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Pharmaceutical chemistry

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https://www.readbyqxmd.com/read/28642381/chemical-transformation-of-xenobiotics-by-the-human-gut-microbiota
#1
REVIEW
Nitzan Koppel, Vayu Maini Rekdal, Emily P Balskus
The human gut microbiota makes key contributions to the metabolism of ingested compounds (xenobiotics), transforming hundreds of dietary components, industrial chemicals, and pharmaceuticals into metabolites with altered activities, toxicities, and lifetimes within the body. The chemistry of gut microbial xenobiotic metabolism is often distinct from that of host enzymes. Despite their important consequences for human biology, the gut microbes, genes, and enzymes involved in xenobiotic metabolism are poorly understood...
June 23, 2017: Science
https://www.readbyqxmd.com/read/28636605/catalytic-allylic-oxidation-of-internal-alkenes-to-a-multifunctional-chiral-building-block
#2
Liela Bayeh, Phong Q Le, Uttam K Tambar
The stereoselective oxidation of hydrocarbons is one of the most notable advances in synthetic chemistry over the past fifty years. Inspired by nature, enantioselective dihydroxylations, epoxidations and other oxidations of unsaturated hydrocarbons have been developed. More recently, the catalytic enantioselective allylic carbon-hydrogen oxidation of alkenes has streamlined the production of pharmaceuticals, natural products, fine chemicals and other functional materials. Allylic functionalization provides a direct path to chiral building blocks with a newly formed stereocentre from petrochemical feedstocks while preserving the olefin functionality as a handle for further chemical elaboration...
June 21, 2017: Nature
https://www.readbyqxmd.com/read/28636596/selective-sp-3-c-h-alkylation-via-polarity-match-based-cross-coupling
#3
Chip Le, Yufan Liang, Ryan W Evans, Ximing Li, David W C MacMillan
The functionalization of carbon-hydrogen (C-H) bonds is one of the most attractive strategies for molecular construction in organic chemistry. The hydrogen atom is considered to be an ideal coupling handle, owing to its relative abundance in organic molecules and its availability for functionalization at almost any stage in a synthetic sequence. Although many C-H functionalization reactions involve C(sp(3))-C(sp(2)) coupling, there is a growing demand for C-H alkylation reactions, wherein sp(3) C-H bonds are replaced with sp(3) C-alkyl groups...
June 21, 2017: Nature
https://www.readbyqxmd.com/read/28636311/insights-into-integrated-lead-generation-and-target-identification-in-malaria-and-tuberculosis-drug-discovery
#4
John Okombo, Kelly Chibale
New, safe and effective drugs are urgently needed to treat and control malaria and tuberculosis, which affect millions of people annually. However, financial return on investment in the poor settings where these diseases are mostly prevalent is very minimal to support market-driven drug discovery and development. Moreover, the imminent loss of therapeutic lifespan of existing therapies due to evolution and spread of drug resistance further compounds the urgency to identify novel effective drugs. However, the advent of new public-private partnerships focused on tropical diseases and the recent release of large data sets by pharmaceutical companies on antimalarial and antituberculosis compounds derived from phenotypic whole cell high throughput screening have spurred renewed interest and opened new frontiers in malaria and tuberculosis drug discovery...
June 21, 2017: Accounts of Chemical Research
https://www.readbyqxmd.com/read/28632928/n-acylsulfonamides-synthetic-routes-and-biological-potential-in-medicinal-chemistry
#5
REVIEW
Alessandra Ammazzalorso, Barbara De Filippis, Letizia Giampietro, Rosa Amoroso
Sulfonamide is a common structural motif in naturally occurring and synthetic medicinal compounds. The rising interest in sulfonamides and N-acyl derivatives is attested by the large number of drugs and lead compounds identified in last years, explored in different fields of medicinal chemistry and showing biological activity. Many acylsulfonamide derivatives were designed and synthesized as isosteres of carboxylic acids, being the characteristics of these functional groups very close. Starting from chemical routes to N-acylsulfonamides, this review explores compounds of pharmaceutical interest, developed as enzymatic inhibitors or targeting receptors...
