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European Journal of Medicinal Chemistry

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https://www.readbyqxmd.com/read/29775937/design-synthesis-and-biological-evaluation-of-a-series-of-novel-2-benzamide-4-6-oxy-n-methyl-1-naphthamide-pyridine-derivatives-as-potent-fibroblast-growth-factor-receptor-fgfr-inhibitors
#1
Manman Wei, Xia Peng, Li Xing, Yang Dai, Ruimin Huang, Meiyu Geng, Ao Zhang, Jing Ai, Zilan Song
Starting from the phase II clinical FGFR inhibitor lucitanib (2), we conducted a medicinal chemistry approach by opening the central quinoline skeleton coupled with a scaffold hopping process thus leading to a series of novel 2-benzamide-4-(6-oxy-N-methyl-1-naphthamide)-pyridine derivatives. Compound 25a was identified to show selective and equally high potency against FGFR1/2 and VEGFR2 with IC50 values less than 5.0 nM. Significant antiproliferative effects on both FGFR1/2 and VEGFR2 aberrant cancer cells were observed...
May 15, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29778893/synthesis-of-proline-derived-benzenesulfonamides-a-potent-anti-trypanosoma-brucei-gambiense-agent
#2
David I Ugwu, Uchechukwu C Okoro, Narendra K Mishra
Thousands of death in Africa and other developing nations are still attributed to trypanosomiasis. Excessive sleep has been associated with increased inflammation. We report herein, the synthesis, antitrypanosomal and anti-inflammatory activities of eight new carboxamide derivatives bearing substituted benzenesulfonamides. The base promoted reactions of l-proline and L-4-hydroxyproline with substituted benzenesulfonyl chlorides gave the benzenesulfonamides (11a-h) in excellent yields. Boric acid mediated amidation of the benzenesulfonamides (11a-h) and p-aminobenzoic acid (12) gave the new carboxamides (13a-h) in excellent yields...
May 14, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29777989/synthesis-antiproliferative-activity-and-mechanism-of-gallium-iii-thiosemicarbazone-complexes-as-potential-anti-breast-cancer-agents
#3
Jinxu Qi, Qian Yao, Kun Qian, Liang Tian, Zhen Cheng, Dongmei Yang, Yihong Wang
Five thiosemicarbazone ligands were synthesized and characterized by condensation with different aldehydes or ketones by 4-phenylthiosemicarbazone. The representative dichlorido[2-(Di-2-pyridinylmethylene)-Nphenylhydrazinecarbothioamide-N,N,S]-gallium(III) (Ga4) was characterized by X-ray single crystal diffraction, which was 1:1 ligand/Ga(III) complexes. The structure-activity relationship of these ligands and Ga (III) complexes have been investigated, and the results demonstrate that the formation of Ga (III) complexes have significant antiproliferative activity over the corresponding ligands...
May 14, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29778892/structure-based-design-of-novel-quinoxaline-2-carboxylic-acids-and-analogues-as-pim-1-inhibitors
#4
Bruno Oyallon, Marie Brachet-Botineau, Cédric Logé, Pascal Bonnet, Mohamed Souab, Thomas Robert, Sandrine Ruchaud, Stéphane Bach, Pascal Berthelot, Fabrice Gouilleux, Marie-Claude Viaud-Massuard, Caroline Denevault-Sabourin
We identified a new series of quinoxaline-2-carboxylic acid derivatives, targeting the human proviral integration site for Moloney murine leukemia virus-1 (HsPim-1) kinase. Seventeen analogues were synthesized providing useful insight into structure-activity relationships studied. Docking studies realized in the ATP pocket of HsPim-1 are consistent with an unclassical binding mode of these inhibitors. The lead compound 1 was able to block HsPim-1 enzymatic activity at nanomolar concentrations (IC50 of 74 nM), with a good selectivity profile against a panel of mammalian protein kinases...
May 11, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29777988/insight-into-structural-requirements-for-selective-and-or-dual-cxcr3-and-cxcr4-allosteric-modulators
#5
Anja Kolarič, Urban Švajger, Tihomir Tomašič, Regine Brox, Theresa Frank, Nikola Minovski, Nuska Tschammer, Marko Anderluh
Based on the previously published pyrazolopyridine-based hit compound for which negative allosteric modulation of both CXCR3 and CXCR4 receptors was disclosed, we designed, synthesized and biologically evaluated a set of novel, not only negative, but also positive allosteric modulators with preserved pyrazolopyridine core. Compound 9e is a dual negative modulator, inhibiting G protein activity of both receptors. For CXCR4 receptor para-substituted aromatic group of compounds distinguishes between negative and positive modulation...
