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Future Medicinal Chemistry

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https://www.readbyqxmd.com/read/28636454/anticancer-potential-of-sanguinarine-for-various-human-malignancies
#1
Iman W Achkar, Fatima Mraiche, Ramzi M Mohammad, Shahab Uddin
Sanguinarine (Sang) - a benzophenanthridine alkaloid extracted from Sanguinaria canadensis - exhibits antioxidant, anti-inflammatory, proapoptotic and growth inhibitory activities on tumor cells of various cancer types as established by in vivo and in vitro studies. Although the underlying mechanism of Sang antitumor activity is yet to be fully elucidated, Sang has displayed multiple biological effects, which remain to suggest its possible use in plant-derived treatments of human malignancies. This review covers the anticancer abilities of Sang including inhibition of aberrantly activated signal transduction pathways, induction of cell death and inhibition of cancer cell proliferation...
June 21, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28636418/dxs-as-a-target-for-structure-based-drug-design
#2
Robin Matthias Gierse, Eswar Redeem, Eleonora Diamanti, Carsten Wrenger, Matthew R Groves, Anna Kh Hirsch
In this review, we analyze the enzyme DXS, the first and rate-limiting protein in the methylerythritol 4-phosphate pathway. This pathway was discovered in 1996 and is one of two known metabolic pathways for the biosynthesis of the universal building blocks for isoprenoids. It promises to offer new targets for the development of anti-infectives against the human pathogens, malaria or tuberculosis. We mapped the sequence conservation of 1-deoxy-xylulose-5-phosphate synthase on the protein structure and analyzed it in comparison with previously identified druggable pockets...
June 21, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28636417/a-novel-antimicrobial-approach-based-on-the-inhibition-of-zinc-uptake-in-salmonella-enterica
#3
Andrea Battistoni, Serena Ammendola, Emilia Chiancone, Andrea Ilari
In this review we discuss evidences suggesting that bacterial zinc homeostasis represents a promising target for new antimicrobial strategies. The ability of the gut pathogen Salmonella enterica sv Typhimurium to withstand the host responses aimed at controlling growth of the pathogen critically depends on the zinc importer ZnuABC. Strains lacking a functional ZnuABC or its soluble component ZnuA display a dramatic loss of pathogenicity, due to a reduced ability to express virulence factors; withstand the inflammatory response; and compete with other gut microbes...
June 21, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28636412/comparative-chemical-and-biological-studies-of-leaves-and-pollens-of-phoenix-canariensis-hort-ex-chabaud
#4
Mohamed S Hifnawy, Amr Mk Mahrous, Amany A Sleem, Rehab Ms Ashour
AIM:  Phoenix canariensis hort. ex Chabaud is one of the most important palm plants. In spite of that, it has not been extensively investigated from a phytochemical or a biological perspective. MATERIALS & METHODS: Air-dried powdered leaves and pollen grains of the plant were extracted using 70% ethanol. The residues were fractionated with different solvents of increasing polarity. Antioxidant, anti-inflammatory, hepatoprotective, anti-hyperglycemic activities were determined using adult male albino rats of wistar strain...
June 21, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28635318/what-structural-modifications-can-be-used-for-brd4-inhibitors-for-their-use-in-leukemia-therapy
#5
Dahong Yao, Jie Liu, Liang Ouyang
No abstract text is available yet for this article.
June 21, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28635317/beyond-the-wall-can-d-amino-acids-and-small-molecule-inhibitors-eliminate-infections
#6
Ilana Kolodkin-Gal
No abstract text is available yet for this article.
June 21, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28635308/combined-hqsar-topomer-comfa-homology-modeling-and-docking-studies-on-triazole-derivatives-as-sglt2-inhibitors
#7
Shuling Yu, Jintao Yuan, Yi Zhang, Shufang Gao, Ying Gan, Meng Han, Yuewen Chen, Qiaoqiao Zhou, Jiahua Shi
AIM: Sodium-glucose cotransporter 2 (SGLT2) is a promising target for diabetes therapy. We aimed to develop computational approaches to identify structural features for more potential SGLT2 inhibitors. MATERIALS & METHODS: In this work, 46 triazole derivatives as SGLT2 inhibitors were studied using a combination of several approaches, including hologram quantitative structure-activity relationships (HQSAR), topomer comparative molecular field analysis (CoMFA), homology modeling, and molecular docking...
