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Pharmaceutical chemistry

Kaiheng Guo, Zihao Wu, Chii Shang, Bo Yao, Shaodong Hou, Xin Yang, Weihua Song, Jingyun Fang
The UV/chlorine process is an emerging advanced oxidation process (AOP) used for the degradation of micropollutants. However, the radical chemistry of this AOP is largely unknown for the degradation of numerous structurally diverse micropollutants in water matrices of varying quality. These issues were addressed by grouping 34 pharmaceuticals and personal care products (PPCPs) according to the radical chemistry of their degradation in the UV/chlorine process at practical PPCP concentrations (1 μg L-1) and in different water matrices...
August 15, 2017: Environmental Science & Technology
Chengwei Liu, Michal Szostak
Considering the ubiquity of organophosphorus compounds in organic synthesis, pharmaceutical discovery agrochemical crop protection and materials chemistry, new methods for their construction hold particular significance. A conventional method for the synthesis of C-P bonds involves cross-coupling of aryl halides and dialkyl phosphites (the Hirao reaction). We report a catalytic deamidative phosphorylation of a wide range of amides using a palladium or nickel catalyst giving aryl phosphonates in good to excellent yields...
August 14, 2017: Angewandte Chemie
Ning Jiao, Xinwei Li, Fengguirong Lin, Kaimeng Huang, Jialiang Wei, Xinyao Li, Xiaoyang Wang, Xiaoyu Geng
Compared to the α-functionalization of aldehydes, ketones, even esters, the direct α-modification of amides is still a big challenge because of the lowest α-CH acidity among all carbonyl chemicals. Most challengingly, α-functionalization of N-H (primary and secondary) amides simultaneous containing the unactived α-C-H bond and a competitively active N-H bond, remains elusive. A general and efficient oxidative α-oxyamination and hydroxylation of aliphatic amides including secondary N-H amides was discribed...
August 11, 2017: Angewandte Chemie
David Ross Stuart
Aromatic rings are found in a wide variety of products, including pharmaceuticals, agrochemicals, and functional materials. Diaryliodonium salts are novel reagents used to transfer aryl groups under both metal-free and metal-catalyzed reactions and thereby synthesize arene-containing compounds. This review focuses on recent studies in selective aryl transfer reactions from unsymmetrical diaryliodonium salts under metal-free conditions. Reactions reported from 2008 to 2017, which represents a period of significant growth in diaryliodonium salt chemistry, are presented and organized by the type of reactive intermediate formed in the reaction...
August 9, 2017: Chemistry: a European Journal
Christopher Mulligan, Joseph A Mindell
Transporters are crucial in a number of cellular functions, including nutrient uptake, cell signaling, and toxin removal. As such, transporters are important drug targets and their malfunction is related to several disease states. Treating transporter-related diseases and developing pharmaceuticals targeting transporters require an understanding of their mechanism. Achieving a detailed understanding of transporter mechanism depends on an integrative approach involving structural and computational approaches as well as biochemical and biophysical methodologies...
2017: Methods in Enzymology
Saira Javed, Farrukh Azeem, Sabir Hussain, Ijaz Rasul, Muhammad Hussnain Siddique, Muhammad Riaz, Muhammad Afzal, Ambreen Kouser, Habibullah Nadeem
Lipase (E.C. belongs to the hydrolases and is also known as fat splitting, glycerol ester hydrolase or triacylglycerol acylhydrolase. Lipase catalyzes the hydrolysis of triglycerides converting them to glycerol and fatty acids in an oil-water interface. These are widely used in food, dairy, flavor, pharmaceuticals, biofuels, leather, cosmetics, detergent, and chemical industries. Lipases are of plant, animal, and microbial origin, but microbial lipases are produced at industrial level and represent the most widely used class of enzymes in biotechnological applications and organic chemistry...
July 31, 2017: Progress in Biophysics and Molecular Biology
Rosa Maria Iacobazzi, Antonio Lopalco, Annalisa Cutrignelli, Valentino Laquintana, Angela Lopedota, Massimo Franco, Nunzio Denora
An interesting mitochondrial biomarker is the 18-kDa mitochondrial translocator protein (TSPO). Decades of study have shown that this protein plays an important role in a wide range of cellular functions, including opening of the mitochondrial permeability transition pore as well as programmed cell death and proliferation. Variations in TSPO expression have been correlated to different diseases, from tumors to endocrine and neurological disorders. TSPO has therefore become an appealing target for both early diagnosis and selective mitochondrial drug delivery...
