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Pharmaceutical chemistry

Eliane Gandolpho Tótoli, Hérida Regina Nunes Salgado
Bacterial conjunctivitis has high impact on the health of the population, since it represents more than a third of ocular pathologies reported by health services worldwide. There is a high incidence of bacterial resistance to the antimicrobials most commonly used for the treatment of conjunctivitis. In this context, besifloxacin stands out, since it is a fluoroquinolone developed exclusively for topical ophthalmic use, presenting a low risk of developing resistance due to its reduced systemic exposure. Bausch & Lomb markets it as ophthalmic suspension, under the trade name Besivance™...
January 18, 2018: Critical Reviews in Analytical Chemistry
Fernando Albericio, Saba Alapour, Beatriz G de la Torre, Deresh Ramjugernath, Neil Anthony Koorbanally
Considerable attention has been devoted to fluorinated compounds due to their unique and interesting properties. Many modern pharmaceuticals contain fluorinated substituents, which are commonly synthesized using selective fluorinating reagents. Decafluorobiphenyl (DFBP) as a fluorinated linker is susceptible to nucleophilic attack. This nucleophilic reaction has been widely studied using various nucleophiles. Sulfur and nitrogen containing nucleophiles have been of particular interest, especially in bioconjugated reactions...
January 17, 2018: Bioconjugate Chemistry
Ashish Tiwari, S J Dhoble
Chemiluminescence (CL) techniques are extensively utilized for detection of analytes due to their high sensitivity, rapidity and selectivity. With the advent of nanotechnology and incorporation of the nanoparticles in the CL system has revolutionized the assays due to their unique optical and mechanical properties. Several CL-based reactions have been developed where these nanoparticle based CL sensors have evolved as excellent prospects for sensing in various analytical applications. This review article addresses the nanoparticles based CL detection system that are recently developed, the mechanisms has been summarized and the role of luminophors have been discussed...
April 1, 2018: Talanta
Serge Mignani, João Rodrigues, Helena Tomas, Rachid Jalal, Parvinder Pal Singh, Jean-Pierre Majoral, Ram A Vishwakarma
During the past decade, decreasing the attrition rate of drug development candidates reaching the market has become one of the major challenges in pharmaceutical research and drug development (R&D). To facilitate the decision-making process, and to increase the probability of rapidly finding and developing high-quality compounds, a variety of multiparametric guidelines, also known as rules and ligand efficiency (LE) metrics, have been developed. However, what are the 'best' descriptors and how far can we simplify these drug-likeness prediction tools in terms of the numerous, complex properties that they relate to?...
January 9, 2018: Drug Discovery Today
I-Chen Sun, Churn-Shiouh Gau
Generic drugs are accounted for majority of medicinal products. To reduce the unnecessary review for incomplete dossiers of generic drugs, Taiwanese government launched a refuse-to-file (RTF) procedure since 2017. The present study aimed to examine the outcome of RTF procedure by analyzing application characteristic, RTF rate and deficiencies found in the submitted dossiers. Descriptions of administrative information, chemistry, manufacturing and controls, bioequivalence study, and comparative dissolution testing were presented during the first 6 months after the implementation of RTF policy...
January 9, 2018: Regulatory Toxicology and Pharmacology: RTP
Haifeng Yang, Peter G Dormer, Nelo R Rivera, Andrew J Hoover
Tritium-labeled molecules are critical tools for elucidating the binding and metabolic properties of bioactive compounds, particularly during pharmaceutical discovery. Direct tritiation of inert C-H bonds with T2 gas is an ideal approach for tritium labeling, but significant gaps remain for direct tritiation of structurally complex molecules with diverse functional groups. Here we report the first application of palladium(II) C-H activation chemistry for tritiation with T2 gas. This practical transformation exhibits novel substrate scope and greater functional group tolerance compared to previous state of the art tritiation methods, and has been applied to directly tritiate 9 complex pharmaceuticals and an unprotected dipeptide...
January 3, 2018: Angewandte Chemie
Tuğçe Yurtluk, Fikriye Alev Akçay, Ayşe Avcı
Biosynthesis of silver nanoparticles (AgNPs) using microorganisms is an important application of nano-biotechnology and green chemistry because of interest by pharmaceutical and food manufacturers. In this study, biosynthesis of AgNPs by a novel Bacillus strain isolated from a soil sample from Sakarya district in Turkey was investigated. Biosynthesis was performed using cell-free supernatant of the bacterium following 24 h growth. Effects of varying AgNO3 concentration (1-10 mM), pH (5-10), and temperature (30-40°C) on the synthesis of AgNPs were determined...
