- Synthesis, characterization of novel coupling products and 4-arylhydrazono-2-pyrazoline-5-ones as potential antimycobacterial agents
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Novel coupling products 7a-d and 4-arylhydrazono-2-pyrazoline-5-ones 8a-e were synthesized and evaluated for antimycobacterial activity against Mycobacterium tuberculosis H37Rv and Mycobacterium avium. Compound 7b was found to be the most potent derivatives of the 7a-d series by an MIC value of 6.25 μg/ml.
- Kuecuekguezel, S. Gueniz,Rollas, Sevim
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- Design and Bioevaluation of Novel Hydrazide-Hydrazones Derived from 4-Acetyl-N-Substituted Benzenesulfonamide
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Abstract: In this research, a series of hydrazine-hydrazone derivatives (Ia–g), (IIa–h) were synthesized to discover new antioxidant and anticholinesterase agents. The structures of synthesized compounds were characterized by spectroscopic data using UV, IR, 1H, 13C NMR, mass spectroscopy, and elemental analysis. The bio-evaluation of the synthesized compounds (Ia–g), (IIa–h) were evaluated according to in vitro activity assays. The results of β-carotene/linoleic acid assay showed that among the synthesized compounds, the (Ib), (Ie), (IIb–IIe), and (IIh) compound exhibited higher activity for the lipid peroxidation inhibitory activity. In the DPPH free scavenging activity and the cation radical scavenging activity in ABTS?+ activity, compound (IIb) was found to be more active. In the CUPRAC reduced power assay, the A0.5 values of all synthesized compounds were better than α-TOC. In AChE assay, compound (IIb) exhibited the most activity with IC50 = 11.12 ± 0.74 μM, while the compounds (Ib–g) and (IIb–h), exhibited excellent activity than the positive standard galantamine (IC50 = 46.06 ± 0.10 μM) in the BChE assay.
- ?ztürk, M.,Bozkurt, E.,Iyido?an, A. Karakü?ük,Oru?-Emre, E. E.,S?cak, Y.
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p. 702 - 714
(2020/10/29)
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- Design of Hydrazide-Bearing HDACIs Based on Panobinostat and Their p53 and FLT3-ITD Dependency in Antileukemia Activity
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Here, we present a new series of hydrazide-bearing class I selective HDAC inhibitors designed based on panobinostat. The cap, linker, and zinc-binding group were derivatized to improve HDAC affinity and antileukemia efficacy. Lead inhibitor 13a shows picomolar or low nanomolar IC50 values against HDAC1 and HDAC3 and exhibits differential toxicity profiles toward multiple cancer cells with different FLT3 and p53 statuses. 13a indirectly inhibits the FLT3 signaling pathway and down-regulates master antiapoptotic proteins, resulting in the activation of pro-caspase3 in wt-p53 FLT3-ITD MV4-11 cells. While in the wt-FLT3 and p53-null cells, 13a is incapable of causing apoptosis at a therapeutic concentration. The MDM2 antagonist and the proteasome inhibitor promote 13a-triggered apoptosis by preventing p53 degradation. Furthermore, we demonstrate that apoptosis rather than autophagy is the key contributing factor for 13a-triggered cell death. When compared to panobinostat, 13a is not mutagenic and displays superior in vivo bioavailability and a higher AUC0-inf value.
- Li, Xiaoyang,Jiang, Yuqi,Peterson, Yuri K.,Xu, Tongqiang,Himes, Richard A.,Luo, Xin,Yin, Guilin,Inks, Elizabeth S.,Dolloff, Nathan,Halene, Stephanie,Chan, Sherine S. L.,Chou, C. James
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p. 5501 - 5525
(2020/06/10)
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- Synthesis, chemical characterization and antimicrobial activity of new acylhydrazones derived from carbohydrates
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A new series of glycosylated acylhydrazones was synthesized and all the chemical structures were confirmed by High Resolution Mass Spectrometry (HRMS), 1H and 13C Nuclear Magnetic Resonance (1H-NMR; 13C-NMR) and Fourier Transform Infrared (FTIR) spectroscopy methods. The mass accuracy between the calculated and found values observed in HRMS analyses were near or lower than 5 ppm, which are acceptable for proposing a molecular formula using this technique. All of the synthesized compounds were screened for their antibacterial, antifungal and antiviral activities. Five compounds (12, 13, 14, 16 and 19) exerted a modest antifungal activity against the strains evaluated. Derivative 14 showed fungicidal activity against Candida glabrata at 173.8 μM and saccharide unit contributed to the increase of the antifungal potential against this strain. New chemical manipulation of derivative 14 can make it possible to obtain new potentially antimicrobial agents.
