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Medicinal chemistry

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https://www.readbyqxmd.com/read/28328151/exploiting-octahedral-stereocenters-from-enzyme-inhibition-to-asymmetric-photoredox-catalysis
#1
REVIEW
Eric Meggers
A simple concept, namely exploiting the structural and stereochemical complexity of octahedral metal complexes, can have unexpected impact in different areas of chemical research, from medicinal chemistry and chemical biology to asymmetric catalysis and photoredox chemistry.
March 22, 2017: Angewandte Chemie
https://www.readbyqxmd.com/read/28328074/the-13-th-winter-conference-on-medicinal-and-bioorganic-chemistry
#2
Scott D Williams
The Medicinal and Bioorganic Chemistry Foundation (MBCF) hosted its 13(th) biannual Winter Conference on Medicinal and Bioorganic Chemistry (WCMBC) this past January 22(nd) -26(th) in Steamboat Springs, Colorado (USA). The gathering this year kept true to the tradition of this conference series, with an impressive lineup of presenters from both academia and industry. With about 125 delegates, the conference took all the advantages of a mid-sized gathering: a sufficiently wide spectrum of scientists in attendance, yet an intimate atmosphere conducive to solid networking and frank, open discussions...
March 22, 2017: ChemMedChem
https://www.readbyqxmd.com/read/28328012/free-fatty-acid-receptor-1-ffar1-as-an-emerging-therapeutic-target-for-type-2-diabetes-mellitus-recent-progress-and-prevailing-challenges
#3
REVIEW
Zheng Li, Xue Xu, Wenlong Huang, Hai Qian
The free fatty acid receptor 1 (FFAR1/GPR40) amplifies glucose-dependent insulin secretion; therefore, it has attracted widespread attention as a promising antidiabetic target. Current clinical proof of concept also indicates that FFAR1 agonists achieve the initially therapeutic endpoint for the treatment of type 2 diabetes mellitus (T2DM) without the hypoglycemic risk. Thus, many pharmaceutical companies and academic institutes are competing to develop FFAR1 agonists. However, several candidates have been discontinued in clinical trials, often without reporting the underlying reasons...
March 22, 2017: Medicinal Research Reviews
https://www.readbyqxmd.com/read/28327664/bioactive-silicon-nitride-a-new-therapeutic-material-for-osteoarthropathy
#4
Giuseppe Pezzotti, Elia Marin, Tetsuya Adachi, Alfredo Rondinella, Francesco Boschetto, Wenliang Zhu, Nobuhiko Sugano, Ryan M Bock, Bryan McEntire, Sonny B Bal
While the reciprocity between bioceramics and living cells is complex, it is principally governed by the implant's surface chemistry. Consequently, a deeper understanding of the chemical interactions of bioceramics with living tissue could ultimately lead to new therapeutic strategies. However, the physical and chemical principles that govern these interactions remain unclear. The intricacies of this biological synergy are explored within this paper by examining the peculiar surface chemistry of a relatively new bioceramic, silicon nitride (Si3N4)...
March 22, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28326602/synthesis-characterization-and-evaluation-of-difluoropyrido-4-3-b-indoles-as-potential-agents-for-acetylcholinesterase-and-antiamnesic-activity
#5
Malavalli Madaiah, Bidarur K Jayanna, Arakere S Manu, Maralekere K Prashanth, Hosakere D Revanasiddappa, Bantal Veeresh
Acetylcholinesterase (AChE) inhibitors are currently the most widely prescribed drugs for Alzheimer's disease. The high potential of indole compounds in medicinal chemistry led us to discover a novel series of fluoroindole compounds. The synthesis and pharmacological analysis of the difluoropyrido[4,3-b]indoles 11-34 are described. Compounds 11-34 were tested for AChE inhibition activity using a rat brain homogenate. Compounds 25-29 display a promising in vitro profile with an IC50 value range of 46-51.6 nM and show significant protective effect on scopolamine-induced amnesia...