June 20, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28627150/-applying-a-set-of-indicators-to-evaluate-the-primary-health-care
#6
Antonio Giampietro Russo, Maria Teresa Greco
OBJECTIVES: to develop a system of indicators to monitor the quality of health care, in terms of safety, effectiveness, and appropriateness to allow the integrated promotion of the welfare of the effectiveness and quality. DESIGN: retrospective study. SETTING AND PARTICIPANTS: all general practitioners (GPs) with at least 100 patients in loading at 1.1.2015 were included. The setting chosen is the Primary Care of the Agency for Health Protection of the Province of Milan (Northern Italy)...
January 2017: Epidemiologia e Prevenzione
https://www.readbyqxmd.com/read/28621561/a-patent-review-of-two-fruitful-decades-1997-2016-of-isocoumarin-research
#7
Hidayat Hussain, Ivan R Green
Isocoumarins comprise a six-membered oxygen heterocycle (α-pyranone) along with one aromatic ring and are known to possess interesting biological properties. During the last two decade (1997-2016), isocoumarin chemistry has attracted attention due to its biological and pharmaceutical effects viz., anticancer, anti-diabetic, antibacterial, antimalarial, and fungicidal effects. Areas covered: This review covers the patents on the therapeutic activities of natural and synthetic isocoumarins over the last two decades (1997-2016)...
June 16, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28619938/kilogram-scale-prexasertib-monolactate-monohydrate-synthesis-under-continuous-flow-cgmp-conditions
#8
Kevin P Cole, Jennifer McClary Groh, Martin D Johnson, Christopher L Burcham, Bradley M Campbell, William D Diseroad, Michael R Heller, John R Howell, Neil J Kallman, Thomas M Koenig, Scott A May, Richard D Miller, David Mitchell, David P Myers, Steven S Myers, Joseph L Phillips, Christopher S Polster, Timothy D White, Jim Cashman, Declan Hurley, Robert Moylan, Paul Sheehan, Richard D Spencer, Kenneth Desmond, Paul Desmond, Olivia Gowran
Advances in drug potency and tailored therapeutics are promoting pharmaceutical manufacturing to transition from a traditional batch paradigm to more flexible continuous processing. Here we report the development of a multistep continuous-flow CGMP (current good manufacturing practices) process that produced 24 kilograms of prexasertib monolactate monohydrate suitable for use in human clinical trials. Eight continuous unit operations were conducted to produce the target at roughly 3 kilograms per day using small continuous reactors, extractors, evaporators, crystallizers, and filters in laboratory fume hoods...
June 16, 2017: Science
https://www.readbyqxmd.com/read/28612408/sufex-mediated-synthesis-of-sterically-hindered-and-electron-deficient-secondary-and-tertiary-amides-via-acyl-fluoride-intermediates
#9
John Edward Moses, Pallavi Sharma, Andrew Barrow, Christian Spiteri, Christopher Smedley, Marie-Claire Giel
Amide bond formation is one of the most executed reactions in chemistry and biology. This is largely due to the ubiquity of the amide functional group in biological molecules, natural products and pharmaceutically important drugs. We report here the development of "SuFExAmide": a new Sulfur Fluoride Exchange (SuFEx) click chemistry based protocol for the efficient amidation of carboxylic acids via acyl fluoride intermediates. We have developed benzene-1,3-disulfonyl fluoride as a cost effective, powerful and versatile coupling agent, which delivers challenging secondary and tertiary amides in excellent yield from sterically hindered and electron-deficient amines...
June 14, 2017: Chemistry: a European Journal
https://www.readbyqxmd.com/read/28605186/synthesis-of-oil-laden-poly-ethylene-glycol-diacrylate-hydrogel-nanocapsules-from-double-nanoemulsions
#10
Mengwen Zhang, Maksymilian Nowak, Paula Malo de Molina, Michael Abramovitch, Katherine Santizo, Samir Mitragotri, Matthew E Helgeson
Multiple emulsions have received great interest due to their ability to be used as templates for the production of multicompartment particles for a variety of applications. However, scaling these complex droplets to nanoscale dimensions has been a challenge due to limitations on their fabrication methods. Here, we report the development of oil-in-water-in-oil (O1/W/O2) double nanoemulsions via a two-step high-energy method and their use as templates for complex nanogels comprised of inner oil droplets encapsulated within a hydrogel matrix...
