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https://www.readbyqxmd.com/read/29793211/synthesis-and-evaluation-of-novel-triazolyl-quinoline-derivatives-as-potential-antileishmanial-agents
#1
Akanksha Upadhyay, Pragati Kushwaha, Sampa Gupta, Ranga Prasad Dodda, Karthik Ramalingam, Ruchir Kant, Neena Goyal, Koneni V Sashidhara
The high potential of quinoline containing natural products and their derivatives in medicinal chemistry led us to discover novel series of 25 compounds for the development of new antileishmanial agents. A series of triazolyl 2-methyl-4-phenylquinoline-3-carboxylate derivatives has been synthesized via click chemistry inspired molecular hybridization approach and evaluated against Leishmania donovani. Most of the screened derivatives exhibited significant in vitro anti-leishmanial activity against promastigote (IC50 ranging from 2...
May 12, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29793128/convolutional-neural-networks-for-seizure-prediction-using-intracranial-and-scalp-electroencephalogram
#2
Nhan Duy Truong, Anh Duy Nguyen, Levin Kuhlmann, Mohammad Reza Bonyadi, Jiawei Yang, Samuel Ippolito, Omid Kavehei
Seizure prediction has attracted growing attention as one of the most challenging predictive data analysis efforts to improve the life of patients with drug-resistant epilepsy and tonic seizures. Many outstanding studies have reported great results in providing sensible indirect (warning systems) or direct (interactive neural stimulation) control over refractory seizures, some of which achieved high performance. However, to achieve high sensitivity and a low false prediction rate, many of these studies relied on handcraft feature extraction and/or tailored feature extraction, which is performed for each patient independently...
May 7, 2018: Neural Networks: the Official Journal of the International Neural Network Society
https://www.readbyqxmd.com/read/29793051/promising-antileishmanial-activity-of-novel-imidazole-antifungal-drug-luliconazole-against-leishmania-major-in-vitro-and-in-silico-studies
#3
Azar Shokri, Mahdi Abastabar, Masoud Keighobadi, Saeed Emami, Mahdi Fakhar, Saeed Hosseini Teshnizi, Koichi Makimura, Ali Rezaei-Matehkolaei, Hassan Mirzaei
OBJECTIVES: Pentavalent antimonials have been used for the treatment of leishmaniasis for more than 70 years; however their toxicity limits their benefits. Unfortunately, the efficacy of the first line drugs has been decreased and resistance seems to be noticeable. Luliconazole is a new azole with unique effects on fungi which has not been tested on Leishmania parasites yet. METHODS: In the present study, we evaluated cytotoxicity and anti-leishmanial activities of Luliconazole on promastigotes and intracellular amastigotes of Leishmania major (L...
May 21, 2018: Journal of Global Antimicrobial Resistance
https://www.readbyqxmd.com/read/29792985/novel-excipients-regulatory-challenges-and-perspectives-the-eu-insight
#4
Piotr Kozarewicz, Thorsteinn Loftsson
Novel excipients are indispensable in development of modern, advanced drug delivery systems and biotechnology-derived drugs. Although numerous novel excipients are developed for pharmaceutical use, they are not frequently seen in medicinal products due to the strict regulatory requirements and perception that their use makes new product evaluation more complex with risk of delays in the approval process. Regulators regard novel excipients as new substances and whenever new excipient is used in a formulation it must be subjected to full evaluation, similarly to the one required for new active substance...
May 21, 2018: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29792851/collagen-induced-arthritis-in-dark-agouti-rats-as-a-model-for-study-of-immunological-sexual-dimorphisms-in-the-human-disease
#5
Mirjana Dimitrijević, Nevena Arsenović-Ranin, Biljana Bufan, Mirjana Nacka-Aleksić, Mirjana Lazarević Macanović, Petar Milovanović, Marija Đurić, Jelena Sopta, Gordana Leposavić
Collagen-induced arthritis (CIA) is a frequently used animal model of rheumatoid arthritis, human autoimmune disease that exhibits clear sex bias in incidence and clinical course. Female Dark Agouti rats immunized for CIA showed also greater incidence and higher arthritic score than their male counterparts. The study investigated sex differences in mechanisms controlling the primary immune responses in draining lymph nodes (dLNs), as a factor contributing to this dimorphism. The higher frequencies of CD4 + CD25 + Foxp3- cells, presumably activated effector T (Teff) cells, and IL-17+, IFN-γ + and IL-17 + IFN-γ + T cells were found in female comapared with male rat dLNs...
