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Medicinal chemistry

James C Courtenay, Ram I Sharma, Janet L Scott
Tissue engineering is a rapidly advancing field in regenerative medicine, with much research directed towards the production of new biomaterial scaffolds with tailored properties to generate functional tissue for specific applications. Recently, principles of sustainability, eco-efficiency and green chemistry have begun to guide the development of a new generation of materials, such as cellulose, as an alternative to conventional polymers based on conversion of fossil carbon (e.g., oil) and finding technologies to reduce the use of animal and human derived biomolecules (e...
March 14, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Jin-Kyoung Yang, Eunjin Lee, In-Jun Hwang, DaBin Yim, Juhee Han, Yoon-Sik Lee, Jong-Ho Kim
The regulation of tyrosinase activity and reactive oxygen species is of great importance for the prevention of dermatological disorders in the fields of medicine and cosmetics. Herein, we report a strategy based on solid-phase peptide chemistry for the synthesis of β-lactoglobulin peptide fragment/caffeic acid (CA) conjugates (CA-Peps) with dual activities of tyrosinase inhibition and antioxidation. The purity of the prepared conjugates, CA-MHIR, CA-HIRL, and CA-HIR significantly increased to 99%, as acetonide-protected CA was employed in solid-phase coupling reactions on Rink amide resins...
March 13, 2018: Bioconjugate Chemistry
Pramod Singh Negi, Jitendra Singh, Geeta Joshi Nee Pant, Msm Rawat
Nitrogen containing five membered heterocyclics play vital role in pharmaceuticals as well as medicinal chemistry. Pyrazolines play a significant role among other heterocycles because of their therapeutic and pharmacological properties. 2-Pyrazolines displayed a wide variety of biological activities such as anticancer, antiepileptic, anti-aids, antimalarial, insecticidal and antitubercular etc. and they are used as pesticides, herbicides, fungicides and also used in agrochemical research and analytical chemistry...
March 13, 2018: Anti-cancer Agents in Medicinal Chemistry
Peter Hertelendy, Jozsef Toldi, Ferenc Fulop, Laszlo Vecsei
Ischemic stroke is one of the leading causes of mortality and permanent disability in developed countries. Stroke induces massive glutamate release, which in turn causes N-Methyl-D-aspartate (NMDA) receptor over-excitation and thus calcium overload in neurons leading to cell death via apoptotic cascades. The kynurenine pathway is a complex enzymatic cascade of tryptophan catabolism, generating various neuroactive metabolites. One metabolite, kynurenic acid (KYNA), is a potent endogenous NMDA glutamate receptor antagonist, making it a possible therapeutic tool to decrease excitotoxicity and neuroinflammation...
March 12, 2018: Current Medicinal Chemistry
Danielle H Dube
"Drug Discovery" is a 13-week lecture and laboratory-based course that was developed to introduce non-science majors to foundational chemistry and biochemistry concepts as they relate to the unifying theme of drug discovery. The first part of this course strives to build students' understanding of molecules, their properties, the differences that enable them to be separated from one another, and their abilities to bind to biological receptors and elicit physiological effects. After building students' molecular worldview, the course then focuses on four classes of drugs: antimicrobials, drugs that affect the mind, steroid-based drugs, and anti-cancer drugs...
March 12, 2018: Biochemistry and Molecular Biology Education
Andrea Tesija Kuna, Kristina Dukic, Nora Nikolac Gabaj, Marijana Miler, Ines Vukasovic, Sanja Langer, Ana-Maria Simundic, Nada Vrkic
Objective: To compare the analytical performances of the enzymatic method (EM) and capillary electrophoresis (CE) for hemoglobin A1c (HbA1c) measurement. Methods: Imprecision, carryover, stability, linearity, method comparison, and interferences were evaluated for HbA1c via EM (Abbott Laboratories, Inc) and CE (Sebia). Results: Both methods have shown overall within-laboratory imprecision of less than 3% for International Federation of Clinical Chemistry and Laboratory Medicine (IFCC) units (<2% National Glycohemoglobin Standardization Program [NGSP] units)...
March 8, 2018: Laboratory Medicine
Shi-Jun Liu, Zhi-Shu Tang, Zhi-Xin Liao, Chun-Li Cui, Hong-Bo Liu, Yan-Ni Liang, Yu Zhang, Hong-Bo Xu, Dong-Bo Zhang, Ya-Ting Zheng, Huan-Xian Shi, Shi-Ying Li
ETHNOPHARMACOLOGICAL RELEVANCE: Ligularia przewalskii (Maxim.) Diels (LP) (called zhangyetuowu in Chinese), is generally found in moist forest areas in the western regions of China. The root, leaves and flower of LP are utilized as a common traditional medicine in China. It has been utilized conventionally in herbal remedies for the remedy of haemoptysis, asthma, pulmonary phthisis, jaundice hepatitis, food poisoning, bronchitis, cough, fever, wound healing, measles, carbuncle, swelling and phlegm diseases...
