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https://www.readbyqxmd.com/read/28102941/synthesis-of-primaquine-glyco-conjugates-as-potential-tissue-schizontocidal-antimalarial-agents
#1
Chandra S Azad, Mridula Saxena, Arif J Siddiqui, Jyoti Bhardwaj, Sunil K Puri, Guru P Dutta, Nity Anand, Anil K Saxena
Primaquine (PQ) is the only drug used to prevent relapse of malaria due to P. vivax and P. ovale, by eradicating the dormant liver form of the parasite (hypnozoites). The side effects associated with PQ limits is uses in treatment of malaria. To overcome the premature oxidative deamination and to increase the life span of drug in the biological system the novel glyco-conjugates of PQ were synthesized by coupling of primaquine with hexoses in phosphate buffer. The saccharide part of the hybrid molecules thought to be direct the drug to the liver, where hypnozoites resides...
January 19, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28102767/synthesis-stereochemical-characterization-and-antimicrobial-evaluation-of-a-potentially-nonnephrotoxic-3-c-acethydrazide-puromycin-analog
#2
Josh Carter, Blair A Weaver, Maria A Chiacchio, Amy R Messersmith, Will E Lynch, Brent D Feske, Giuseppe Gumina
Puromycin is a peptidyl nucleoside endowed with significant antibiotic and anticancer properties, but also with an unfortunate nephrotoxic character that has hampered its use as a chemotherapeutic agent. Since hydrolysis of puromycin's amide to puromycin aminonucleoside is the first metabolic step leading to nephrotoxicity, we designed a 3'-C-hydrazide analog where the nitrogen and carbon functionality around the amide carbonyl of puromycin are inverted. The title compound, synthesized in 11 steps from D-xylose, cannot be metabolized to the nephrotoxic aminonucleoside...
January 19, 2017: Nucleosides, Nucleotides & Nucleic Acids
https://www.readbyqxmd.com/read/28102676/novel-antitumor-platinum-ii-conjugates-containing-the-nonsteroidal-anti-inflammatory-agent-diclofenac-synthesis-and-dual-mechanisms-of-antiproliferative-effects
#3
Francesco Paolo Intini, Juraj Zajac, Vojtech Novohradsky, Teresa Saltarella, Concetta Pacifico, Viktor Brabec, Giovanni Natile, Jana Kasparkova
One concept how to improve anticancer effects of conventional metallodrugs consists in conjugation of these compounds with other biologically (antitumor) active agents, acting by a different mechanism. Here, we present synthesis, biological effects, and mechanisms of action of new Pt(II) derivatives containing one or two nonsteroidal anti-inflammatory diclofenac (DCF) ligands also known for their antitumor effects. The antiproliferative properties of these metallic conjugates show that these compounds are potent and cancer cell selective cytotoxic agents exhibiting activity in cisplatin resistant and the COX-2 positive tumor cell lines...
January 19, 2017: Inorganic Chemistry
https://www.readbyqxmd.com/read/28102546/ataluren-and-similar-compounds-specific-therapies-for-premature-termination-codon-class-i-mutations-for-cystic-fibrosis
#4
REVIEW
Aisha A Aslam, Colin Higgins, Ian P Sinha, Kevin W Southern
BACKGROUND: Cystic fibrosis is a common life-shortening genetic disorder in the Caucasian population (less common in other ethnic groups) caused by the mutation of a single gene that codes for the production of the cystic fibrosis transmembrane conductance regulator protein. This protein coordinates the transport of salt (and bicarbonate) across cell surfaces and the mutation most notably affects the airways. In the lungs of people with cystic fibrosis, defective protein results in a dehydrated surface liquid and compromised mucociliary clearance...
January 19, 2017: Cochrane Database of Systematic Reviews
https://www.readbyqxmd.com/read/28102474/anti-amnestic-effect-of-curcumin-in-combination-with-donepezil-an-anticholinesterase-drug-involvement-of-cholinergic-system
#5
Ayodele Jacob Akinyemi, Ganiyu Oboh, Sunday Idowu Oyeleye, Opeyemi Ogunsuyi
Recently, combination therapy involving cholinesterase (ChE) inhibitor with other neuroprotective agents has shown better desirable effect in the management/prevention of dementia but limited information is available on their effect with dietary polyphenols. Hence, this study sought to assess the combined pretreatment effect of curcumin, the major polyphenolic compound of turmeric (Curcuma longa) rhizomes, with donepezil, a cholinesterase inhibitor, on cognitive function in scopolamine-induced memory impairment in rats...