May 11, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29778894/new-n-phenylpyrrolamide-dna-gyrase-b-inhibitors-optimization-of-efficacy-and-antibacterial-activity
#6
Martina Durcik, Denise Lovison, Žiga Skok, Cristina Durante Cruz, Päivi Tammela, Tihomir Tomašič, Davide Benedetto Tiz, Gábor Draskovits, Ákos Nyerges, Csaba Pál, Janez Ilaš, Lucija Peterlin Mašič, Danijel Kikelj, Nace Zidar
The ATP binding site located on the subunit B of DNA gyrase is an attractive target for the development of new antibacterial agents. In recent decades, several small-molecule inhibitor classes have been discovered but none has so far reached the market. We present here the discovery of a promising new series of N-phenylpyrrolamides with low nanomolar IC50 values against DNA gyrase, and submicromolar IC50 values against topoisomerase IV from Escherichia coli and Staphylococcus aureus. The most potent compound in the series has an IC50 value of 13 nM against E...
May 10, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29754075/corrigendum-to-optimization-of-physicochemical-properties-for-4-anilinoquinazoline-inhibitors-of-trypanosome-proliferation-eur-j-med-chem-141-2017-446-459
#7
Jennifer L Woodring, Kelly A Bachovchin, Kimberly G Brady, Mitchell F Gallerstein, Jessey Erath, Scott Tanghe, Susan E Leed, Ana Rodriguez, Kojo Mensa-Wilmot, Richard J Sciotti, Michael P Pollastri
No abstract text is available yet for this article.
May 10, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29777987/phthalocyanine-sulfonamide-conjugates-synthesis-and-photodynamic-inactivation-of-gram-negative-and-gram-positive-bacteria
#8
Raquel Nunes da Silva, Ângela Cunha, Augusto C Tomé
Phthalocyanines bearing four or eight sulfonamide units were synthesized and their efficiency in the photodynamic inactivation of Gram-negative (Escherichia coli) and Gram-positive (Staphylococcus aureus) bacteria was evaluated. Conjugates with simpler sulfonamide units (N,N-diethylbenzenesulfonamide, N-isopropylbenzenesulfonamide and N-(4-methoxyphenyl)benzenesulfonamide) caused stronger inactivation than those with heterocyclic groups (N-(thiazol-2-yl)benzenesulfonamide) or long alkyl chains (N-dodecylbenzenesulfonamide) in both bacteria...
May 9, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29775936/from-hit-to-lead-structure-based-discovery-of-naphthalene-1-sulfonamide-derivatives-as-potent-and-selective-inhibitors-of-fatty-acid-binding-protein-4
#9
Ding-Ding Gao, Hui-Xia Dou, Hai-Xia Su, Ming-Ming Zhang, Ting Wang, Qiu-Feng Liu, Hai-Yan Cai, Hai-Peng Ding, Zhuo Yang, Wei-Liang Zhu, Ye-Chun Xu, He-Yao Wang, Ying-Xia Li
Fatty acid binding protein 4 (FABP4) plays a critical role in metabolism and inflammatory processes and therefore is a potential therapeutic target for immunometabolic diseases such as diabetes and atherosclerosis. Herein, we reported the identification of naphthalene-1-sulfonamide derivatives as novel, potent and selective FABP4 inhibitors by applying a structure-based design strategy. The binding affinities of compounds 16dk, 16do and 16du to FABP4, at the molecular level, are equivalent to or even better than that of BMS309403...
May 9, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29775935/design-synthesis-antiproliferative-activity-and-docking-studies-of-quinazoline-derivatives-bearing-2-3-dihydro-indole-or-1-2-3-4-tetrahydroquinoline-as-potential-egfr-inhibitors
#10
Yiqiang OuYang, Wensheng Zou, Liang Peng, Zunhua Yang, Qidong Tang, Mengzi Chen, Shuang Jia, Hong Zhang, Zhou Lan, Pengwu Zheng, Wufu Zhu
Eight series of quinazoline derivatives bearing 2,3-dihydro-indole or 1,2,3,4-tetrahydroquinoline were designed, synthesized and evaluated for the IC50 values against three cancer cell lines (A549, MCF-7 and PC-3). Most of the forty nine target compounds showed excellent antiproliferative activity against one or several cancer cell lines. The compound 13a showed the best activity against A549, MCF-7 and PC-3 cancer cell lines, with the IC50 values of 1.09 ± 0.04 μM, 1.34 ± 0.13 μM and 1.23 ± 0...
