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Medicinal chemistry

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https://www.readbyqxmd.com/read/28211307/local-and-systemic-changes-associated-with-long-term-percutaneous-static-implantation-of-titanium-alloys-in-rhesus-macaques-macaca-mulatta
#1
Galit H Frydman Robert P Marini Vasudevan Bakthavatchalu Kathleen E Biddle Sureshkumar Muthupalani Charles R Vanderburg Barry Lai Pavan K Bendapudi Ronald G Tompkins And James G Fox
Metal alloys are frequently used as implant materials in veterinary medicine. Recent studies suggest that many alloys induce both local and systemic inflammatory responses. In this study, 37 rhesus macaques with long-term skull-anchored percutaneous titanium alloy implants (duration, 0 to 14 y) were evaluated for changes in their hematology, coagulation, and serum chemistry profiles. Negative controls (n = 28) did not have implants. Macaques with implants had higher plasma D-dimer and lower antithrombin III concentrations than nonimplanted animals...
February 16, 2017: Comparative Medicine
https://www.readbyqxmd.com/read/28210931/serotonin-syndrome-from-5-hydroxytryptophan-supplement-ingestion-in-a-9-month-old-labrador-retriever
#2
Hopkins Jennifer, Pardo Mariana, Bischoff Karyn
INTRODUCTION: 5-Hydroxytryptophan (5-HTP) supplements are available over the counter and labeled as sleeping aids and anxiolytics for human use. 5-HTP is a serotonin precursor and overdose can lead to serotonin syndrome. CASE REPORT: A 9-month-old female Labrador retriever was evaluated after ingestion of a 5-HTP supplement. Signs of agitation developed within 1 h of ingestion, and emesis was attempted by the owner with  3% hydrogen peroxide (H2O2) orally. On presentation, the dog was obtunded, bilaterally mydriatic and salivating...
February 16, 2017: Journal of Medical Toxicology: Official Journal of the American College of Medical Toxicology
https://www.readbyqxmd.com/read/28205403/functionalized-calix-4-arenes-as-potential-therapeutic-agents
#3
Muhammad Moazzam Naseer, Mukhtiar Ahmed, Shahid Hameed
Calixarenes, composed of phenolic units linked by methylene bridges at the 2,6-positions, represent a versatile class of macrocyclic compounds in supramolecular chemistry that can host small molecules or ions in their well-defined hydrophobic cavities. In recent years, it has been recognized that this class of compounds has the potential to serve as platform for the design of biological active compounds. Therefore, the calixarenes functionalized with different pharmacophoric groups have been synthesized as target structure by many researchers and were further evaluated for their biological activities...
February 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28205401/computer-aided-drug-design-to-explore-cyclodextrin-therapeutics-and-biomedical-applications
#4
Azizeh Abdolmaleki, Fatemeh Ghasemi, Jahan B Ghasemi
Cyclodextrin (CD) is a subset of the macrocyclic structural class, which is an important class of small organic agents that are useful functional excipients. They have wide range application possibilities in different fields of sciences such as material preparation, medicine, analytical chemistry, and separation processes. They are used widely in pharmaceutical formulations and drug delivery for increasing the water solubility of low soluble drugs and drug candidates. Due to the ring structure, they behave differently than smaller molecules and may be capable of hitting new classes of targets...
February 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28198919/natural-compounds-from-mexican-medicinal-plants-as-potential-drug-leads-for-anti-tuberculosis-drugs
#5
Rocio Gómez-Cansino, Silvia Laura Guzmán-Gutiérrez, María Guadalupe Campos-Lara, Clara Ines Espitia-Pinzón, Ricardo Reyes-Chilpa
In Mexican Traditional Medicine 187 plant species are used in the treatment of respiratory conditions that may be associated with tuberculosis. In this contribution, we review the ethnobotany, chemistry and pharmacology of 63 species whose extracts have been assayed for antimycobacterial activity in vitro. Among these, the most potent is Aristolochia brevipes (MIC= 12.5 µg/mL), followed by Aristolochia taliscana, Citrus sinensis, Chrysactinia mexicana, Persea americana, and Olea europaea (MIC<64 µg/mL)...