January 19, 2017: Neurotoxicity Research
https://www.readbyqxmd.com/read/28102412/organobase-catalyzed-1-2-brook-rearrangement-of-silyl-glyoxylates
#6
Man-Yi Han, Fei-Yan Yang, Di Zhou, Zhigang Xu
A highly efficient [1,2]-Brook rearrangement of silyl glyoxylates has been developed using DBU as the organobase-catalyst. This [1,2]-Brook rearrangement is applicable to a number of thiols and secondary phosphine oxides containing acidic protons. These nucleophiles afford the corresponding Brook products in high yields. Using this methodology, a formal synthesis of anti-HIV drug compound lamivudine was realized.
January 19, 2017: Organic & Biomolecular Chemistry
https://www.readbyqxmd.com/read/28101577/viscumins-functionally-modulate-cell-motility-associated-gene-expression
#7
Sonja Schötterl, Miriam Hübner, Angela Armento, Vivien Veninga, Naita Maren Wirsik, Simon Bernatz, Hans Lentzen, Michel Mittelbronn, Ulrike Naumann
In Europe extracts from Viscum album L., the European white-berry mistletoe, are widely used as a complementary cancer therapy. Viscumins (mistletoe lectins, ML) have been scrutinized as important active components of mistletoe and exhibit a variety of anticancer effects such as stimulation of the immune system, induction of cytotoxicity, reduction of tumor cell motility as well as changes in the expression of genes associated with cancer development and progression. By microarray expression analysis, quantitative RT-PCR and RT-PCR based validation of microarray data we demonstrate for the Viscum album extract Iscador Qu and for the lectins Aviscumine and ML-1 that in glioma cells these drugs differentially modulate the expression of genes involved in the regulation of cell migration and invasion, including processes modulating cell architecture and cell adhesion...
February 2017: International Journal of Oncology
https://www.readbyqxmd.com/read/28101455/pharmaceutical-cocrystals-regulatory-and-strategic-aspects-design-and-development
#8
REVIEW
Dipak Dilip Gadade, Sanjay Sudhakar Pekamwar
Cocrystal is a concept of the supramolecular chemistry which is gaining the extensive interest of researchers from pharmaceutical and chemical sciences and of drug regulatory agencies. The prominent reason of which is its ability to modify physicochemical properties of active pharmaceutical ingredients. During the development of the pharmaceutical product, formulators have to optimize the physicochemical properties of active pharmaceutical ingredients. Pharmaceutical cocrystals can be employed to improve vital physicochemical characteristics of a drug, including solubility, dissolution, bioavailability and stability of pharmaceutical compounds while maintaining its therapeutic activity...
December 2016: Advanced Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28101351/pro-inflammatory-effect-of-a-traditional-chinese-medicine-formula-with-potent-anti-cancer-activity-in-vitro-impedes-tumor-inhibitory-potential-in-vivo
#9
Lei Xia, Maksym Plachynta, Tangjingjun Liu, Xiao Xiao, Jialei Song, Xiaogang Li, Mu Zhang, Yao Yao, Heng Luo, Xiaojiang Hao, Yaacov Ben-David
Medicinal formulas are a part of the complex discipline of traditional Chinese medicine that has been used for centuries in China and East Asia. These formulas predominantly consist of the extracts isolated from herbal plants, animal parts and medicinal minerals. The present study aimed to investigate the impact of 150 formulas, used as non-prescription drugs in China, on the treatment of cancer. A formula was identified, C54, commonly used to treat sore throats, which exhibited marked growth inhibition in vitro, associated with cell cycle arrest and apoptosis...
December 2016: Molecular and Clinical Oncology
https://www.readbyqxmd.com/read/28101344/evaluation-of-pharmacological-relaxation-effect-of-the-natural-product-naringin-on-in-vitro-cultured-airway-smooth-muscle-cells-and-in-vivo-ovalbumin-induced-asthma-balb-c-mice
#10
Yue Wang, Yun Lu, Mingzhi Luo, Xiaohao Shi, Yan Pan, Huilong Zeng, Linhong Deng
Asthma has become a common chronic respiratory disease worldwide and its prevalence is predicted to continue increasing in the next decade, particularly in developing countries. A key component in asthma therapy is to alleviate the excessive bronchial airway narrowing ultimately due to airway smooth muscle contraction, which is often facilitated by a smooth muscle relaxant, such as the β2-adrenergic agonists. Recently, bitter taste receptor (TAS2R) agonists, including saccharin and chloroquine, have been found to potently relax the airway smooth muscle cells (ASMCs) via intracellular Ca(2+) signaling...
