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Nagarjuna Reddy K, Subhadra U, Sridhar B, Subba Reddy B V
A novel one-pot strategy has been developed for the construction of spiro-isoindolinone-benzosultams through a Ru(ii)-catalyzed sequential C-C and C-N bond formation. This method is highly atom-economical and compatible with a wide range of substituents. This is the first report on the spirocyclization of 3-aryl N-sulfonyl ketimines with aryl isocyanates to produce highly rigid and pharmaceutically relevant spirocycles through a C-H bond activation.
March 22, 2018: Organic & Biomolecular Chemistry
Jing Tao, Yu-Qin Zhao, Chang-Feng Chi, Bin Wang
In the experiment, crude proteins from spotless smoothhound ( Mustelus griseus ), cartilages were isolated by HCl-Guanidine buffer, and its hydrolysate was prepared using trypsin at pH 8.0, 40 °C with a total enzyme dose of 2.5%. Subsequently, three antioxidant peptides were purified from the hydrolysate using membrane ultrafiltration, anion-exchange chromatography, gel filtration chromatography, and reverse phase high-performance liquid chromatography. The amino acid sequences of isolated peptides were identified as Gly-Ala-Glu-Arg-Pro (MCPE-A); Gly-Glu-Arg-Glu-Ala-Asn-Val-Met (MCPE-B); and Ala-Glu-Val-Gly (MCPE-C) with molecular weights of 528...
March 22, 2018: Marine Drugs
Mostefa Lefahal, Nabila Zaabat, Radia Ayad, El Hani Makhloufi, Lakhdar Djarri, Merzoug Benahmed, Hocine Laouer, Gema Nieto, Salah Akkal
Background: Capnophyllum peregrinum (L.) Lange (Apiaceae) is the unique taxon of capnophyllum genus in Algerian flora. It has never been investigated in regards to its total phenolic and flavonoid contents and antioxidant and photoprotective activities. Methods: C. peregrinum aerial parts extracted with absolute methanol. The total flavonoid and phenolic contents of the extract were evaluated to determine their correlation with the antioxidant and photoprotective activities of the extract. Results: The methanolic extract demonstrated a significant amount of phenolics and flavonoids (74...
March 22, 2018: Medicines (Basel, Switzerland)
Xiaobin Mo, Timothy D R Morgan, Hwee Ting Ang, Dennis G Hall
Catalytic activation of hydroxyl functionalities is of great interest for the production of pharmaceuticals and commodity chemicals. Here, 2-alkoxycarbonyl- and 2-phenoxycarbonyl-phenylboronic acid were identified as efficient catalysts for the direct and chemoselective activation of oxime N-OH bonds in the Beckmann rearrangement. This classical organic reaction provides a unique approach to prepare functionalized amide products that may be difficult to access using traditional amide coupling between carboxylic acids and amines...
March 22, 2018: Journal of the American Chemical Society
Mayura Kale, Gajanan Sonwane, Rajesh Nawale, Vishnukant Mourya
There has been a rapid surge in the research and exchange of ideas in various areas of chemistry such as organic, pharmaceutical, analytical, and medicinal chemistry. It is well recognized that heterocycles are vital components of many biochemical processes. Pharma industry comprises of more than 75% of top selling drugs that are of heterocyclic origin. Among many diseases, cancer can be considered to be a dreaded disease that has overtaken the masses across the globe. Hence, there has been a need to develop drugs that are less toxic and do not provide resistance in the long run...
March 20, 2018: Current Computer-aided Drug Design
Andrew M Hill, Melissa J Barber, Dzintars Gotham
Introduction: There are persistent gaps in access to affordable medicines. The WHO Model List of Essential Medicines (EML) includes medicines considered necessary for functional health systems. Methods: A generic price estimation formula was developed by reviewing published analyses of cost of production for medicines and assuming manufacture in India, which included costs of formulation, packaging, taxation and a 10% profit margin. Data on per-kilogram prices of active pharmaceutical ingredient exported from India were retrieved from an online database...