June 12, 2017: Langmuir: the ACS Journal of Surfaces and Colloids
https://www.readbyqxmd.com/read/28604633/fluoroalkyl-amino-reagents-fars-a-general-approach-towards-the-synthesis-of-heterocyclic-compounds-bearing-emergent-fluorinated-substituents
#11
REVIEW
Bruno Commare, Etienne Schmitt, Fallia Aribi, Armen Panossian, Jean-Pierre Vors, Sergiy Pazenok, Frédéric R Leroux
Fluorinated heterocycles are important building blocks in pharmaceutical, agrochemical and material sciences. Therefore, organofluorine chemistry has witnessed high interest in the development of efficient methods for the introduction of emergent fluorinated substituents (EFS) onto heterocycles. In this context, fluoroalkyl amino reagents (FARs)-a class of chemicals that was slightly forgotten over the last decades-has emerged again recently and proved to be a powerful tool for the introduction of various fluorinated groups onto (hetero)aromatic derivatives...
June 12, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28603797/a-highly-enantioselective-access-to-chiral-chromanones-and-thiochromanones-via-copper-catalyzed-asymmetric-conjugated-reduction-of-chromones-and-thiochromones
#12
Donglu Xiong, Wenxi Zhou, Zhiwu Lu, Suping Zeng, Jun Joelle Wang
The chromanone scaffold is a privileged structure in heterocyclic chemistry and drug discovery. A highly efficient copper-catalyzed asymmetric conjugated reduction of chromones is developed to give chiral chromanones with good yields (80-99%) and excellent ee values (94->99% ee). Particularly noteworthy is that chiral thiochromanones are also constructed using this method in 74-87% yields with 96-97% ee. The established asymmetric synthesis paves the way for their further pharmaceutical studies.
June 22, 2017: Chemical Communications: Chem Comm
https://www.readbyqxmd.com/read/28598411/ruthenium-ii-catalysed-remote-c-h-alkylations-as-a-versatile-platform-to-meta-decorated-arenes
#13
Jie Li, Korkit Korvorapun, Suman De Sarkar, Torben Rogge, David J Burns, Svenja Warratz, Lutz Ackermann
The full control of positional selectivity is of prime importance in C-H activation technology. Chelation assistance served as the stimulus for the development of a plethora of ortho-selective arene functionalizations. In sharp contrast, meta-selective C-H functionalizations continue to be scarce, with all ruthenium-catalysed transformations currently requiring difficult to remove or modify nitrogen-containing heterocycles. Herein, we describe a unifying concept to access a wealth of meta-decorated arenes by a unique arene ligand effect in proximity-induced ruthenium(II) C-H activation catalysis...
June 9, 2017: Nature Communications
https://www.readbyqxmd.com/read/28597435/micro-morphological-study-of-evolvulus-spp-convolvulaceae-the-old-world-medicinal-plants
#14
Kanapol Ketjarun, George W Staples, Sasivimon C Swangpol, Paweena Traiperm
BACKGROUND: Several medicinal properties have been reported for plants in the genus Evolvulus, such as a brain tonic and antifungal from Evolvulus alsinoides, and a sedative and an anthelmintic from Evolvulus nummularius. Therefore, the correct identification of the source plants is critically important. The aim of this research was to investigate the micromorphology of two Evolvulus taxa used for herbal medicines compared with one worldwide ornamental species by using peeling, paraffin embedding, acetolysis, and SEM methods in order to support species identification...
December 2016: Botanical Studies (Taipei, Taiwan)
https://www.readbyqxmd.com/read/28578943/efficient-synthesis-of-secondary-amines-by-reductive-amination-of-curdlan-staudinger-ylides
#15
Ruoran Zhang, Shu Liu, Kevin J Edgar
Staudinger-related reactions between azides and phosphines are important in organic chemistry due to their chemoselectivity, high efficiency, and mild reaction conditions. Staudinger reduction of azides affords highly reactive iminophosphorane ylides; the reactivity of the negatively charged ylide nitrogen atom has not previously been fully explored in polysaccharide chemistry. Curdlan, a natural, biocompatible, and bioactive β-1,3-glucan with low toxicity, has remarkable potential in biomedical and pharmaceutical applications...