December 2016: Biomedical Reports
https://www.readbyqxmd.com/read/28101253/2-chromon-3-yl-imidazole-derivatives-as-potential-antimicrobial-agents-synthesis-biological-evaluation-and-molecular-docking-studies
#11
Shweta Sharma, Vishal Sharma, Gurpreet Singh, Harpreet Kaur, Shubham Srivastava, Mohan Paul S Ishar
A series of novel 2-(chromon-3-yl)-4,5-diphenyl-1H-imidazoles (4a-h) were synthesized by one pot condensation of substituted 3-formylchromones (1a-h), benzil (2) and ammonium acetate (3) in refluxing acetic acid at 110 °C under N2 atmosphere. Allylation of compounds 4a-h with allyl bromide in the presence of fused K2CO3 furnished N-allyl-2-(chromon-3-yl)-4,5-diphenyl-1H-imidazoles (6a-h). The synthesized compounds were characterized spectroscopically and evaluated for in vitro antimicrobial activity against various pathogenic bacterial and fungal strains by disc diffusion method...
January 2017: Journal of Chemical Biology
https://www.readbyqxmd.com/read/28100218/antiviral-effect-of-compounds-derived-from-the-seeds-of-mammea-americana-and-tabernaemontana-cymosa-on-dengue-and-chikungunya-virus-infections
#12
Cecilia Gómez-Calderón, Carol Mesa-Castro, Sara Robledo, Sergio Gómez, Santiago Bolivar-Avila, Fredyc Diaz-Castillo, Marlen Martínez-Gutierrez
BACKGROUND: The transmission of Dengue virus (DENV) and Chikungunya virus (CHIKV) has increased worldwide, due in part to the lack of a specific antiviral treatment. For this reason, the search for compounds with antiviral potential, either as licensed drugs or in natural products, is a research priority. The objective of this study was to identify some of the compounds that are present in Mammea americana (M. americana) and Tabernaemontana cymosa (T. cymosa) plants and, subsequently, to evaluate their cytotoxicity in VERO cells and their potential antiviral effects on DENV and CHIKV infections in those same cells...
January 18, 2017: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/28100151/renin-inhibition-by-soyasaponin-i-a-potent-native-anti-hypertensive-compound
#13
Zeinab Tavassoli, Majid Taghdir, Bijan Ranjbar
One way to control hypertension is inactivation of the Renin- Angiotensin- Aldosterone System (RAAS). Inhibition of renin as a rate-limiting step of this system is an effective way to stop up RAAS. It has been proved that soyasaponin I, an herbal compound obtained from soybeans, has anti-hypertensive effect via renin inhibition, so it has the potential of being an anti-hypertensive drug. Herein, some theoretical approaches such as Docking Simulation, Molecular Dynamics (MD) Simulation and MMPBSA analysis have been used to study how soyasaponin I inhibits renin at the structural level...
January 19, 2017: Journal of Biomolecular Structure & Dynamics
https://www.readbyqxmd.com/read/28100083/%C3%AE-glucosidase-inhibitory-activity-and-cytotoxic-effects-of-some-cyclic-urea-and-carbamate-derivatives
#14
Jelena B Popović-Djordjević, Ivana I Jevtić, Nadja Dj Grozdanić, Sandra B Šegan, Mario V Zlatović, Milovan D Ivanović, Tatjana P Stanojković
The inhibitory activities of selected cyclic urea and carbamate derivatives (1-13) toward α-glucosidase (α-Gls) in in vitro assay were examined in this study. All examined compounds showed higher inhibitory activity (IC50) against α-Gls compared to standard antidiabetic drug acarbose. The most potent was benzyl (3,4,5-trimethoxyphenyl)carbamate (12) with IC50 = 49.85 ± 0.10 µM. In vitro cytotoxicity of the investigated compounds was tested on three human cancer cell lines HeLa, A549 and MDA-MB-453 using MTT assay...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28099878/screening-verification-and-analysis-of-biomarkers-for-drug-induced-cardiac-toxicity-in-vitro-based-on-rtca-coupled-with-pcr-array-technology
#15
Lu Zhang, Meng-Xi Xu, Qing-Sheng Yin, Cai-Ying Zhu, Xue-Lian Cheng, Yi-Ran Ren, Peng-Wei Zhuang, Yan-Jun Zhang
Cardiotoxicity is one of the most serious side effects of new drugs. Early detection of the drug induced cardiotoxicity based on the biomarkers provides an important preventative strategy for detecting potential cardiotoxicity of candidate drugs. In this study, we aim to identify the predictive genomics biomarkers for drug-induced cardiac toxicity based on the RTCA coupled with PCR Array technology in primary cells. Three prototypical cardiotoxic compounds (doxorubicin, isoproterenol, ouabain) with different mechanisms were firstly real-time monitored to diagnose the cytotoxicity by using the RTCA, while the functional alterations of cardiomyocytes were also monitored by analyzing the beating frequency of cardiomyocytes...