March 22, 2017: Archiv der Pharmazie
https://www.readbyqxmd.com/read/28325143/synthesis-and-characterization-of-a-new-benzo-indole-derivative-with-apoptotic-activity-against-colon-cancer-cells
#6
Fatemeh Hajiaghaalipou, Fadhil Lafta Faraj, Elham Bagheri, Hamid Khaledi, Hapipah Mohd Ali, Nazia Abdul Majid, Mahmood Ameen Abdulla
BACKGROUND: Colorectal cancer is the third most common form of cancer in both men and women around the world. The chemistry and biological study of heterocyclic compounds have been an interesting area for a long time in pharmaceutical and medicinal chemistry. METHODS: A new synthetic compound, 2-(1,1-Dimethyl-1,3-dihydro-benzo[e]indol-2-ylidene)-3-(2-hydroxy-phenylimino)-propionaldehyde, abbreviated as DBID has been synthesized by reaction of 2-(1,1-Dimethyl-1,3-dihydro-benzo[e]indol-2-ylidene)-malonaldehyde with 2-aminophenol...
March 20, 2017: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/28324911/synthesis-of-two-c-14-labeled-cathepsin-c-inhibitors-the-use-of-a-cyanide-to-displace-a-benzotriazole
#7
Lee Kingston, Jonas Bergare, Hans Lönn, Cecilia Ericsson, Gunnar Grönberg, Song Chen, Charles S Elmore
In support of the development of a new treatment for COPD, two C-14 labeled compounds were required for in vitro animal studies. The synthesis of nitrile [(14) C]-1 was completed in 3 steps from C-14 labeled 4-bromobenzonitrile in accord with the previously developed medicinal chemistry route. The second compound, 2, did not possess an arylnitrile as did 1 which made the synthetic design more complex. An advanced, unlabeled benzotriazole containing intermediate, 10, was synthesized in low yield over 3 steps and was subsequently reacted with K(14) CN to give a mixture of diastereomers 12...
March 21, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
https://www.readbyqxmd.com/read/28322729/standardisation-and-use-of-the-alcohol-biomarker-carbohydrate-deficient-transferrin-cdt
#8
Anders Helander, Jos Wielders, Raymond Anton, Torsten Arndt, Vincenza Bianchi, Jean Deenmamode, Jan-Olof Jeppsson, John B Whitfield, Cas Weykamp, François Schellenberg
Carbohydrate-deficient transferrin (CDT) is a glycoform profile of serum transferrin that increases in response to sustained high alcohol intake and over the last decades has become an important alcohol biomarker with clinical and forensic applications. However, the wide range of CDT measurement procedures has resulted in lack of uniform results and reference limits, and hampered comparison of results. In 2005, the IFCC therefore founded a special working group (WG) aiming for standardisation of CDT measurement...
March 18, 2017: Clinica Chimica Acta; International Journal of Clinical Chemistry
https://www.readbyqxmd.com/read/28322497/single-molecule-force-spectroscopy-to-compare-natural-versus-artificial-antibody-antigen-interaction
#9
Congzhou Wang, Rong Hu, Jeremiah J Morrissey, Evan D Kharasch, Srikanth Singamaneni
Biorecognition is central to various biological processes and finds numerous applications in virtually all areas of chemistry, biology, and medicine. Artificial antibodies, produced by imprinting synthetic polymers, are designed to mimic the biological recognition capability of natural antibodies, while exhibiting superior thermal, chemical, and environmental stability compared to their natural counterparts. The binding affinity of the artificial antibodies to their antigens characterizes the biorecognition ability of these synthetic nanoconstructs and their ability to replace natural recognition elements...
March 21, 2017: Small
https://www.readbyqxmd.com/read/28322139/heparin-tailored-biopolymeric-nanocarriers-in-site-specific-delivery-a-systematic-review
#10
Ashish Garg, Rajeev Sharma, Vikas Pandey, Vaibhav Patel, Awesh K Yadav
The combination of nanocarriers and biological molecules is of intense interest because of the synergistic properties offered by such newly synthesized composites. Heparin conjugated to nanomaterials has recently been investigated for its beneficial chemical and biological properties and its capacity to improve the biocompatibility of nanocarriers, increasing their performance in various biological applications. A variety of recent research combines heparin and nanomaterials for a myriad of uses. For example, heparin has been conjugated to the surface of magnetic and metallic nanoparticles, biodegradable and nondegradable synthetic polymers, nanocomposites, dendrimers, and the like...