March 8, 2018: Journal of Ethnopharmacology
Zijian Guo, Jing Zhao
No abstract text is available yet for this article.
April 2018: Current Opinion in Chemical Biology
Cássio S Meira, José Maurício Dos Santos Filho, Caroline C Sousa, Pâmela S Anjos, Jéssica V Cerqueira, Humberto A Dias Neto, Rafael G da Silveira, Helena M Russo, Jean-Luc Wolfender, Emerson F Queiroz, Diogo R M Moreira, Milena B P Soares
4-(Nitrophenyl)hydrazone derivatives of N-acylhydrazone were synthesized and screened for suppress lymphocyte proliferation and nitrite inhibition in macrophages. Compared to an unsubstituted N-acylhydrazone, active compounds were identified within initial series when hydroxyl, chloride and nitro substituents were employed. Structure-activity relationship was further developed by varying the position of these substituents as well as attaching structurally-related substituents. Changing substituent position revealed a more promising compound series of anti-inflammatory agents...
February 25, 2018: Bioorganic & Medicinal Chemistry
Mohammed Benadallah, Oualid Talhi, Fatiha Nouali, Nourredine Choukchou-Braham, Khaldoun Bachari, Artur M S Silva
The present review deals with the progress in medicinal chemistry of spirocyclic compounds, a wider class of natural and synthetic organic molecules, defined as a hybrid of two molecular entities covalently linked via a unique tetrahedral carbon. This spiro central carbon confers to the molecules a tridimensional structurally oriented framework, which is found in many medicinally relevant compounds, a well-known example is the anti-hypertensive spironolactone. Various bioactive natural products possess the privileged spiro linkage and different chemo-types thereof become synthetically accessible since the 20th century...
March 9, 2018: Current Medicinal Chemistry
Agnieszka Zagorska, Anna Partyka, Adam Bucki, Alicja Gawalska, Anna Czopek, Maciej Pawlowski
BACKGROUND: The phosphodiesterase 10 (PDE10) family, identified in 1999, is mainly expressed in the brain, particularly in the striatum, within the medium spiny neurons, nucleus accumbens, and olfactory tubercle. Inhibitors of PDE10 (PDE10-Is) are a conceptually rational subject for medicinal chemistry with potential use in the treatment of psychiatric and neurodegenerative diseases. OBJECTIVE: This review is based on peer-reviewed published articles, and summarizes the cellular and molecular biology of PDE10 as a rational target for psychiatric and neurodegenerative drug discovery...
March 8, 2018: Current Medicinal Chemistry
Xifeng Chen, Dawei Yang, Yuguo Tang, Peng Miao
DNA endonucleases play critical roles in medicinal chemistry, which are also commonly used in molecular biology investigation. Sensitive quantification of endonuclease activity is of great significance. In this study, a reliable electrochemical approach for endonuclease activity sensing is developed with the adoption of copper nanoparticles (CuNPs) as electrochemical reporters. Firstly, a DNA duplex is designed and modified on a gold electrode, which acts as the template for the synthesis of CuNPs. Subsequently, the formed NPs are dissolved and then electrodeposited on a glassy carbon electrode for DPV measurements...
March 7, 2018: Analyst
Kodai Kato, Koji Hirano, Masahiro Miura
A CuCl/(R,R)-PTBP-BDPP-catalyzed regioselective and enantioselective aminoboration of simple and unactivated terminal alkenes with bis(pinacolato)diboron (pinB-Bpin) and hydroxylamines has been developed. The amino group and boryl group are incorporated at the internal position and terminal position, respectively, and the corresponding chiral beta-borylalkylamines are obtained with good to high enantiomeric ratios. The asymmetric copper catalysis allows for rapid and concise transformation of readily available olefinic feedstock-like materials into functionalized chiral alkylamines of high potential in medicinal and pharmaceutical chemistry...
March 7, 2018: Chemistry: a European Journal
Giuseppe Lippi, Janne Cadamuro, Alexander von Meyer, Ana-Maria Simundic
No abstract text is available yet for this article.