January 15, 2017: Toxicology Letters
https://www.readbyqxmd.com/read/28099856/screening-bioactives-reveals-nanchangmycin-as-a-broad-spectrum-antiviral-active-against-zika-virus
#16
Keiko Rausch, Brent A Hackett, Nathan L Weinbren, Sophia M Reeder, Yoel Sadovsky, Christopher A Hunter, David C Schultz, Carolyn B Coyne, Sara Cherry
Zika virus is an emerging arthropod-borne flavivirus for which there are no vaccines or specific therapeutics. We screened a library of 2,000 bioactive compounds for their ability to block Zika virus infection in three distinct cell types with two different strains of Zika virus. Using a microscopy-based assay, we validated 38 drugs that inhibited Zika virus infection, including FDA-approved nucleoside analogs. Cells expressing high levels of the attachment factor AXL can be protected from infection with receptor tyrosine kinase inhibitors, while placental-derived cells that lack AXL expression are insensitive to this inhibition...
January 17, 2017: Cell Reports
https://www.readbyqxmd.com/read/28099816/new-treatment-options-and-emerging-drugs-for-axial-spondyloarthritis-biological-and-targeted-synthetic-agents
#17
Eric Toussirot
Ankylosing spondylitis (AS) and axial spondyloarthritis (ax SpA) are chronic inflammatory diseases mainly involving the axial skeleton. Pharmacological treatments for AS and ax SpA usually include local glucocorticoid injections, NSAIDs and anti-TNFa agents. Since around 30% to 40% of patients are non responders or intolerant to anti-TNFa agents, we need new therapeutic options for AS and ax SpA. Areas covered: This review describes the new biological agents that can be used or are in development for AS or ax SpA as well as emerging synthetic targeted drugs...
January 18, 2017: Expert Opinion on Pharmacotherapy
https://www.readbyqxmd.com/read/28099781/old-drug-scaffold-new-activity-thalidomide-correlated-compounds-exerting-different-effects-on-breast-cancer-cell-growth-and-progression
#18
Alessia Carocci, Alessia Catalano, Domenico Iacopetta, Maria Stefania Sinicropi
Thalidomide was firstly used as morning sickness relief in pregnant women and then withdrawn from market because of its dramatic effects on fetal normal development. Over the last decades, it has been successfully used for the care of several pathologies, including cancer. Many analogues with improved activity were synthesized and tested. Herein, we report some effects on MCF-7 and MDA-MB-231 breast cancer cells growth and progression of a small series of thalidomide correlated compounds, very effective in inducing cancer cells death by triggering TNFα-mediated apoptosis...
January 18, 2017: ChemMedChem
https://www.readbyqxmd.com/read/28099006/constituents-of-the-rhizomes-of-boesenbergia-pandurata-and-their-antiausterity-activities-against-the-panc-1-human-pancreatic-cancer-line
#19
Nhan Trung Nguyen, Mai Thanh Thi Nguyen, Hai Xuan Nguyen, Phu Hoang Dang, Dya Fita Dibwe, Hiroyasu Esumi, Suresh Awale
Human pancreatic cancer cell lines have a remarkable tolerance to nutrition starvation, which enables them to survive under a tumor microenvironment. The search for agents that preferentially inhibit the survival of cancer cells under low nutrient conditions represents a novel antiausterity strategy in anticancer drug discovery. In this investigation, a methanol extract of the rhizomes of Boesenbergia pandurata showed potent preferential cytotoxicity against PANC-1 human pancreatic cancer cells under nutrient-deprived conditions, with a PC50 value of 6...
January 18, 2017: Journal of Natural Products
https://www.readbyqxmd.com/read/28098433/synthesis-and-evaluation-of-anti-inflammatory-n-substituted-3-5-bis-2-trifluoromethyl-benzylidene-piperidin-4-ones
#20
Zixin Xie, Zaikui Zhang, Shufang Yu, Donghua Cheng, Huan Zhang, Chao Han, Handeng Lv, Faqing Ye
A total of 24 N-substituted 3,5-bis(2-(trifluoromethyl)benzylidene)piperidin-4-one derivatives were synthesized via aldol condensation, and their anti-inflammatory activities were evaluated. These compounds were found to have no significant cytotoxicity against mouse bone marrow cells in vitro. However, some compounds, such as c6 (N-(3-methylbenzoyl)-3,5-bis-(2-(trifluoromethyl)benzylidene)piperidin-4-one) and c10 (N-(2-chlorobenzoyl)-3,5-bis-(2-(trifluoromethyl)benzylidene)piperidin-4-one), displayed potent anti-inflammatory activity by inhibiting lipopolysaccharide (LPS)-stimulated tumor necrosis factor (TNF)-α, interleukin-6 (IL-6), IL-1β, prostaglandin E2 (PGE2), and nitric oxide (NO) production in RAW 264...
January 18, 2017: ChemMedChem
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