2017: Critical Reviews in Therapeutic Drug Carrier Systems
https://www.readbyqxmd.com/read/28319779/supramolecular-biofunctional-materials
#11
REVIEW
Jie Zhou, Jie Li, Xuewen Du, Bing Xu
This review discusses supramolecular biofunctional materials, a novel class of biomaterials formed by small molecules that are held together via noncovalent interactions. The complexity of biology and relevant biomedical problems not only inspire, but also demand effective molecular design for functional materials. Supramolecular biofunctional materials offer (almost) unlimited possibilities and opportunities to address challenging biomedical problems. Rational molecular design of supramolecular biofunctional materials exploit powerful and versatile noncovalent interactions, which offer many advantages, such as responsiveness, reversibility, tunability, biomimicry, modularity, predictability, and, most importantly, adaptiveness...
March 12, 2017: Biomaterials
https://www.readbyqxmd.com/read/28318093/synthesis-of-imidazo-1-2-a-pyridines-c-h-functionalization-in-the-direction-of-c-s-bond-formation
#12
REVIEW
Chitrakar Ravi, Subbarayappa Adimurthy
Imidazo[1,2-a]pyridines play an important role in medicinal chemistry. In spite of very drastic developments on syntheses and functionalization in this area, the use of inexpensive catalysts and mild reaction conditions constitutes an important role in pharmaceutical applications. This account describes our recent efforts on the development of new methods for the synthesis of imidazo[1,2-a]pyridines using readily available starting substrates and catalysts under very mild reaction conditions. In the direction of enhancement of biological activity, we also described the synthesis of functionalized imidazo [1,2-a]pyridine derivatives...
March 20, 2017: Chemical Record: An Official Publication of the Chemical Society of Japan ... [et Al.]
https://www.readbyqxmd.com/read/28314411/small-molecule-inhibition-of-interleukin-1-receptor-associated-kinase-4-irak4
#13
N E Genung, K M Guckian
In recent years, interleukin-1 receptor-associated kinase 4, IRAK4, has become an attractive target for many medicinal chemistry programmes. Target inhibition is of potential therapeutic value in areas including autoimmune disorders, cancer, inflammatory diseases, and possibly neurodegenerative diseases. Results from high-throughput screening efforts have led, in conjunction with structure-based drug design, to the identification of highly potent and selective small molecule IRAK4 inhibitors from many diverse chemical series...
2017: Progress in Medicinal Chemistry
https://www.readbyqxmd.com/read/28302468/spectroscopic-electrochemical-and-molecular-docking-study-of-the-binding-interaction-of-a-small-molecule-5h-naptho-2-1-f-1-2-oxathieaphine-2-2-dioxide-with-calf-thymus-dna
#14
Abhijit Mukherjee, Shovan Mondal, Bula Singh
The interaction of 5H-naptho[2,1-f][1,2]oxathieaphine2,2-dioxide (NOTD) with calf thymus DNA in Tris-HCl buffer at physiological pH was investigated with the help of various spectroscopic and electrochemical methods along with molecular docking study. Studying the non-covalent binding interaction of a neutral fluorophore with ctDNA has become an active field of research at the interface between medicinal chemistry and biological science. NOTD is known for its various toxicological, skin sensitization, and antiviral properties...
March 13, 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/28300061/iridium-catalysed-regioselective-borylation-of-carboranes-via-direct-b-h-activation
#15
Ruofei Cheng, Zaozao Qiu, Zuowei Xie
Carboranes are carbon-boron molecular clusters, which can be viewed as three-dimensional analogues to benzene. They are finding many applications in medicine, materials and organometallic chemistry. On the other hand, their exceptional thermal and chemical stabilities, as well as 3D structures, make them very difficult to be functionalized, in particular the regioselective functionalization of BH vertex among ten similar B-H bonds. Here we report a very efficient iridium-catalysed borylation of cage B(3,6)-H bonds of o-carboranes with excellent yields and regioselectivity using bis(pinacolato)diboron (B2pin2) as a reagent...