January 9, 2018: Preparative Biochemistry & Biotechnology
William A Tarpeh, James M Barazesh, Tzahi Y Cath, Kara L Nelson
Recovering nitrogen from separately collected urine can potentially reduce costs and energy of wastewater nitrogen removal and fertilizer production. Through benchtop experiments, we demonstrate the recovery of nitrogen from urine as ammonium sulfate using electrochemical stripping, a combination of electrodialysis and membrane stripping. Nitrogen was selectively recovered with 93% efficiency in batch experiments with real urine and required 30.6 MJ kg N-1 in continuous-flow experiments (slightly less than conventional ammonia stripping)...
January 5, 2018: Environmental Science & Technology
Seyed Mohammad Nabavi, Gian Luigi Russo, Idolo Tedesco, Maria Daglia, Ilkay Erdogan Orhan, Seyed Fazel Nabavi, Anupam Bishayee, Kalyan C Nagulapalli Venkata, Mohammad Abdollahi, Zohreh Hajheydari
Melanoma is the most deadly form of skin cancer, with about 48,000 deaths each year worldwide. Growing evidence suggests that individual nutrients or dietary patterns might have important roles in the prevention of melanoma. Considering that melanoma is a potentially life-threatening cancer, novel protective and adjuvant treatments are needed to improve its prognosis. Curcumin is a bioactive substance extracted from rhizome of Curcuma longa L. Its global market is expected to grow in the next few years, especially in the pharmaceutical industry, due to its numerous physiological and pharmacological properties...
January 4, 2018: Nutrition and Cancer
María José Bagur, Gonzalo Luis Alonso Salinas, Antonia M Jiménez-Monreal, Soukaina Chaouqi, Silvia Llorens, Magdalena Martínez-Tomé, Gonzalo L Alonso
The spice saffron is made from the dried stigmas of the plant Crocus sativus L. The main use of saffron is in cooking, due to its ability to impart colour, flavour and aroma to foods and beverages. However, from time immemorial it has also been considered a medicinal plant because it possesses therapeutic properties, as illustrated in paintings found on the island of Santorini, dated 1627 BC. It is included in Catalogues of Medicinal Plants and in the European Pharmacopoeias, being part of a great number of compounded formulas from the 16th to the 20th centuries...
December 23, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Thomas E Smith, Christopher D Pond, Elizabeth Pierce, Zachary P Harmer, Jason Kwan, Malcolm M Zachariah, Mary Kay Harper, Thomas P Wyche, Teatulohi K Matainaho, Tim S Bugni, Louis R Barrows, Chris M Ireland, Eric W Schmidt
Chemistry drives many biological interactions between the microbiota and host animals, yet it is often challenging to identify the chemicals involved. This poses a problem, as such small molecules are excellent sources of potential pharmaceuticals, pretested by nature for animal compatibility. We discovered anti-HIV compounds from small, marine tunicates from the Eastern Fields of Papua New Guinea. Tunicates are a reservoir for new bioactive chemicals, yet their small size often impedes identification or even detection of the chemicals within...
January 1, 2018: Nature Chemical Biology
Scott A Snyder
Efforts to achieve the laboratory synthesis of complex natural products have long served as a means to advance the science of organic chemistry. Indeed, core physical organic principles, new reagents and synthetic transformations, effective strategies for stereocontrolled synthesis, and useful pharmaceutical agents are but a few advances that have issued from such endeavors over the course of the past century. Within this review are recounted selected research programs from the author's laboratory seeking to add to that repertoire of discoveries by targeting complex polycyclic alkaloids for synthesis...
December 1, 2017: Chimia
Zhu-Bao Yin, Jian-Heng Ye, Wen-Jun Zhou, Yi-Han Zhang, Li Ding, Yong-Yuan Gui, Si-Shun Yan, Jing Li, Da-Gang Yu
A selective oxy-difluoroalkylation of allylamines with carbon dioxide (CO2) via visible-light photoredox catalysis is reported. These multicomponent reactions are efficient and environmentally friendly to generate a series of important 2-oxazolidinones with functionalized difluoroalkyl groups. The good functional group tolerance, broad substrate scope, easy scalability, mild reaction conditions, and facile functionalization of products provide great potential for application in organic synthesis and pharmaceutical chemistry...
December 27, 2017: Organic Letters
Ming Zhang, Bo An, Yang Qu, Shichen Shen, Wei Fu, Yuan-Ju Chen, Xue Wang, Rebeccah Young, John M Canty, Joseph P Balthasar, Keeley Murphy, Debadeep Bhattacharyya, Jonathan L Josephs, Luca Ferrari, Shaolian Zhou, Surendra Bansal, Faye Vazvaei, Jun Qu
For LC-MS-based targeted quantification of biotherapeutics/biomarkers in clinical and pharmaceutical environments, high sensitivity, high throughput, and excellent robustness are all essential, but remain challenging. For example, though nano-LC-MS has been employed to enhance analytical sensitivity, it falls short due to its low loading capacity, poor throughput and low operational robustness. Furthermore, high chemical noise in protein bioanalysis typically limits the sensitivity. Here we describe a novel Trapping-micro-LC-MS (T-µLC-MS) strategy for targeted protein bioanalysis, achieving high sensitivity with exceptional robustness and high throughput...