May 21, 2018: Experimental and Molecular Pathology
https://www.readbyqxmd.com/read/29792845/current-frontline-endocrine-treatment-options-for-women-with-hormone-receptor-positive-human-epidermal-growth-factor-receptor-2-her2-negative-advanced-stage-breast-cancer
#6
REVIEW
Hikmat N Abdel-Razeq
Despite the recent advances in breast cancer early detection and awareness, a significant portion of patients present with an advanced-stage disease and more patients will progress to stage IV despite adequate treatment of their initial early-stage disease. Hormone receptor (HR)-positive, Human Epidermal Growth Factor Receptor-2 (HER2)-negative subtype is the commonest among all breast cancer subtypes. The management of the advanced-stage disease of this subtype has evolved significantly over the past few years...
May 19, 2018: Hematology/oncology and Stem Cell Therapy
https://www.readbyqxmd.com/read/29792805/a-cheminformatic-insight-into-the-differences-between-terrestrial-and-marine-originated-natural-products
#7
Jun Shang, Ben Hu, Junmei Wang, Feng Zhu, Yu Kang, Dan Li, Huiyong Sun, De-Xin Kong, Tingjun Hou
This is a new golden age for the drug discovery based on natural products derived from both marine and terrestrial sources. Herein, a straightforward but important question is what are the major structural differences between marine natural products (MNPs) and terrestrial natural products (TNPs). To answer this question, we analyzed the important physicochemical properties, structural features and drug-likeness of the two types of natural products and discussed their differences from the perceptive of evolution...
May 24, 2018: Journal of Chemical Information and Modeling
https://www.readbyqxmd.com/read/29792734/clinical-updates-on-perianal-fistulas-in-crohn-s-disease
#8
Ori Rackovsky, Robert Hirten, Ryan Ungaro, Jean-Frederic Colombel
Perianal fistulizing disease is an aggressive and debilitating phenotype of Crohn's disease (CD), representing a significant therapeutic challenge. New work has led to advancement in epidemiology and long term outcomes of perianal disease. The range of therapeutic options continues to expand, including new biologic agents, biosimilars, and stem cell therapy. Areas covered: We discuss updates to all aspects of management of perianal disease, with a focus on the last three years of published data. Areas considered include new data on epidemiology and prognostication, medical and surgical therapy, and stem cell therapy...
May 24, 2018: Expert Review of Gastroenterology & Hepatology
https://www.readbyqxmd.com/read/29792714/docking-screens-for-dual-inhibitors-of-disparate-drug-targets-for-parkinson-s-disease
#9
Mariama Jaiteh, Alexey Zeifman, Marcus Saarinen, Per Svenningsson, José M Brea, Maria Isabel Loza, Jens Carlsson
Modulation of multiple biological targets with a single drug can lead to synergistic therapeutic effects and has been demonstrated to be essential for efficient treatment of CNS disorders. However, rational design of compounds that interact with several targets is very challenging. Here, we demonstrate that structure-based virtual screening can guide the discovery of multi-target ligands of unrelated proteins relevant for Parkinson's disease. A library with 5.4 million molecules was docked to crystal structures of the A2A adenosine receptor (A2AAR) and monoamine oxidase B (MAO-B)...
May 24, 2018: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29792353/gastroretentive-raft-liquid-delivery-system-as-a-new-approach-to-release-extension-for-carrier-mediated-drug
#10
Samar M Abouelatta, Ahmed A Aboelwafa, Omaima N El-Gazayerly
Gabapentin (GBP), an antiepileptic and anti-neuropathic agent, suffers from short half-life (5-7 h), has narrow absorption window, and is absorbed via carrier-mediated mechanism resulting in frequent dosing, poor compliance, and poor bioavailability (<60%). Moreover, GBP is a freely water-soluble drug, thus it is considered a challenging candidate to be formulated as extended release dosage form. In this study, raft forming systems were investigated as a potential drug delivery system for prolonging gastric residence time of GBP...