2018: BMJ Global Health
Joel Lexchin
Background: Competing claims are made about the amount of money that pharmaceutical companies spend on research and development (R&D) versus promotion. This study investigates this question in the Canadian context. Methods: Two methods for determining industry-wide figures for spending on promotion were employed. First, total industry spending on detailing and journal advertising for 2013-2016 was abstracted from reports from QuintilesIMS. Second, the mean total promotion spending for the years 2002-2005 was used to estimate total spending for 2013-2016...
2018: Journal of Pharmaceutical Policy and Practice
Hayden B Bosworth, Barbara Ngouyombo, Jan Liska, Leah L Zullig, Caroline Atlani, Anne C Beal
Lipid-lowering medications have been shown to be efficacious, but adherence is suboptimal. This is a narrative, perspective review of recently published literature in the field of medication adherence research for lipid-lowering medications. We provide an overview of the impact of suboptimal adherence and use a World Health Organization framework (patient, condition, therapy, socioeconomic, and health system-related systems) to discuss factors that influence hyperlipidemia treatment adherence. Further, the review involves an evaluation of intervention strategies to increase hyperlipidemia treatment adherence with a special focus on mHealth interventions, patient reminders on packaging labels, nurse- and pharmacist-led interventions, and health teams...
2018: Patient Preference and Adherence
Chang Xu, Wen-Hao Guo, Xu He, Yin-Long Guo, Xue-Ying Zhang, Xingang Zhang
Relatively low reactivity hinders using chlorodifluoromethane (ClCF2 H) for general difluoromethylation with organic molecules, despite its availability as an inexpensive industrial chemical. To date, transformations of ClCF2 H are very limited and most of them involve difluorocarbene intermediate. Here, we describe a strategy for difluoromethylation of aromatics through nickel-catalyzed cross-coupling of ClCF2 H with readily accessible (hetero)aryl chlorides. The reaction proceeds under mild reaction conditions with high efficiency and features synthetic simplicity without preformation of arylmetals and broad substrate scope, including a variety of heteroaromatics and commercially available pharmaceuticals...
March 21, 2018: Nature Communications
Giovanni E Lombardo, Valentina Maggisano, Marilena Celano, Donato Cosco, Chiara Mignogna, Federica Baldan, Saverio M Lepore, Lorenzo Allegri, Sonia Moretti, Cosimo Durante, Giuseppe Damante, Massimo Fresta, Diego Russo, Stefania Bulotta, Efisio Puxeddu
The high frequency of hTERT-promoting mutations and the increased expression of hTERT mRNA in anaplastic thyroid cancer (ATC) make TERT a suitable molecular target for the treatment of this lethal neoplasm. In this study, we encapsulated an anti-hTERT oligonucleotide in biocompatible nanoparticles and analyzed the effects of this novel pharmaceutical preparation in preclinical models of ATC. Biocompatible nanoparticles were obtained in an acidified aqueous solution containing chitosan, anti-hTERT oligoRNAs and poloxamer 188 as a stabilizer...
March 21, 2018: Molecular Cancer Therapeutics
Maureen Mackintosh, Julius Mugwagwa, Geoffrey Banda, Paula Tibandebage, Jires Tunguhole, Samuel Wangwe, Mercy Karimi Njeru
The benefits of local production of pharmaceuticals in Africa for local access to medicines and to effective treatment remain contested. There is scepticism among health systems experts internationally that production of pharmaceuticals in sub-Saharan Africa (SSA) can provide competitive prices, quality and reliability of supply. Meanwhile low-income African populations continue to suffer poor access to a broad range of medicines, despite major international funding efforts. A current wave of pharmaceutical industry investment in SSA is associated with active African government promotion of pharmaceuticals as a key sector in industrialization strategies...