December 25, 2017: Analytical Chemistry
Gulam Rabbani, Inho Choi
Nature selected osmolytes to protect intracellular macromolecules exposed to denaturing conditions and stabilize proteins. Osmolytes are small naturally occurring compounds that act as chemical chaperones under changing environmental conditions and in disease states, and are present in microorganisms, animals, and plants. In the intracellular environment osmolytes naturally accumulate at high concentrations when cells/tissues are exposed to stressful conditions, which is important because protein aggregation, misfolding, and destabilization underlie the pathogeneses of several life-threatening neurodegenerative disorders...
December 20, 2017: International Journal of Biological Macromolecules
Srinivasulu Cherukupalli, Girish A Hampannavar, Sampath Chinnam, Balakumar Chandrasekaran, Nisar Sayyad, Francis Kayamba, Rajeshwar Reddy Aleti, Rajshekhar Karpoormath
Pyrazolo[4,3-d]pyrimidine, a fused heterocycle bearing pyrazole and pyrimidine portions has gained a significant attention in the field of bioorganic and medicinal chemistry. Pyrazolo[4,3-d]pyrimidine derivatives have demonstrated numerous pharmacological activities particularly, anti-cancer, anti-infectious, phosphodiesterase inhibitors, adenosine antagonists and cytokinin antagonists etc. This review extensively unveils the synthetic and pharmacological diversity with special emphasis on structural variations around pyrazolo[4,3-d]pyrimidine scaffold...
October 25, 2017: Bioorganic & Medicinal Chemistry
Ivana Perković, Višnja Stepanić, Vesna Gabelica Marković
The Croatian Chemical Society was established in 1926 and has developed over the decades into a society that actively supports all chemical activities in Croatia. The Society has eight divisions, the youngest of which, the Division of Medicinal and Pharmaceutical Chemistry, was established in 2012 and immediately became a member of the European Federation of Medicinal Chemistry (EFMC). The mission of the Medicinal and Pharmaceutical Chemistry Division is the promotion and development of scientific, professional, and educational activities within the medicinal chemistry community in Croatia, as well as to build partnerships and collaborations with other primarily EU-based medicinal chemistry societies...
December 18, 2017: ChemMedChem
Vânia André, Sílvia Quaresma, João Luís Ferreira da Silva, M Teresa Duarte
Mechanochemistry is a powerful and environmentally friendly synthetic technique successfully employed in different fields of synthetic chemistry. Application spans from organic to inorganic chemistry including the synthesis of coordination compounds. Metal-organic frameworks (MOFs) are a class of compounds with numerous applications, from which we highlight herein their application in the pharmaceutical field (BioMOFs), whose importance has been growing and is now assuming a relevant and promising domain. The need to find cleaner, greener and more energy and material-efficient synthetic procedures led to the use of mechanochemistry into the synthesis of BioMOFs...
2017: Beilstein Journal of Organic Chemistry
Chularat Wattanakit, Thittaya Yutthalekha, Sunpet Asssavapanumat, Veronique Lapeyre, Alexander Kuhn
Asymmetric synthesis of molecules is of crucial importance to obtain pure chiral compounds, which are of primary interest in many areas including medicine, biotechnology, and chemistry. Various methods have been used very successfully to increase the enantiomeric yield of reaction pathways, but there is still room for the development of alternative highly enantioselective reaction concepts, either as a scientific challenge of tremendous fundamental significance, or owing to the increasing demand for enantiopure products, e...
December 12, 2017: Nature Communications
Matthew J DellaVecchia, Alyssa M Claudio, Jamie L Fairclough
BACKGROUND AND PURPOSE: To describe 1) a pharmacy student's teaching assistant (TA) role in an undergraduate medicinal chemistry course, 2) an active learning module co-developed by the TA and instructor, and 3) the unexpected opportunities for pharmacy educational outreach that resulted from this collaboration. EDUCATIONAL ACTIVITY AND SETTING: Medicinal Chemistry (CHM3413) is an undergraduate course offered each fall at Palm Beach Atlantic University (PBA). As a TA for CHM3413, a pharmacy student from the Gregory School of Pharmacy (GSOP) at PBA co-developed and implemented an active learning module emphasizing foundational medicinal chemistry concepts as they pertain to performance enhancing drugs (PEDs)...
November 2017: Currents in Pharmacy Teaching & Learning
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