September 1, 2017: Carbohydrate Polymers
https://www.readbyqxmd.com/read/28578243/comparative-study-on-pharmaceuticals-adsorption-in-reclaimed-water-desalination-concentrate-using-biochar-impact-of-salts-and-organic-matter
#16
Lu Lin, Wenbin Jiang, Pei Xu
The synergistic impact of salts and organic matter on adsorption of ibuprofen and sulfamethoxazole by three types of biochar and an activated carbon was investigated using reclaimed water reverse osmosis (RO) concentrate and synthetic solutions spiked with target organic compounds and non-target water constituents (e.g., Na(+), Ca(2+), Mg(2+), K(+), Cl(-), SO4(2-), alkalinity, humic acid (HA), and bovine serum albumin (BSA)). Kinetic modeling was used to better understand the adsorption process between the carbon adsorbents and pharmaceuticals and to elucidate the impact of water chemistry on pharmaceuticals adsorption...
June 1, 2017: Science of the Total Environment
https://www.readbyqxmd.com/read/28572733/the-jordan-food-and-drug-administration-comparison-of-its-registration-process-with-australia-canada-saudi-arabia-and-singapore
#17
Wesal Salem Al Haqaish, Hayel Obeidat, Prisha Patel, Stuart Walker
OBJECTIVE: This study outlines the current regulatory review process and good review practices (GRevPs) at the Jordan Food and Drug Administration (JFDA) and compares them with those of regulatory agencies in Australia, Canada, Saudi Arabia and Singapore to gauge how well the JFDA is performing. We identify opportunities for further development of the JFDA as a key global reference agency. METHODS: Personnel within the JFDA completed a questionnaire comprising four sections: organisation, key milestones, review timelines, and GRevPs...
2017: Pharmaceutical Medicine
https://www.readbyqxmd.com/read/28534207/construction-of-polyarylenes-with-various-structural-features-via-bergman-cyclization-polymerization
#18
REVIEW
Youfu Wang, Shudan Chen, Aiguo Hu
Synthetic polymer chemistry is a fundamental part of polymer science, and highly efficient polymerization reactions are essential for the synthesis of high-performance polymers. Development of new synthetic methods for emerging polymer science is of great importance in this regard. Bergman cyclization is a chemical process in which highly reactive aryl diradicals form from enediyne precursors, having a strong impact in a number of fields including pharmaceutics, synthetic chemistry, and materials science. Diradical intermediates stemming from enediynes can cause DNA cleavage under physiological conditions, leading to the strong cytotoxicity of many naturally occurring enediyne antibiotics...
June 2017: Topics in Current Chemistry (Journal)
https://www.readbyqxmd.com/read/28531154/announcing-the-2017-pharmaceuticals-travel-award-for-young-post-doctoral-researchers
#19
EDITORIAL
Jean Jacques Vanden Eynde
Last year, for the first time in its history, our Journal was able to offer a travel grant of 800 CHF to a young researcher in the field of medicinal chemistry.
May 22, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28530197/green-fabricated-cuo-nanobullets-via-olea-europaea-leaf-extract-shows-auspicious-antimicrobial-potential
#20
Qaisar Maqbool, Sidra Iftikhar, Mudassar Nazar, Fazal Abbas, Asif Saleem, Talib Hussain, Rizwan Kausar, Sadaf Anwaar, Nyla Jabeen
In present investigation, copper oxide (CuO) nanostructures have been prepared via green chemistry. Olea europaea leaf extract act as strong chelating agent for tailoring physical as well as bio-medical characteristics of CuO at the nano-size. Physical characterisation such as scanning electron microscope analysis depicts the formation of homogenised spherical shape nanoparticles (NPs) with average size of 42 nm. X-ray diffraction and Fourier transform infrared spectroscopy further confirmed the crystalline pure phase and monoclinic structure...
June 2017: IET Nanobiotechnology
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