February 9, 2017: Anais da Academia Brasileira de Ciências
https://www.readbyqxmd.com/read/28198622/a-cell-penetrant-manganese-superoxide-dismutase-mnsod-mimic-is-able-to-complement-mnsod-and-exerts-an-antiinflammatory-effect-on-cellular-and-animal-models-of-inflammatory-bowel-diseases
#6
Emilie Mathieu, Anne-Sophie Bernard, Nicolas Delsuc, Elodie Quévrain, Géraldine Gazzah, Barry Lai, Florian Chain, Philippe Langella, Maria Bachelet, Joelle Masliah, Philippe Seksik, Clotilde Policar
Inorganic complexes are increasingly used for biological and medicinal applications, and the question of the cell penetration and distribution of metallodrugs is key to understanding their biological activity. Oxidative stress is known to be involved in inflammation and in inflammatory bowel diseases for which antioxidative defenses are weakened. We report here the study of the manganese complex Mn1 mimicking superoxide dismutase (SOD), a protein involved in cell protection against oxidative stress, using an approach in inorganic cellular chemistry combining the investigation of Mn1 intracellular speciation using mass spectrometry and of its quantification and distribution using electron paramagnetic resonance and spatially resolved X-ray fluorescence with evaluation of its biological activity...
February 15, 2017: Inorganic Chemistry
https://www.readbyqxmd.com/read/28197301/intramolecular-hydrogen-bond-expectations-in-medicinal-chemistry
#7
EDITORIAL
Fabrizio Giordanetto, Christian Tyrchan, Johan Ulander
Design strategies centered on intramolecular hydrogen bonds are sometime used in drug discovery, but their general applicability has not been addressed beyond scattered examples or circumstantial evidence. A total of 1053 matched molecular pairs where only one of the two molecules is able to form an intramolecular hydrogen bond via monatomic transformations have been identified across the ChEMBL database. These pairs were used to investigate the effect of intramolecular hydrogen bonds on biological activity...
February 9, 2017: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28195724/a-drug-of-such-damned-nature-challenges-and-opportunities-in-translational-platinum-drug-research
#8
Dorian M Cheff, Matthew D Hall
The platinum-based anti-cancer agents cisplatin, carboplatin and oxaliplatin, represent a spectacular translational science achievement. The basic research observations that led to the discovery of Pt complexes as DNA-binding agents that elicit cell arrest, the pre-clinical tumor regression studies, and the inorganic medicinal chemistry that led to clinical implementation of effective platinum complexes in the clinic, have fueled multi-disciplinary research into platinum-based drugs. While the successes are clear and the research activity continues, a significant window of time has passed since a new Pt drug has been approved for clinical use...
February 14, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28187957/discovery-of-n-2-aminoethyl-n-benzyloxyphenyl-benzamides-new-potent-trypanosoma-brucei-inhibitors
#9
Andriy Buchynskyy, J Robert Gillespie, Matthew A Hulverson, Joshua McQueen, Sharon A Creason, Ranae M Ranade, Nicole A Duster, Michael H Gelb, Frederick S Buckner
A phenotypic screen of a compound library for antiparasitic activity on Trypanosoma brucei, the causative agent of Human African Trypanosomiasis (HAT), led to the identification of N-(2-aminoethyl)-N-phenyl benzamides as a starting point for hit-to-lead medicinal chemistry. Eighty two analogues were prepared, which led to the identification of a set of highly potent N-(2-aminoethyl)-N-benzyloxyphenyl benzamides with the most potent compound 73 having an in vitro EC50=0.001μM. The compounds displayed drug-like properties when tested in a number of in vitro assays...
November 12, 2016: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28185540/medicinal-chemistry-approaches-of-controlling-gastrointestinal-side-effects-of-non-steroidal-anti-inflammatory-drugs-endogenous-protective-mechanisms-and-drug-design
#10
Paraskevi Tziona, Panagiotis Theodosis-Nobelos, Eleni A Rekka
BACKGROUND: Non steroidal anti-inflammatory drugs are of the oldest and most widely used medicines. However, their untoward effects, especially gastrointestinal toxicity, remain the main obstacle to their application. Because of their mechanism of action, cycloxygenase (COX) inhibition, in combination with the weekly acidic character of most of them, major protective mechanisms of the gastrointestinal system are suppressed and deregulated. OBJECTIVE: In this review, several compounds designed to retain anti-inflammatory activity, but devoid of gastrointestinal side effects, are presented...