March 19, 2018: Health Policy and Planning
Mark Sherman, Lydia Contreras
Recent advances in computational and experimental methods have led to novel avenues for therapeutic development. Utilization of nucleic acids as therapeutic agents and/or targets has been recently gaining attention due to their potential as high-affinity, selective molecular building blocks for various therapies. Notably, development of computational algorithms for predicting accessible RNA binding sites, identifying therapeutic target sequences, modeling delivery into tissues, and designing binding aptamers have enhanced therapeutic potential for this new drug category...
March 18, 2018: Current Opinion in Biotechnology
Noura S Abul-Husn, Xiping Cheng, Alexander H Li, Yurong Xin, Claudia Schurmann, Panayiotis Stevis, Yashu Liu, Julia Kozlitina, Stefan Stender, G Craig Wood, Ann N Stepanchick, Matthew D Still, Shane McCarthy, Colm O'Dushlaine, Jonathan S Packer, Suganthi Balasubramanian, Nehal Gosalia, David Esopi, Sun Y Kim, Semanti Mukherjee, Alexander E Lopez, Erin D Fuller, John Penn, Xin Chu, Jonathan Z Luo, Uyenlinh L Mirshahi, David J Carey, Christopher D Still, Michael D Feldman, Aeron Small, Scott M Damrauer, Daniel J Rader, Brian Zambrowicz, William Olson, Andrew J Murphy, Ingrid B Borecki, Alan R Shuldiner, Jeffrey G Reid, John D Overton, George D Yancopoulos, Helen H Hobbs, Jonathan C Cohen, Omri Gottesman, Tanya M Teslovich, Aris Baras, Tooraj Mirshahi, Jesper Gromada, Frederick E Dewey
BACKGROUND: Elucidation of the genetic factors underlying chronic liver disease may reveal new therapeutic targets. METHODS: We used exome sequence data and electronic health records from 46,544 participants in the DiscovEHR human genetics study to identify genetic variants associated with serum levels of alanine aminotransferase (ALT) and aspartate aminotransferase (AST). Variants that were replicated in three additional cohorts (12,527 persons) were evaluated for association with clinical diagnoses of chronic liver disease in DiscovEHR study participants and two independent cohorts (total of 37,173 persons) and with histopathological severity of liver disease in 2391 human liver samples...
March 22, 2018: New England Journal of Medicine
Robert J Motzer, Nizar M Tannir, David F McDermott, Osvaldo Arén Frontera, Bohuslav Melichar, Toni K Choueiri, Elizabeth R Plimack, Philippe Barthélémy, Camillo Porta, Saby George, Thomas Powles, Frede Donskov, Victoria Neiman, Christian K Kollmannsberger, Pamela Salman, Howard Gurney, Robert Hawkins, Alain Ravaud, Marc-Oliver Grimm, Sergio Bracarda, Carlos H Barrios, Yoshihiko Tomita, Daniel Castellano, Brian I Rini, Allen C Chen, Sabeen Mekan, M Brent McHenry, Megan Wind-Rotolo, Justin Doan, Padmanee Sharma, Hans J Hammers, Bernard Escudier
Background Nivolumab plus ipilimumab produced objective responses in patients with advanced renal-cell carcinoma in a pilot study. This phase 3 trial compared nivolumab plus ipilimumab with sunitinib for previously untreated clear-cell advanced renal-cell carcinoma. Methods We randomly assigned adults in a 1:1 ratio to receive either nivolumab (3 mg per kilogram of body weight) plus ipilimumab (1 mg per kilogram) intravenously every 3 weeks for four doses, followed by nivolumab (3 mg per kilogram) every 2 weeks, or sunitinib (50 mg) orally once daily for 4 weeks (6-week cycle)...