June 21, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28635307/synthesis-evaluation-and-modeling-of-some-triazolothienopyrimidinones-as-anti-inflammatory-and-antimicrobial-agents
#8
Adnan A Bekhit, Ahmed M Farghaly, Ragab M Shafik, Mona Ma Elsemary, Mai S El-Shoukrofy, Alaa El-Din A Bekhit, Tamer M Ibrahim
AIM: New triazolotetrahydrobenzothienopyrimidinone derivatives were synthesized. EXPERIMENTAL: Their structures were confirmed, and their anti-inflammatory, antimicrobial activities and ulcerogenic potentials were evaluated. RESULTS: Compounds 7a, 10a and 11a showed minimal ulcerogenic effect and high selectivity toward human recombinant COX-2 over COX-1 enzyme with IC50 values of 1.39, 1.22 and 0.56 μM, respectively. Their docking outcome correlated with their biological activity and confirmed the high selectivity binding toward COX-2...
June 21, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28632451/prolyl-oligopeptidase-and-its-role-in-the-organism-attention-to-the-most-promising-and-clinically-relevant-inhibitors
#9
Katerina Babkova, Jan Korabecny, Ondrej Soukup, Eugenie Nepovimova, Daniel Jun, Kamil Kuca
Prolyl oligopeptidase (POP), also called prolyl endopeptidase, is a cytosolic enzyme investigated by several research groups. It has been proposed to play an important role in physiological processes such as modulation of the levels of several neuronal peptides and hormones containing a proline residue. Due to its proteolytic activity and physiological role in cell signaling pathways, inhibition of POP offers an emerging approach for the treatment of Alzheimer's and Parkinson's diseases as well as other diseases related to cognitive impairment...
June 20, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28632448/neuroregeneration-versus-neurodegeneration-toward-a-paradigm-shift-in-alzheimer-s-disease-drug-discovery
#10
Elisa Uliassi, Annachiara Gandini, Rosaria Carmela Perone, Maria Laura Bolognesi
Alzheimer's disease represents an enormous global burden in terms of human suffering and economic cost. To tackle the current lack of effective drugs and the continuous clinical trial failures might require a shift from the prevailing paradigm targeting pathogenesis to the one targeting neural stem cells (NSCs) regeneration. In this context, small molecules have come to the forefront for their potential to manipulate NSCs, provide therapeutic tools and unveil NSCs biology. Classically, these molecules have been generated either by target-based or phenotypic approaches...
June 20, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28632446/multitarget-drug-design-strategy-in-alzheimer-s-disease-focus-on-cholinergic-transmission-and-amyloid-%C3%AE-aggregation
#11
Elena Simoni, Manuela Bartolini, Izuddin F Abu, Alix Blockley, Cecilia Gotti, Giovanni Bottegoni, Roberta Caporaso, Christian Bergamini, Vincenza Andrisano, Andrea Cavalli, Ian R Mellor, Anna Minarini, Michela Rosini
AIM: Alzheimer pathogenesis has been associated with a network of processes working simultaneously and synergistically. Over time, much interest has been focused on cholinergic transmission and its mutual interconnections with other active players of the disease. Besides the cholinesterase mainstay, the multifaceted interplay between nicotinic receptors and amyloid is actually considered to have a central role in neuroprotection. Thus, the multitarget drug-design strategy has emerged as a chance to face the disease network...
June 20, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28632424/the-progress-in-the-research-of-antiplatelet-agents-1995-2017
#12
Oscar Benimana, Lulu Zhao, Yi Kong, Zhiyu Li, Zhouling Xie
Antiplatelet therapy displays a critical role in the treatment and prevention of antithrombotic disorders. Many new antiplatelet agents have been developed following the emergence of various clinical limitations of classical antiplatelet drugs. This review covers mainly the recent advances in the development of P2Y12 antagonists and GPIIb/IIIa antagonists. Meanwhile, it summarizes promising approaches to new platelet surface receptors such as prostanoid EP3 receptor, thromboxane A2 prostanoid receptor, protease-activated receptors, GPIb-IX-V receptor and P-selectin...
June 20, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28632420/medicinal-chemistry-advances-in-neurodegenerative-disease-therapy-part-2
#13
Rachel Coleby
No abstract text is available yet for this article.
June 20, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28632415/synthesis-and-biological-evaluation-of-tanshinone-iia-derivatives-as-novel-endothelial-protective-agents
#14
Xiaoling Bi, Kuojun Zhang, Long He, Biao Gao, Qinlan Gu, Xueyan Li, Jun Chen, Jinxin Wang
AIM: Oxidative stress-induced endothelial injury is a main risk factor in the pathogenesis of cardiovascular diseases. Tanshinone IIA (Tan IIA) exerts protective functions on endothelial cells in response to oxidative stress. To exploit new bioactive compounds from this natural product, 12 derivatives were first synthesized and evaluated for endothelial protective activities. MATERIALS & METHODS: Title compounds were prepared according to high-yielded synthetic routes, and their protective effects on human endothelial EA...