August 3, 2017: ChemMedChem
Giuseppe Meola, Henrik Braband, Sara Jordi, Thomas Fox, Olivier Blacque, Bernhard Spingler, Roger Alberto
Sandwich complexes are important building blocks in medicinal inorganic chemistry for group 6 and 8 elements but are almost unknown for the manganese triad. We present the syntheses and full characterization of the mixed-arene (99)Tc sandwich complexes [(99)Tc(η(6)-hmbz)(η(6)-C6H5-NH3)](PF6)2 and [(99)Tc(η(6)-hmbz)(η(6)-C6H5-Br)](PF6). Both comprise functionalities for conjugation to targeting molecules or for being included as substructures in pharmaceutically active lead compounds. Since η(6)-benzene ligands are too stably bound to be replaced with incoming ligands, we prepared naphthalene complexes [Re(η(6)-C6H6)(η(6)-napht)](+) and [Re(η(6)-napht)2](+)...
August 2, 2017: Dalton Transactions: An International Journal of Inorganic Chemistry
Dolores Morales-Cosme, Carlos Viesca-Treviño
This paper analyzes the articles published on chemicals and pharmaceuticals in the Periódico de la Academia de Medicina de Mégico. Through these publications it is possible to illustrate the transformation in the study of medical material of the era. At the same time, it shows discussions held by doctors and pharmacists about scientific news and analysis of local therapeutic resources.
May 2017: Gaceta Médica de México
Nilesh M Meghani, Hardik H Amin, Beom-Jin Lee
The concept of click chemistry (CC), first introduced by K.B. Sharpless, has been widely adopted for use in drug discovery, novel drug delivery systems (DDS), polymer chemistry, and material sciences. In this review, we outline novel aspects of CC related to drug discovery and drug delivery, with a brief overview of molecular mechanisms underlying each click reaction commonly used by researchers, and the main patents that paved the way for further diverse medicinal applications. We also describe recent progress in drug discovery and polymeric and carbon material-based drug delivery for potential pharmaceutical applications and advancements based on the CC approach, and discuss some intrinsic limitations of this popular conjugation reaction...
July 25, 2017: Drug Discovery Today
Priyanka Kalal, Divyani Gandhi, Prakash Prajapat, Shikha Agarwal
BACKGROUND: Thiazoles are promising scaffolds in the area of medicinal and pharmaceutical chemistry and have accounted to show different pharmacophoric properties. For the last years, thiazole derivatives have focused too much attention to develop different new CNS active agents. It has been broadly used to generate diverse therapeutic agents against various CNS targets. Histamine H3 receptors are seriously involved in the pathophysiology of numerous disorders of the central nervous system...
July 24, 2017: Current Drug Discovery Technologies
Alessandro Pellis, Sara Cantone, Cynthia Ebert, Lucia Gardossi
The unique selectivity of enzymes, along with their remarkable catalytic activity, constitute powerful tools for transforming renewable feedstock and also for adding value to an array of building blocks and monomers produced by the emerging bio-based chemistry sector. Although some relevant biotransformations run at the ton scale demonstrate the success of biocatalysis in industry, there is still a huge untapped potential of catalytic activities available for targeted valorization of new raw materials, such as waste streams and CO2...
July 22, 2017: New Biotechnology
Christine A Arbour, Hasina Y Saraha, Timothy F McMillan, Jennifer Stockdill
C-terminally modified peptides are important targets for pharmaceutical and biochemical applications. Known methods for C-terminal diversification are limited mainly in terms of the scope of accessible modifications or by epimerization of the C-terminal amino acid. In this work, we present a broadly applicable approach that enables access to a variety of C-terminally functionalized peptides in either protected or unprotected form. This chemistry proceeds without epimerization of C-terminal Ala and tolerates nucleophiles of varying nucleophilicity...
July 24, 2017: Chemistry: a European Journal
Haihui Peng, Fen-Er Chen
Prostaglandins (PGs) are a series of hormone-like chemical messengers and play a critical role in regulating physiological activity. The diversified therapeutic activities and complex molecular architectures of PGs have attracted special attention, and huge progress has been made in asymmetric total synthesis and discovery of pharmaceutically useful drug candidates. In the last 10 years, several powerful syntheses have emerged as new solutions to the problem of building PGs and represent major breakthroughs in this area...