- Guilherme, Fernanda Dias,Simonetti, Julia évelin,Folquitto, Lais Regina Santos,Reis, Adriana Cotta Cardoso,Oliver, Josidel Concei??o,Dias, Amanda Latércia Tranches,Dias, Danielle Ferreira,Carvalho, Diogo Teixeira,Brand?o, Geraldo Célio,Souza, Thiago Belarmino de
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p. 349 - 356
(2019/03/04)
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- Development of novel Asf1-H3/H4 inhibitors
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The histone chaperone anti-silencing function 1 (Asf1) has emerged as a promising target for therapeutic intervention for multiple cancers (Cell 2006, 127, 458). Asf1 is involved in the packaging of the eukaryotic genome into chromatin, which is essential
- Miknis, Greg F.,Stevens, Sarah J.,Smith, Luke E.,Ostrov, David A.,Churchill, Mair E.A.
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supporting information
p. 963 - 968
(2015/02/19)
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- GPR17 Receptor Modulators
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Chemical compounds are provided which act on GPR17 receptors and are useful in the treatment or amelioration of chronic and/or acute neurodegenerative diseases, such as multiple sclerosis, inflammatory diseases, pathologies involving the immune system, cardiovascular diseases, and renal diseases.
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Paragraph 0042; 0043
(2015/05/26)
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- Synthesis of 1-aroyl-3,5-dimethyl-1H-pyrazoles as anti-HCV and anticancer agents
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1-Aroyl-3,5-dimethyl-1H-pyrazole derivatives (7-12) were synthesized from some hydrazides (1-6) with acetylacetone (2,4-pentanedione) by microwave irradiation. Their structures were elucidated by FT-IR and 1H-NMR spectral data and elemental analysis. Compound activities were evaluated against HCV NS5B and in cell based HCV reporters. Compound 8 was the most promising of this series in inhibiting intracellular NS5B activity and HCV RNA replication in reporter cells. The selected compounds 9, 10 and 12 by National Institue of Health were screened for their anticancer activity against 60 human tumor cell lines. Compound 9 (3-[(3,5-dimethyl-1H-pyrazol-1-yl)carbonyl]-2′,4′- difluorobiphenyl-4-ol) possessed significant activity against human immortalized myelogenous leukemia (K-562) exhibiting cell growth promotion 30.05%, with inhibition of 69.95% at 10-5M concentration. Compounds 3 and 9 were evaluated for cell viability and growth inhibition by K-562 cells of MTT assay, at different doses (10-6- 10-2M). Further, compound 9 exhibited anticancer activity against K-562 cells with IC50 value of 4 μM . Apoptosis levels of compound 9 were determined for three different concentrations (10-6, 10-5 and 10-3M) at two time points (24 and 48 h). Compound 9 induced apoptosis of K-562 cells, thus suggesting that compound 9 might be a potential chemopreventive agent for chronic myelogenous leukemia.
- Aydin, Sevil,Kaushik-Basu, Neerja,Oezbas-Turan, Suna,Akbuga, Juelide,Tiber, Pinar Mega,Orun, Oya,Gurukumar,Basu, Amartya,Kuecuekguezel, S. Gueniz
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p. 121 - 131
(2014/03/21)
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- Synthesis of new biheterocycles containing a 1,4-benzodioxane fragment
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The reaction of 1,4-benzodioxane-2-carbonyl chloride with 5-(4-aminophenyl)-1,3,4-oxa- and -thiadiazole-2-thiols afforded new biheterocyclic compounds which were converted into the corresponding S-benzyl derivatives by treatment with benzyl chloride. 5-(4
- Avakyan,Vartanyan,Sargsyan,Markaryan
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p. 434 - 438
(2014/06/09)
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- GPR17 RECEPTOR MODULATORS
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The present invention relates to chemical compounds acting through GPR17 receptor for use in the treatment o f diseases, in particular for use in chronic and/or acute neurodegenerative diseases, preferably Multiple Sclerosis, inflammatory diseases, pathologies involving the immune system, cardiovascular diseases, renal diseases.