May 9, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29763807/positional-scanning-library-applied-to-the-human-eosinophil-cationic-protein-rnase3-n-terminus-reveals-novel-and-potent-anti-biofilm-peptides
#11
David Pulido, Guillem Prats-Ejarque, Clara Villalba, Marcel Albacar, Mohammed Moussaoui, David Andreu, Rudolf Volkmer, Marc Torrent, Ester Boix
Eradication of established biofilm communities of pathogenic bacteria is one of the pending challenges in the development of new antimicrobial agents. In particular, the dreaded nosocomial Pseudomonas aeruginosa forms microbial communities that offer an enhanced resistance to conventional antibiotics. Recently, we have described an engineered antimicrobial peptide derived from the human RNase3, also named the eosinophil cationic protein (ECP), RN3 (5-36), which combines bactericidal activity with high cell agglutination and lipopolysaccharide (LPS) affinity...
May 8, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29763806/a-review-on-flavonoid-based-scaffolds-as-multi-target-directed-ligands-mtdls-for-alzheimer-s-disease
#12
REVIEW
Leili Jalili-Baleh, Elaheh Babaei, Shahin Abdpour, Syed Nasir Abbas Bukhari, Alireza Foroumadi, Ali Ramazani, Mohammad Sharifzadeh, Mohammad Abdollahi, Mehdi Khoobi
Alzheimer's disease (AD), the most common form of dementia, is a multifactorial neurodegenerative disease. The target enzymes inhibition including cholinesterase, beta-secretase, monoamine oxidase and inhibition of amyloid-β aggregation as well as oxidative stress and metal chelation play an important role in the pathogenesis of AD. Chroman-4-one scaffold with benzo-γ-pyrone network is a privileged structure in organic synthesis and drug design. A large number of research has been carried out on modified naturally occurring chromanone scaffolds and/or synthesized new analogues, to obtain effective drugs for AD management...
May 7, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29754076/discovery-of-novel-%C3%AE-carboline-acylhydrazone-hybrids-as-potent-antitumor-agents-and-overcome-drug-resistance
#13
Yong Li, Wei Yan, Jianhong Yang, Zhuang Yang, Mengshi Hu, Peng Bai, Minghai Tang, Lijuan Chen
Twenty-four novel β-carboline/acylhydrazone hybrids were synthesized and evaluated for their in vitro antiproliferative activity. Among them, 12r exhibited the most potent activity, with IC50 values of 1-2 μM against panel of cancer cell lines and retained significant activity in multidrug resistant cancer cells. Treated cells were not arrested in any phase of cell cycle but resulted in late cellular apoptosis on both MCF-7 and MCF-7/ADR cancer cells. Importantly, 12r showed certain antitumor effect on inhibiting the tumor growth with low toxic and side effects and without significant body weight loss...
May 7, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29747120/corrigendum-to-design-synthesis-dft-study-and-antifungal-activity-of-the-derivatives-of-pyrazolecarboxamide-containing-thiazole-or-oxazole-ring-eur-j-med-chem-149-2018-170-181
#14
Zhongzhong Yan, Aiping Liu, Mingzhi Huang, Minhua Liu, Hui Pei, Lu Huang, Haibo Yi, Weidong Liu, Aixi Hu
No abstract text is available yet for this article.
May 7, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29763805/design-synthesis-and-biological-evaluation-of-novel-quinazoline-2-4-diones-conjugated-with-different-amino-acids-as-potential-chitin-synthase-inhibitors
#15
Nada A Noureldin, Hend Kothayer, El-Sayed M Lashine, Mohamed M Baraka, Yanrong Huang, Bing Li, Qinggang Ji
A series of (2-(1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl) acetamido) acids) (6 a-m), (7) has been designed to inhibit the action of fungus chitin synthase enzyme (CHS). The synthesis of the designed compounds was carried out in four steps starting from the reaction between 1-methylquinazoline-2,4(1H,3H)-dione and ethyl chloroacetate to yield the ethyl acetate derivative. This ester was hydrolyzed to the corresponding carboxylic acid derivative that was then utilized to couple several amino acids getting the final designed compounds...