August 2, 2017: Organic & Biomolecular Chemistry
S K Hong, K-W Lee, K C Yoon, H-S Kim, H Kim, N-J Yi, K-S Suh
BACKGROUND: Generic immunosuppressants may be cost-effective if clinical outcomes are equivalent to the brand-name medications. Mycophenolate mofetil in the form of My-rept may be cost-effective being a generic immunosuppressant, which is available as a 500-mg tablet as well as a 250-mg capsule (Chong Kun Dang Pharmaceutical Corporation, Seoul, Korea). OBJECTIVE: This study aimed to evaluate the efficacy, safety, cost-effectiveness, and convenience of My-rept 500-mg tablets in liver transplant recipients...
July 2017: Transplantation Proceedings
Anna Meneghello, Stefano Tartaggia, Maria Domenica Alvau, Federico Polo, Giuseppe Toffoli
Therapeutic drug monitoring (TDM) is the clinical practice of measuring pharmaceutical drug concentrations in patients' biofluids at designated intervals to allow a close and timely control of their dosage. This practice allows for rapid medical intervention in case of toxicity-related issues and/or adjustment of dosage to better fit the therapeutic demand. Currently, TDM is performed in centralized laboratories employing instruments, such as immunoassay analyzers and mass spectrometers that can be run only by trained personnel...
July 20, 2017: Current Medicinal Chemistry
Kaila A Margrey, Joshua B McManus, Simone Bonazzi, Frederic Zecri, David A Nicewicz
Direct C-H functionalization of aromatic compounds is a useful synthetic strategy that has garnered much attention because of its application to pharmaceuticals, agrochemicals, and late-stage functionalization reactions on complex molecules. On the basis of previous methods disclosed by our lab, we sought to develop a predictive model for site selectivity and extend this aryl functionalization chemistry to a selected set of heteroaromatic systems commonly used in the pharmaceutical industry. Using electron density calculations, we were able to predict the site selectivity of direct C-H functionalization in a number of heterocycles and identify general trends observed across heterocycle classes...
August 16, 2017: Journal of the American Chemical Society
Victor A Levin, Lauren E Abrey, Timothy P Heffron, Peter J Tonge, Arvin C Dar, William A Weiss, James M Gallo
CNS Anticancer Drug Discovery and Development November 2016, AZ, USA The 2016 second CNS Anticancer Drug Discovery and Development Conference addressed diverse viewpoints about why new drug discovery/development focused on CNS cancers has been sorely lacking. Despite more than 70,000 individuals in the USA being diagnosed with a primary brain malignancy and 151,669-286,486 suffering from metastatic CNS cancer, in 1999, temozolomide was the last drug approved by the US FDA as an anticancer agent for high-grade gliomas...
July 18, 2017: CNS Oncology
Weichao Huang, Fayza Daboussi
Diatoms have attracted considerable attention due to their success in diverse environmental conditions, which probably is a consequence of their complex origins. Studies of their metabolism will provide insight into their adaptation capacity and are a prerequisite for metabolic engineering. Several years of investigation have led to the development of the genome engineering tools required for such studies, and a profusion of appropriate tools is now available for exploring and exploiting the metabolism of these organisms...
September 5, 2017: Philosophical Transactions of the Royal Society of London. Series B, Biological Sciences
Jonathan Kil, Edward Lobarinas, Christopher Spankovich, Scott K Griffiths, Patrick J Antonelli, Eric D Lynch, Colleen G Le Prell
BACKGROUND: Noise-induced hearing loss is a leading cause of occupational and recreational injury and disease, and a major determinant of age-related hearing loss. No therapeutic agent has been approved for the prevention or treatment of this disorder. In animal models, glutathione peroxidase 1 (GPx1) activity is reduced after acute noise exposure. Ebselen, a novel GPx1 mimic, has been shown to reduce both temporary and permanent noise-induced hearing loss in preclinical studies. We assessed the safety and efficacy of ebselen for the prevention of noise-induced hearing loss in young adults in a phase 2 clinical trial...
July 14, 2017: Lancet
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