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Page/Page column 25
(2013/12/03)
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- Synthesis of 5-(4-aminophenyl)-2-(arylamino)-1,3,4-thiadiazoles and their schiff base derivatives as antimycobacterial agents
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The condensation reaction of 5-(4-aminophenyl)-N-aryl-1,3,4-thiadiazol-2- ylamines with salicylaldehyde, 3-hydroxybenzaldehyde, 4-hydroxybenzaldehyde, 5-bromosalicylaldehyde, 5-chlorosalicylaldehyde, 4-methoxybenzaldehyde, 3-nitrobenzaldehyde, and 4-nitro
- Dilmaghani,Jazani,Nasuhi Pur,Shokoufeh,Ghadiri,Fakhraee
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p. 362 - 367
(2012/08/27)
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- OXADIAZOLE DERIVATIVES AND THEIR USE AS NICOTINIC ACETYLCHOLINE RECEPTOR MODULATORS
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The present invention relates to novel oxadiazole derivatives as nAChR agonists having pharmacological activity, processes for their preparation, compositions containing them and their use in the treatment of neurological, psychiatric disorders and gastro
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Page/Page column 28
(2009/07/17)
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- Synthesis and anticonvulsant activity of new N-(alkyl/Sub-stituted aryl)-N'-[4-(5-cyclohexylamino)-1,3,4-thiadiazole-2-ylphenyl]thioureas
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A series of novel thiourea derivatives carrying the 5-cylohexylamino-1,3,4- thiadiazole moiety was synthesized and their anticonvulsant activity was evaluated. Structures of the synthesized compounds have been confirmed by IR, 1H-NMR, and eleme
- Karakus, Sevgi,Kocyigit-Kaymakcioglu, Bedia,Toklu, Hale Z.,Aricioglu, Feyza,Rollas, Sevim
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scheme or table
p. 48 - 53
(2009/06/17)
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- 2-PHENYL-5-AMINO-1,3,4-OXADIAZOLES AND THEIR USE AS NICOTINIC ACETYLCHOLINE RECEPTOR LIGANDS
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The present invention relates to novel oxadiazole derivatives of formula (1) having pharmacological activity, processes for their preparation, compositions containing them and their use in the treatment of neurological, psychiatric disorders and gastrointestinal disorders through modulation of the nicotinic α7 receptor formula (I).
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Page/Page column 45
(2008/06/13)
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- Synthesis, characterization and biological activities of substituted oxadiazole, triazole, thiadiazole and 4-thiazolidinone derivatives
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The synthesis and biological activities (anti-inflammatory and antibacterial) of a number of 2,5-substituted 1,2,4-triazole, 1,3,4-thiadiazole/oxadiazole and 2,3-substituted-4-thiazolidinone derivatives are described. The anti-inflammatory activity was ca
- Amir, Mohd,Khan,Zaman
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p. 2189 - 2194
(2007/10/03)
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- Synthesis and antituberculosis activity of new N-phenyl-N′-[4-(5-alkyl/arylamino-1,3,4-thiadiazole-2-yl)phenyl] thioureas
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In this study, eight original N-phenyl-N′-[4-(5-alkyl/arylamino-1,3,4-thiadiazole-2-yl)phenyl] thiourea derivatives were synthesized and tested for antituberculosis activity. Antituberculosis activities of the synthesized compounds were screened in vitro
- Karakus,Rollas
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p. 577 - 581
(2007/10/03)
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- Some 3-Thioxo/Alkylthio-1,2,4-triazoles with a Substituted Thiourea Moiety as Possible Antimycobacterials
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A series of novel N-alkyl/aryl-N'-[4-(4-alkyl/aryl-2,4-dihydro-3H-1,2,4-triazole-3-thione-5-yl)phenyl]thioureas 1-19 and three S-alkylated representatives of the former, N-alkyl/aryl-N'-[4-(3-aralkylthio-4-alkyl/aryl-4H-1,2,4-triazole-5-yl)phenyl]thioureas 20-22, were synthesized and tested for antimycobacterial activity against Mycobacterium tuberculosis H37Rv as well as Mycobacterium fortuitum ATCC 6841 which is a rapid growing opportunistic pathogen. Compounds 4 and 9-11 were found to possess the same MIC value with that of Tobramycin against M. fortuitum ATCC 6841 whereas 1-3 and 21 had positive response against M. tuberculosis H37Rv at varying degrees. Compound 21 was identified as the most potent derivative of the 1-22 series by an MIC value of 6.25 μg/ml and selectivity index of 1.6
- Kuecuekguezel, Ilkay,Kuecuekguezel, S. Gueniz,Rollas, Sevim,Kiraz, Muammer
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p. 1703 - 1708
(2007/10/03)
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