November 2018: Drug Delivery
https://www.readbyqxmd.com/read/29792346/synthesis-of-novel-camphene-based-thiosemicarbazones-and-evaluation-of-anti-mycobacterium-tuberculosis-activity
#11
Mariana R P Souza, Narcimário P Coelho, Vanessa P Baldin, Regiane B L Scodro, Rosilene F Cardoso, Cleuza C da Silva, Fábio Vandresen
In this work the aim of study was the synthesis and evaluation of in vitro anti-Mycobacterium tuberculosis activity as well as the cytotoxicity in VERO cells of a series of 17 novel thiosemicarbazones derived from the natural monoterpene (-)-camphene by REMA and MTT methods. Overall, the majority of tested compounds exhibited considerable inhibitory effects on the growth of M. tuberculosis H37 Rv, especially the derivatives 3, 4a-c, 4f, 4i, 4k, 5 and 6a-b. MIC values of 20 tested compounds ranged from 3.9 to > 250 μg/mL...
May 24, 2018: Natural Product Research
https://www.readbyqxmd.com/read/29792329/residual-complexity-does-impact-organic-chemistry-and-drug-discovery-the-case-of-rufomyazine-and-rufomycin
#12
Mary P Choules, Larry L Klein, David C Lankin, James B McAlpine, Sang-Hyun Cho, Jinhua Cheng, Hanki Lee, Joo-Won Suh, Birgit U Jaki, Scott G Franzblau, Guido F Pauli
Residual complexity (RC) involves the impact of subtle but critical structural and biological features on drug lead validation, including unexplained effects related to unidentified impurities. RC commonly plagues drug discovery efforts due to the inherent imperfections of chromatographic separation methods. The new diketopiperazine, rufomyazine (6), and the previously known antibiotic, rufomycin (7), represent a prototypical case of RC that (almost) resulted in the misassignment of biological activity. The case exemplifies that impurities well below the natural abundance of 13 C (1...
May 24, 2018: Journal of Organic Chemistry
https://www.readbyqxmd.com/read/29792307/putative-vaccine-candidates-and-drug-targets-identified-by-reverse-vaccinology-and-subtractive-genomics-approaches-to-control-haemophilus-ducreyi-the-causative-agent-of-chancroid
#13
Alissa de Sarom, Arun Kumar Jaiswal, Sandeep Tiwari, Letícia de Castro Oliveira, Debmalya Barh, Vasco Azevedo, Carlo Jose Oliveira, Siomar de Castro Soares
Chancroid is a sexually transmitted infection (STI) caused by the Gram-negative bacterium Haemophilus ducreyi The control of chancroid is difficult and the only current available treatment is antibiotic therapy; however, antibiotic resistance has been reported in endemic areas. Owing to recent outbreaks of STIs worldwide, it is important to keep searching for new treatment strategies and preventive measures. Here, we applied reverse vaccinology and subtractive genomic approaches for the in silico prediction of potential vaccine and drug targets against 28 strains of H...
May 2018: Journal of the Royal Society, Interface
https://www.readbyqxmd.com/read/29792227/integrated-time-course-omics-analysis-distinguishes-immediate-therapeutic-response-from-acquired-resistance
#14
Genevieve Stein-O'Brien, Luciane T Kagohara, Sijia Li, Manjusha Thakar, Ruchira Ranaweera, Hiroyuki Ozawa, Haixia Cheng, Michael Considine, Sandra Schmitz, Alexander V Favorov, Ludmila V Danilova, Joseph A Califano, Evgeny Izumchenko, Daria A Gaykalova, Christine H Chung, Elana J Fertig
BACKGROUND: Targeted therapies specifically act by blocking the activity of proteins that are encoded by genes critical for tumorigenesis. However, most cancers acquire resistance and long-term disease remission is rarely observed. Understanding the time course of molecular changes responsible for the development of acquired resistance could enable optimization of patients' treatment options. Clinically, acquired therapeutic resistance can only be studied at a single time point in resistant tumors...
May 23, 2018: Genome Medicine
https://www.readbyqxmd.com/read/29792196/ethnozoological-study-of-traditional-medicinal-appreciation-of-animals-and-their-products-among-the-indigenous-people-of-metema-woreda-north-western-ethiopia
#15
Fasil Adugna Kendie, Sileshi Andualem Mekuriaw, Melkamu Andargie Dagnew
BACKGROUND: Using animals for different purposes goes back to the dawn of mankind. Animals served as a source of food, medicine, and clothing for humans and provided other services. This study was designed to undertake a cross-sectional ethnozoological field survey among the residents of Metema Woreda from November 2015 to May 2016. METHODS: Data were collected through studied questionnaires, interviews, and focus group discussions with 36 purposively selected respondents...