March 3, 2018: Clinical Biochemistry
Giulio Sergio Roi, Giovanni Mosconi, Valentina Totti, Maria Laura Angelini, Erica Brugin, Patrizio Sarto, Laura Merlo, Sergio Sgarzi, Michele Stancari, Paola Todeschini, Gaetano La Manna, Andrea Ermolao, Ferdinando Tripi, Lucia Andreoli, Gianluigi Sella, Alberto Anedda, Laura Stefani, Giorgio Galanti, Rocco Di Michele, Franco Merni, Manuela Trerotola, Daniela Storani, Alessandro Nanni Costa
AIM: To evaluate the effect of a 12-mo supervised aerobic and resistance training, on renal function and exercise capacity compared to usual care recommendations. METHODS: Ninety-nine kidney transplant recipients (KTRs) were assigned to interventional exercise (Group A; n = 52) and a usual care cohort (Group B; n = 47). Blood and urine chemistry, exercise capacity, muscular strength, anthropometric measures and health-related quality of life (HRQoL) were assessed at baseline, and after 6 and 12 mo...
February 24, 2018: World Journal of Transplantation
Viktoriia Holubnycha, Oksana Kalinkevich, Olena Ivashchenko, Maksym Pogorielov
BACKGROUND: Investigation of new effective drugs against the methicillin-resistant strains of Staphylococcus aureus (MRSA) is an urgent issue of modern medicine. Antiseptics as an alternative of antibiotics are strong, sustained, and active preparations against resistant strains and do not violate microbiocenosis. MATERIALS AND METHODS: The activity of in situ prepared chitosan-Ag nanoparticles (Ag NPs) solution with different component ratio was tested against MRSA isolated from patients...
March 2, 2018: Nanoscale Research Letters
Joseph Derosa, Miriam L O'Duill, Matthew Holcomb, Mark N Boulous, Ryan L Patman, Fen Wang, Michelle Tran-Dubé, Indrawan McAlpine, Keary M Engle
Small molecules containing cyclopropane-heteroatom linkages are commonly needed in medicinal chemistry campaigns, yet are problematic to prepare using existing methods. To address this issue, a scalable Chan-Lam cyclopropylation reaction using potassium cyclopropyl trifluoroborate has been developed. With phenol nucleophiles, the reaction effects O-cyclopropylation, whereas with 2-pyridones, 2-hydroxybenzimidazoles, and 2-aminopyridines the reaction brings about N-cyclopropylation. The transformation is catalyzed by Cu(OAc)2 and 1,10-phenanthroline and employs 1 atm O2 as the terminal oxidant...
March 2, 2018: Journal of Organic Chemistry
Anne-Mari Mustonen, Maija Määttänen, Vesa Kärjä, Katri Puukka, Jari Aho, Seppo Saarela, Petteri Nieminen
Rhabdomyolysis (destruction of striated muscle) is a novel form of mushroom poisoning in Europe and Asia indicated by increased circulating creatine kinase levels. Particular wild fungi have also been reported to induce elevated creatine kinase activities in mice. Flammulina velutipes (enokitake or winter mushroom) is one of the most actively cultivated mushroom species globally. As it is marketed as a medicinal mushroom and functional food, it is important to examine whether it could induce potentially harmful health effects similar to some previously studied edible fungi...
January 1, 2018: Experimental Biology and Medicine
Urska Kamensek, Natasa Tesic, Gregor Sersa, Maja Cemazar
Plasmids, which are currently used in interleukin 12 (IL-12) gene electrotransfer (GET) clinical trials in the USA, contain antibiotic resistance genes and are thus, according to the safety recommendation of the European Medicines Agency (EMA), not suitable for clinical trials in the EU. In the current study, our aim was to prepare an IL-12 plasmid without an antibiotic resistance gene and test its functionality and toxicity after GET in a preclinical B16F10 mouse melanoma model. The antibiotic resistance-free plasmid encoding the human IL-12 fusion gene linked to the p21 promoter, i...
February 27, 2018: Cancers
Mercedes G Montalbán, Jeannine M Coburn, A Abel Lozano-Pérez, José L Cenis, Gloria Víllora, David L Kaplan
Curcumin, extracted from the rhizome of Curcuma longa , has been widely used in medicine for centuries due to its anti-inflammatory, anti-cancer, anti-oxidant and anti-microbial effects. However, its bioavailability during treatments is poor because of its low solubility in water, slow dissolution rate and rapid intestinal metabolism. For these reasons, improving the therapeutic efficiency of curcumin using nanocarriers (e.g., biopolymer nanoparticles) has been a research focus, to foster delivery of the curcumin inside cells due to their small size and large surface area...
February 24, 2018: Nanomaterials
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