June 20, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28632413/%C3%AE-synuclein-aggregation-modulation-an-emerging-approach-for-the-treatment-of-parkinson-s-disease
#15
Sushil K Singh, Aloke Dutta, Gyan Modi
Parkinson's disease (PD) is a multifactorial progressive neurological disorder. Pathological hallmarks of PD are characterized by the presence of α-synuclein (αSyn) aggregates known as Lewy bodies. αSyn aggregation is one of the leading causes for the neuronal dysfunction and death in PD. It is also associated with neurotransmitter and calcium release. Current therapies of PD are limited to only symptomatic relief without addressing the underlying pathogenic factors of the disease process such as aggregation of αSyn...
June 20, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28632406/tailored-pharmacophore-model-to-enhance-virtual-screening-and-drug-discovery-a-case-study-on-the-identification-of-potential-inhibitors-against-drug-resistant-mycobacterium-tuberculosis-3r-hydroxyacyl-acp-dehydratases
#16
Kgothatso E Machaba, Ndumiso N Mhlongo, Yussif M Dokurugu, Mahmoud Es Soliman
AIM: Virtual screening (VS) is powerful tool in discovering molecular inhibitors that are most likely to bind to drug targets of interest. Herein, we introduce a novel VS approach, so-called 'tailored-pharmacophore', in order to explore inhibitors that overcome drug resistance. Methodology & results: The emergence and spread of drug resistance strains of tuberculosis is one of the most critical issues in healthcare. A tailored-pharmacophore approach was found promising to identify in silico predicted hit with better binding affinities in case of the resistance mutations in MtbHadAB as compared with thiacetazone, a prodrug used in the clinical treatment of tuberculosis...
June 20, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28632402/3-benzyloxy-1-5-18-f-fluoropentyl-5-nitro-1h-indazole-a-pet-radiotracer-to-measure-acetylcholinesterase-in-brain
#17
Soledad Fernández, Javier Giglio, Ana Laura Reyes, Andrés Damián, Concepción Pérez, Daniel I Pérez, Mercedes González, Patricia Oliver, Ana Rey, Henry Engler, Hugo Cerecetto
AIM: Noninvasive studies of the acetylcholinesterase (AChE) level in Alzheimer's disease (AD) patients can contribute to a better understanding of the disease and its therapeutic. We propose 3-(benzyloxy)-1-(5-[(18)F]fluoropentyl)-5-nitro-1H-indazole, [(18)F]-IND1, structurally related to the AChE-inhibitor CP126,998, as a new positron emission tomography-radiotracer. EXPERIMENTAL: Radiosynthesis, with 18F, stability, lipophilicity and protein binding of [18F]-IND1 were studied...
June 20, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28632395/design-synthesis-and-multitarget-biological-profiling-of-second-generation-anti-alzheimer-rhein-huprine-hybrids
#18
Francisco Javier Pérez-Areales, Nibal Betari, Antonio Viayna, Caterina Pont, Alba Espargaró, Manuela Bartolini, Angela De Simone, José Fernando Rinaldi Alvarenga, Belén Pérez, Raimon Sabate, Rosa Maria Lamuela-Raventós, Vincenza Andrisano, Francisco Javier Luque, Diego Muñoz-Torrero
AIM: Simultaneous modulation of several key targets of the pathological network of Alzheimer's disease (AD) is being increasingly pursued as a promising option to fill the critical gap of efficacious drugs against this condition. MATERIALS & METHODS: A short series of compounds purported to hit multiple targets of relevance in AD has been designed, on the basis of their distinct basicities estimated from high-level quantum mechanical computations, synthesized, and subjected to assays of inhibition of cholinesterases, BACE-1, and Aβ42 and tau aggregation, of antioxidant activity, and of brain permeation...
June 20, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28513196/synthesis-and-in-vivo-antimalarial-activity-of-novel-naphthoquine-derivatives-with-linear-cyclic-structured-pendants
#19
Ling Tang, Zhuchun Bei, Yabin Song, Likun Xu, Hong Wang, Dongna Zhang, Yuanyuan Dou, Kai Lv, Hongquan Wang
AIM: Naphthoquine (NQ) was discovered by our institute as an antimalarial candidate in 1980s, and currently employed as an artemisinin-based combination therapy partner drug. Resistance to NQ was found in mouse model in laboratory, and might emerge in future as widely used. METHODOLOGY: We herein report the design and synthesis of NQ derivatives by replacing t-butyl moiety with linear/cyclic structured pendants. All the target compounds 6a-l and intermediates 5a-h were tested for their in vivo antimalarial activity against Plasmodium berghei K173 strain in mice...
May 17, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28504914/g-protein-coupled-receptor-based-drugs-rediscovered
#20
Kenneth Lundstrom
No abstract text is available yet for this article.
May 15, 2017: Future Medicinal Chemistry
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