May 23, 2018: Journal of Ethnobiology and Ethnomedicine
https://www.readbyqxmd.com/read/29792154/exploration-of-hetero-aryl-derived-thienylchalcones-for-antiviral-and-anticancer-activities
#16
Vikrant Patil, Siddappa A Patil, Renukadevi Patil, Alejandro Bugarin, Kenneth Beaman, Shivaputra A Patil
BACKGROUND: Search for new antiviral and anticancer agents are essential because of the emergence of drug resistance in recent years. In continuation of our efforts in identifying the new small molecule antiviral and anticancer agents, we identified chalcones as potent antiviral and anticancer agents. OBJECTIVE: With the aim of identifying the broad acting antiviral and anticancer agents, we discovered substituted aryl/heteroaryl derived thienyl chalcones as antiviral and anticancer agents...
May 23, 2018: Medicinal Chemistry
https://www.readbyqxmd.com/read/29792151/pyrazole-and-imidazo-1-2-b-pyrazole-derivatives-as-new-potential-anti-tuberculosis-agents
#17
Elda Meta, Chiara Brullo, Michele Tonelli, Scott G Franzblau, Yuehong Wang, Rui Ma, Wan Baojie, Beatrice Silvia Orena, Maria Rosalia Pasca, Olga Bruno
BACKGROUND: We screened a large library of differently decorated imidazo-pyrazole and pyrazole derivatives as possible new antitubercular agents and this preliminary screening showed that many compounds are able to totally inhibit Mycobacterium growth (>90 %). Among the most active compounds, we selected some new possible hits based on their similarities and, at the same time, their novelty respect to the pipeline drugs. METHODS: In order to increase the potency and obtain more information about structure activity relationship (SAR), we design and synthesized three new series of compounds (2a-e, 3a-e, and 4a-l)...
May 23, 2018: Medicinal Chemistry
https://www.readbyqxmd.com/read/29792145/1-2-4-oxadiazole-as-a-privileged-scaffold-for-anti-inflammatory-and-analgesic-activities-a-complete-review
#18
Gita Chawla, Chanda Ranjan, Anees A Siddiqui
1,2,4-Oxadiazole is one of the important heterocycles used by medicinal chemists in designing a new therapeutic molecule. The compounds containing this nucleus are reported to have a wide range of pharmaceutical and biological applications including anti-inflammatory and analgesic activities. The fused and pendent 1,2,4-oxadiazole moiety has been traced in a number of well established, commercially available drugs. This review article provides an up to date information about techniques adopted for the synthesis of 1,2,4-oxadiazoles, and their therapeutic importance as an anti-inflammatory and analgesic agents...
May 23, 2018: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/29792142/collaboration-of-the-joint-research-centre-and-the-european-customs-laboratories-for-identification-of-new-psychoactive-substances
#19
Claude Guillou, Fabiano Reniero, Joana Lobo Pereira Vicente, Margaret Holland, Kamil Kolar, Hubert Chassaigne, Salvatore Tirendi, Herve Schepers
The emergence of designer drugs as substances of abuse has seen a dramatic increase over the last few years. Customs officials are responsible for the control of products entering the European Union (EU) market. This control applies to chemicals in general, pharmaceutical products and medicines. Numerous products imported from non-EU countries, often -declared as 'bath salts' or 'fertilizers', may in fact contain new psychoactive substance (NPS). These are not necessarily controlled under international law, but are subject to monitoring in agreement with EU legislation...
May 23, 2018: Current Pharmaceutical Biotechnology
https://www.readbyqxmd.com/read/29792137/recent-trends-in-nanocrystals-for-pharmaceutical-applications
#20
Leming Sun, Yanzi Hu, Lianbing Zhang
BACKGROUND: As the quick development of modern methods and technologies currently, more and more drugs have been invented with a better efficiency. However, the poor water solubility has limited the drugs' pharmaceutical application. METHODS: Tremendous research has been put in the design and development of nanocrystals for pharmaceutical applications over the past few decades. The nanocrystals not only have the chance to solve the poor solubility problem, but also could conquer the bioavailability and even the specific delivery problems...
May 23, 2018: Current Pharmaceutical Design
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