February 9, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/28183645/synthesis-of-e7-peptide-modified-biodegradable-polyester-with-the-improving-affinity-to-mesenchymal-stem-cells
#11
Qian Li, Dongming Xing, Lie Ma, Changyou Gao
As the most promising stem cell, bone marrow-derived mesenchymal stem cells (BMSCs) has attracted many attentions and applied widely in regenerative medicine. A biodegradable polyester with tunable affinity to BMSCs plays critical role in determining the properties of the BMSCs-based constructs. In this study, maleimide functionalized biodegradable polyester (P(MTMC-LA)) was synthesized through ring-opening copolymerization between l-lactide (LA) and furan-maleimide functionalized trimethylene carbonate (FMTMC) and a subsequent retro Diels-Alder reaction...
April 1, 2017: Materials Science & Engineering. C, Materials for Biological Applications
https://www.readbyqxmd.com/read/28182989/6-cyclohexylmethyl-3-hydroxypyrimidine-2-4-dione-as-an-inhibitor-scaffold-of-hiv-reverase-transcriptase-impacts-of-the-3-oh-on-inhibiting-rnase-h-and-polymerase
#12
Jing Tang, Karen A Kirby, Andrew D Huber, Mary C Casey, Juan Ji, Daniel J Wilson, Stefan G Sarafianos, Zhengqiang Wang
3-Hydroxypyrimidine-2,4-dione (HPD) represents a versatile chemical core in the design of inhibitors of human immunodeficiency virus (HIV) reverse transcriptase (RT)-associated RNase H and integrase strand transfer (INST). We report herein the design, synthesis and biological evaluation of an HPD subtype (4) featuring a cyclohexylmethyl group at the C-6 position. Antiviral testing showed that most analogues of 4 inhibited HIV-1 in the low nanomolar to submicromolar range, without cytotoxicity at concentrations up to 100 μM...
January 30, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28182577/expressing-analytical-performance-from-multi-sample-evaluation-in-laboratory-eqa
#13
Marc H M Thelen, Rob T P Jansen, Cas W Weykamp, Herman Steigstra, Ron Meijer, Christa M Cobbaert
BACKGROUND: To provide its participants with an external quality assessment system (EQAS) that can be used to check trueness, the Dutch EQAS organizer, Organization for Quality Assessment of Laboratory Diagnostics (SKML), has innovated its general chemistry scheme over the last decade by introducing fresh frozen commutable samples whose values were assigned by Joint Committee for Traceability in Laboratory Medicine (JCTLM)-listed reference laboratories using reference methods where possible...
February 9, 2017: Clinical Chemistry and Laboratory Medicine: CCLM
https://www.readbyqxmd.com/read/28181080/madurastatin-b3-a-rare-aziridine-derivative-from-actinomycete-nocardiopsis-sp-ls150010-with-potent-anti-tuberculosis-activity
#14
Xinjun Zhang, Hongtao He, Rong Ma, Zengchun Ji, Qi Wei, Huanqin Dai, Lixin Zhang, Fuhang Song
Since the discovery of the first antibiotic, natural products have played an important role in chemistry, biology and medicine. To explore the potential of bioactive compounds from microbes isolated from the southeast of Tibet, China, a crude extract library was constructed and screened against Staphylococcus aureus. The strain Nocardiopsis sp. LS150010 was scaled up and subjected to further chemical studies, resulting in the identification of N-salicyloyl-2-aminopropan-1,3-diol (2) and its rare aziridine derivative, madurastatin B3 (1)...
February 8, 2017: Journal of Industrial Microbiology & Biotechnology
https://www.readbyqxmd.com/read/28178358/substrate-analogous-inhibitors-exert-antimalarial-action-by-targeting-the-plasmodium-lactate-transporter-pffnt-at-nanomolar-scale
#15
André Golldack, Björn Henke, Bärbel Bergmann, Marie Wiechert, Holger Erler, Alexandra Blancke Soares, Tobias Spielmann, Eric Beitz
Resistance against all available antimalarial drugs calls for novel compounds that hit unexploited targets in the parasite. Here, we show that the recently discovered Plasmodium falciparum lactate/proton symporter, PfFNT, is a valid druggable target, and describe a new class of fluoroalkyl vinylogous acids that potently block PfFNT and kill cultured parasites. The original compound, MMV007839, is derived from the malaria box collection of potent antimalarials with unknown targets and contains a unique internal prodrug principle that reversibly switches between a lipophilic transport form and a polar, substrate-analogous active form...
