohamed, Abdel Maaboud I.,Bekhit, Alaa El-Din A.
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experimental part
p. 69 - 77
(2012/04/05)
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