March 21, 2018: New England Journal of Medicine
Aurelia Vasile, Maria Ignat, Mirela Fernanda Zaltariov, Liviu Sacarescu, Iulian Stoleriu, Dan Draganescu, Mihai Dumitras, Lacramioara Ochiuz
The present study reports the first time use of MCM-41 mesoporous silica as highly efficient carrier for bexarotene - an antineoplastic agent specific for cutaneous T-cell lymphoma treatment. Bexarotene is highly toxic and poor-water soluble, having low bioavailability in the conventional pharmaceutical forms. Comparative uptake of bexarotene on amino-functionalized silica host at various functionalization degrees is discussed in details taking into account all structural features, of matrix as well as properties of the drug molecules...
March 2018: Acta Chimica Slovenica
Mohamed Ezzat Khalifa
Aminothiazole nuclei and their various derivatives have been long used as precursors for the synthesis of biologically active molecules. As a typical heterocyclic amine, 2-aminothiazole is a cornerstone for the synthesis of many compounds, including sulfur drugs, biocides, fungicides, various types of dyes for synthetic fibers and chemical reaction accelerators and as intermediates in the synthesis of antibiotics, where a large number of 2-aminothiazoles have been substituted with different groups for various pharmaceutical purposes, besides their activity as corrosion inhibitors for mild steel protection as well...
March 2018: Acta Chimica Slovenica
Panteleimon D Mavroudis, Helen E Hermes, Donato Teutonico, Thomas G Preuss, Sebastian Schneckener
The environmental fates of pharmaceuticals and the effects of crop protection products on non-target species are subjects that are undergoing intense review. Since measuring the concentrations and effects of xenobiotics on all affected species under all conceivable scenarios is not feasible, standard laboratory animals such as rabbits are tested, and the observed adverse effects are translated to focal species for environmental risk assessments. In that respect, mathematical modelling is becoming increasingly important for evaluating the consequences of pesticides in untested scenarios...
2018: PloS One
Kate S Collison, Angela Inglis, Sherin Shibin, Soad Saleh, Bernard Andres, Rosario Ubungen, Jennifer Thiam, Princess Mata, Futwan A Al-Mohanna
RATIONALE: Aspartame (L-aspartyl phenylalanine methyl ester) is a non-nutritive sweetener (NNS) approved for use in more than 6000 dietary products and pharmaceuticals consumed by the general public including adults and children, pregnant and nursing mothers. However a recent prospective study reported a doubling of the risk of being overweight amongst 1-year old children whose mothers consumed NNS-sweetened beverages daily during pregnancy. We have previously shown that chronic aspartame (ASP) exposure commencing in utero may detrimentally affect adulthood adiposity status, glucose metabolism and aspects of behavior and spatial cognition, and that this can be modulated by developmental N-methyl-D-aspartate receptor (NMDAR) blockade with the competitive antagonist CGP 39551 (CGP)...
2018: PloS One
Chrysovalantis Voutouri, Triantafyllos Stylianopoulos
Hyaluronan is abundant in the extracellular matrix of many desmoplastic tumors and determines in large part the tumor biochemical and mechanical microenvironment. Additionally, it has been identified as one of the major physiological barriers to the effective delivery of drugs to solid tumors and its targeting with the use of pharmaceutical agents has shown to decompress tumor blood vessels, and thus improve tumor perfusion and efficacy of cytotoxic drugs. In this study, we investigated the contribution of hyaluronan to the accumulation of mechanical forces in tumors...
2018: PloS One
Beatrice Xuan Ho, Nicole Min Qian Pek, Boon-Seng Soh
The rising interest in human induced pluripotent stem cell (hiPSC)-derived organoid culture has stemmed from the manipulation of various combinations of directed multi-lineage differentiation and morphogenetic processes that mimic organogenesis. Organoids are three-dimensional (3D) structures that are comprised of multiple cell types, self-organized to recapitulate embryonic and tissue development in vitro. This model has been shown to be superior to conventional two-dimensional (2D) cell culture methods in mirroring functionality, architecture, and geometric features of tissues seen in vivo...
March 21, 2018: International Journal of Molecular Sciences
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