May 4, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29751237/current-anti-diabetic-agents-and-their-molecular-targets-a-review
#16
REVIEW
Nagaraju Kerru, Ashona Singh-Pillay, Paul Awolade, Parvesh Singh
Diabetes mellitus is a medical condition characterized by the body's loss of control over blood sugar. The frequency of diagnosed cases and consequential increases in medical costs makes it a rapidly growing chronic disease that threatens human health worldwide. In addition, its unnerving statistical projections are perilous to both the economy of the nation and man's life expectancy. Type-I and type-II diabetes are the two clinical forms of diabetes mellitus. Type-II diabetes mellitus (T2DM) is illustrated by the abnormality of glucose homeostasis in the body, resulting in hyperglycemia...
May 3, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29751235/functionalized-spirooxindole-indolizine-hybrids-stereoselective-green-synthesis-and-evaluation-of-anti-inflammatory-effect-involving-tnf-%C3%AE-and-nitrite-inhibition
#17
Raju Suresh Kumar, Paulrayer Antonisamy, Abdulrahman I Almansour, Natarajan Arumugam, Govindasami Periyasami, Mohammad Altaf, Ha-Rim Kim, Kang-Beom Kwon
Stereoselective synthesis of a small library of novel spiroheterocyclic hybrids including indolizine, oxindole, and substituted piperidine units has been accomplished in [bmim]Br using a [3 + 2] cycloaddition strategy in good yield and were tested for their anti-inflammatory activities. The effects of compounds (4a-o) against inflammation were studied using carrageenan-induced hind paw oedema, croton oil-induced ear oedema, and cotton pellet-induced granuloma models. Among the heterocyclic hybrids, compounds 4d, 4g, and 4o showed significant anti-inflammatory activities against acute and chronic inflammatory models...
May 3, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29763808/design-synthesis-and-evaluation-of-novel-multi-target-directed-ligands-for-treatment-of-alzheimer-s-disease-based-on-coumarin-and-lipoic-acid-scaffolds
#18
Leili Jalili-Baleh, Hamid Forootanfar, Tuba Tüylü Küçükkılınç, Hamid Nadri, Zahra Abdolahi, Alieh Ameri, Mandana Jafari, Beyza Ayazgok, Maryam Baeeri, Mahban Rahimifard, Syed Nasir Abbas Bukhari, Mohammad Abdollahi, Mohammad Reza Ganjali, Saeed Emami, Mehdi Khoobi, Alireza Foroumadi
A novel series of coumarin-lipoic acid conjugates were synthesized via cycloaddition click reaction to find out new multi-target-directed ligands (MTDLs) for treatment of Alzheimer's disease (AD). All of synthesized compounds were screened for neuroprotective and anti-cholinesterase activities. Based on primary screening, two compounds (5 and 11) were subjected to further biological evaluations. In particular, compound 11 which was the most potent AChE inhibitor showed good inhibitory effect on Aβ-aggregation and intracellular ROS (reactive oxygen species) formation, as well as the ability of selective bio-metal chelation and neuroprotection against H2 O2 - and Aβ1-42 -induced cytotoxicity...
May 2, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29758517/identification-of-chalcone-based-antileishmanial-agents-targeting-trypanothione-reductase
#19
Margherita Ortalli, Andrea Ilari, Gianni Colotti, Ilenia De Ionna, Theo Battista, Alessandra Bisi, Silvia Gobbi, Angela Rampa, Rita M C Di Martino, Giovanna A Gentilomi, Stefania Varani, Federica Belluti
All currently used first-line and second-line drugs for the treatment of leishmaniasis exhibit several drawbacks including toxicity, high costs and route of administration. Furthermore, some drugs are associated with the emergence of drug resistance. Thus, the development of new treatments for leishmaniasis is a priority in the field of neglected tropical diseases. The present work highlights the use of natural derived products, i.e. chalcones, as potential source of antileishmanial agents. Thirty-one novel chalcone compounds have been synthesized and their activity has been evaluated against promastigotes of Leishmania donovani; 16 compounds resulted active against L...
May 2, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29751233/new-developments-in-non-quinolone-based-antibiotics-for-the-inhibiton-of-bacterial-gyrase-and-topoisomerase-iv
#20
REVIEW
Syed Lal Badshah, Asad Ullah
The inhibition of pathogenic bacteria at the replication stage is important to halt their further reproduction and spread. The replication enzymes include the DNA gyrase and topoisomerase IV that are recognized targets for the infection control. Novel antibiotic compounds are always in demand for targeting different active sites of these enzymes. Although quinolones are the current drug of choice for targeting these enzymes, emerging resistance is a global concern. Wide-scale efforts are needed to overcome the emerging resistance by designing more potent drugs...
May 1, 2018: European Journal of Medicinal Chemistry
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