March 16, 2017: Nature Communications
https://www.readbyqxmd.com/read/28299742/virtual-high-throughput-screening-for-matrix-metalloproteinase-inhibitors
#16
Jun Yong Choi, Rita Fuerst
Structure-based virtual screening (SBVS) is a common method for the fast identification of hit structures at the beginning of a medicinal chemistry program in drug discovery. The SBVS, described in this manuscript, is focused on finding small molecule hits that can be further utilized as a starting point for the development of inhibitors of matrix metalloproteinase 13 (MMP-13) via structure-based molecular design. We intended to identify a set of structurally diverse hits, which occupy all subsites (S1'-S3', S2, and S3) centering the zinc containing binding site of MMP-13, by the virtual screening of a chemical library comprising more than ten million commercially available compounds...
2017: Methods in Molecular Biology
https://www.readbyqxmd.com/read/28295709/ring-expansion-reactions-in-the-synthesis-of-macrocycles-and-medium-sized-rings
#17
James Robert Donald, William Paul Unsworth
Functionalised macrocycles and medium-sized rings have applications in a number of scientific fields, ranging from medicinal chemistry and supramolecular chemistry, to catalysis and nanotechnology. However, their value in these areas can be undermined by a simple, but important limitation: large ring systems are very often difficult to make. Traditional end-to-end cyclisation reactions of long linear precursors are typically unpredictable and impractical processes, mainly due to unfavourable enthalpic and entropic factors...
March 15, 2017: Chemistry: a European Journal
https://www.readbyqxmd.com/read/28295448/drug-rechallenge-following-drug-induced-liver-injury
#18
REVIEW
Christine M Hunt, Julie I Papay, Vid Stanulovic, Arie Regev
Drug induced hepatocellular injury is identified internationally by ALT 5x upper limits normal (ULN) appearing within 3 months of drug initiation, after alternative causes are excluded. Upon withdrawing the suspect drug, ALT generally decreases by 50% or more. With drug readministration, a positive rechallenge has recently been defined by an ALT 3-5xULN or greater. Nearly 50 drugs are associated with positive rechallenge after drug-induced liver injury (DILI): antimicrobials, central nervous system, cardiovascular and oncology therapeutics...
March 13, 2017: Hepatology: Official Journal of the American Association for the Study of Liver Diseases
https://www.readbyqxmd.com/read/28292015/evaluation-of-antioxidant-and-anticancer-activity-of-copper-oxide-nanoparticles-synthesized-using-medicinally-important-plant-extracts
#19
Dilaveez Rehana, D Mahendiran, R Senthil Kumar, A Kalilur Rahiman
Copper oxide (CuO) nanoparticles were synthesized by green chemistry approach using different plant extracts obtained from the leaves of Azadirachta indica, Hibiscus rosa-sinensis, Murraya koenigii, Moringa oleifera and Tamarindus indica. In order to compare their efficiency, the same copper oxide nanoparticles was also synthesized by chemical method. Phytochemical screening of the leaf extracts showed the presence of carbohydrates, flavonoids, glycosides, phenolic compounds, saponins, tannins, proteins and amino acids...
March 10, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28289374/discovery-of-compounds-that-positively-modulate-the-high-affinity-choline-transporter
#20
Parul Choudhary, Emma J Armstrong, Csilla C Jorgensen, Mary Piotrowski, Maria Barthmes, Rubben Torella, Sarah E Johnston, Yuya Maruyama, John S Janiszewski, R Ian Storer, Sarah E Skerratt, Caroline L Benn
Cholinergic hypofunction is associated with decreased attention and cognitive deficits in the central nervous system in addition to compromised motor function. Consequently, stimulation of cholinergic neurotransmission is a rational therapeutic approach for the potential treatment of a variety of neurological conditions. High affinity choline uptake (HACU) into acetylcholine (ACh)-synthesizing neurons is critically mediated by the sodium- and pH-dependent high-affinity choline transporter (CHT, encoded by the SLC5A7 gene)...
2017: Frontiers in Molecular Neuroscience
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