February 2017: PLoS Pathogens
https://www.readbyqxmd.com/read/28176326/identification-of-novel-inhibitors-of-the-amino-acid-transporter-b-0-at1-slc6a19-a-potential-target-to-induce-protein-restriction-and-to-treat-type-2-diabetes
#16
Qi Cheng, Nishank Shah, Angelika Bröer, Stephen Fairweather, Yang Jiang, Dieter Schmoll, Ben Corry, Stefan Bröer
BACKGROUND AND PURPOSE: The neutral amino acid transporter B(0) AT1 (SLC6A19) has recently been identified as a possible target to treat type 2 diabetes and related disorders. B(0) AT1 mediates the Na(+) -dependent uptake of all neutral amino acids. For surface expression and catalytic activity, B(0) AT1 requires coexpression of collectrin (TMEM27). In this study, we established tools to identify and evaluate novel inhibitors of B(0) AT1. EXPERIMENTAL APPROACH: A CHO-based cell line was generated, stably expressing collectrin and B(0) AT1...
February 8, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28171830/a-review-on-antioxidant-potential-of-bioactive-heterocycle-benzofuran-natural-and-synthetic-derivatives
#17
REVIEW
Karam Chand, Rajeshwari, Asha Hiremathad, Mahak Singh, M Amelia Santos, Rangappa S Keri
The majority of heterocycle compounds and typically common heterocycle fragments present in most pharmaceuticals currently marketed, alongside with their intrinsic versatility and unique physicochemical properties, have poised them as true cornerstones of medicinal chemistry. In this context, oxygen heterocycles exhibit diverse biological and pharmacological activities due in part to the similarities with many natural and synthetic molecules with known biological activity. Among oxygen containing heterocycles, benzofuran (synthetic and natural isolated) and its derivatives have attracted medicinal chemists and pharmacologists due to their pronounced biological activities and their potential applications as pharmacological agents such as antioxidant, antitumor, antiplatelet, antimalarial, antiinflammatory, antidepressant and anticonvulsant properties...
November 18, 2016: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/28164761/mitogen-activated-protein-kinase-mapk-interacting-kinases-1-and-2-mnk1-and-mnk2-as-targets-for-cancer-therapy-recent-progress-in-the-development-of-mnk-inhibitors
#18
Agnieszka Dreas, Maciej Mikulski, Mariusz Milik, Charles-Henry Fabritius, Krzysztof Brzózka, Tomasz Rzymski
BACKGROUND: MNK1 and MNK2 are MAP kinase-interacting serine/threonine kinases, which are activated by RAS and MAPK signaling pathways and are involved in regulation of protein translation. Both kinases phosphorylate translation initiation factor eIF4E on a conserved serine 209. Overactivated eIF4E can act as an oncogene and contribute to the transformation both in vitro and in vivo and is highly expressed in diverse types of cancer. Interestingly, knockout mice that lack both Mnk1 and Mnk2 do not have any apparent phenotype...
February 3, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28164758/angiotensin-peptides-as-at2-receptor-agonists
#19
Mathias Hallberg, Jonas Sävmarker, Anders Hallberg
In 2004, the first nonpeptide selective angiotensin II type 2 receptor (AT2R) agonist was reported. This nonpeptide (C21), which, exerts anti-inflammatory and antifibrotic actions in vivo, has been extensively explored and is currently in clinical trials. Subsequently, a large number of related drug-like AT2R agonists have been disclosed. Reviews that summarize known structure-activity relationships (SAR) of nonpeptide AT2R agonists have recently appeared in the literature; however, very few reviews discuss the role of angiotensin peptides as AT2R agonists...
February 3, 2017: Current Protein & Peptide Science
https://www.readbyqxmd.com/read/28164756/integrin-targeted-peptide-and-peptidomimetic-drug-conjugates-for-the-treatment-of-tumors
#20
Daniela Arosio, Leonardo Manzoni, Cristina Corno, Paola Perego
BACKGROUND: Integrins are heterodimeric cell surface receptors that mediate cell-cell and cell-extracellular matrix adhesion. These molecules play a role in processes such as cell growth and proliferation, differentiation, migration, cell trafficking, besides contributing to angiogenesis and tumor development. Given their biological role, integrins have been proposed as amenable targets in medicinal chemistry. In particular, ανβ3, ανβ5, ανβ6 and α5β1, integrins involved in tumor angiogenesis and metastasis, have been the subject of studies aimed at the discovery of novel cancer therapeutics...
February 3, 2017: Recent Patents on Anti-cancer Drug Discovery
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