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https://www.readbyqxmd.com/read/29245088/-ghost-peak-of-clofazimine-a-solution-degradation-product-of-clofazimine-via-nucleophilic-substitution-by-nitrite-leaching-from-certain-glass-hplc-vials
#1
Jinsheng Lin, Zhenghuai Lin, Dan Li, Mengxue Feng, Qin Yang, Wenping Hu, Yang Han, Wenquan Zhu, Min Li, LuShan Yu
Analytical solutions of clofazimine drug substance stored in glass HPLC vials were found to undergo degradation at room temperature occasionally. At the time of each sample preparation, it was unpredictable if a particular solution would undergo such solution degradation. Once the degradation peak was observed in a particular vial, typically within 24h, it would keep growing until reaching a total yield of approximately 2%. By using a strategy that combines LC-PDA/UV-MSn with mechanism-based stress studies, followed by preparative HPLC separation and subsequent structure characterization by 1D and 2D NMR, the unknown peak was identified as a clofazimine nitrite ester...
November 26, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/29244080/quantification-of-methadone-and-main-metabolites-in-nails
#2
Teresa Patrícia Magalhães, Sara Cravo, Diana Dias da Silva, Ricardo Jorge Dinis-Oliveira, Carlos Afonso, Maria de Lourdes Bastos, Helena Carmo
The quantification of drugs of abuse in keratinized matrices is becoming of special relevance for monitoring consumption and for post-mortem investigations. We aimed to implement an analytical method for the simultaneous detection of morphine (MORF), 6-monoacetylmorphine (6-MAM), methadone (MET), 2-ethylidene-1,5-dimethyl-3,3-diphenylpyrrolidine (EDDP) and 2-ethyl-5-methyl-3,3-diphenylpyrrolidine (EMDP) in nails. After decontamination, the nail samples (30 mg) were submitted to an alkaline digestion followed by a two-step liquid-liquid and SPE extraction using mixed-mode cation exchange cartridges...
December 13, 2017: Journal of Analytical Toxicology
https://www.readbyqxmd.com/read/29243921/extra-sugar-on-vancomycin-new-analogues-for-combating-multidrug-resistant-staphylococcus-aureus-and-vancomycin-resistant-enterococci
#3
Dongliang Guan, Feifei Chen, Lun Xiong, Feng Tang, Faridoon Faridoon, Yunguang Qiu, Naixia Zhang, Likun Gong, Jian Li, Lefu Lan, Wei Huang
Lipophilic substitution on vancomycin is an effective strategy for development of novel vancomycin analogues against drug-resistant bacteria by enhancing bacterial cell wall interaction. However, hydrophobic structures usually led to long elimination half-life and accumulative toxicity, therefore hydrophilic fragments were also introduced to the lipo-vancomycin to regulate their PK/PD properties. Here, we synthesized a series of new vancomycin analogues carrying various sugar moieties on the 7th-amino acid phenyl ring and lipophilic substitutions on vancosamine with extensive SAR analysis...
December 15, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29243388/the-treatment-outcomes-of-antiretroviral-substitutions-in-routine-clinical-settings-in-asia-data-from-the-treat-asia-hiv-observational-database-tahod
#4
In Young Jung, David Boettiger, Wing Wai Wong, Man Po Lee, Sasisopin Kiertiburanakul, Romanee Chaiwarith, Anchalee Avihingsanon, Junko Tanuma, Nagalingeswaran Kumarasamy, Adeeba Kamarulzaman, Fujie Zhang, Pacharee Kantipong, Oon Tek Ng, Benedict Lim Heng Sim, Matthew Law, Jeremy Ross, Jun Yong Choi
INTRODUCTION: Although substitutions of antiretroviral regimen are generally safe, most data on substitutions are based on results from clinical trials. The objective of this study was to evaluate the treatment outcomes of substituting antiretroviral regimen in virologically suppressed HIV-infected patients in non-clinical trial settings in Asian countries. METHODS: The study population consisted of HIV-infected patients enrolled in the TREAT Asia HIV Observational Database (TAHOD)...
December 2017: Journal of the International AIDS Society
https://www.readbyqxmd.com/read/29242964/-bone-substitute-materials-as-local-drug-carriers-current-status-of-substitutes-of-various-origins
#5
REVIEW
K-D Kühn, C Berberich, H Bösebeck
BACKGROUND: Autologous bone grafts (autografts) are used in surgery for defect filling and impaction grafting during hip socket and femur reconstruction. Because of their superior osteoinductive capacity, autografts are considered the "gold standard" for these treatments. However, because of a better cost-benefit ratio, allografts are also often used. In the case of limited donor availability for autologous or allogenic bone grafts, bone substitute materials (BSMs) are a reasonable alternative or supplement...
December 14, 2017: Der Orthopäde
https://www.readbyqxmd.com/read/29242710/retreatment-options-following-hcv-direct-acting-antiviral-failure
#6
Autumn Zuckerman, Cody A Chastain, Susanna Naggie
Despite the excellent efficacy of direct acting antivirals (DAA) for hepatitis C virus (HCV), treatment failures do occur. Until recently, retreatment decisions after DAA failure were influenced by the number of available agents, concerns about HCV drug resistance, and lack of data regarding retreatment. Recommended treatment approaches previously depended on limited clinical trials and expert opinion. In this article, we review the current state of the evidence for HCV retreatment after DAA failure. Based on recent clinical trial data, most patients who fail HCV treatment with DAA agents now have excellent retreatment options...
December 2017: Current Treatment Options in Infectious Diseases
https://www.readbyqxmd.com/read/29238888/synthesis-and-evaluation-of-bile-acid-amides-of-formula-see-text-cyanostilbenes-as-anticancer-agents
#7
Devesh S Agarwal, Rajnish Prakash Singh, K Lohitesh, Prabhat N Jha, Rajdeep Chowdhury, Rajeev Sakhuja
A series of amino-substituted [Formula: see text]-cyanostilbene derivatives and their bile acid (cholic and deoxycholic acid) amides were designed and synthesized. A comparative study on the anticancer and antibacterial activity evaluation on the synthesized analogs was carried against the human osteosarcoma (HOS) cancer cell line, and two gram -ve (E. coli and S. typhi) and two gram [Formula: see text]ve (B. subtilis and S. aureus) bacterial strains. All the cholic acid [Formula: see text]-cyanostilbene amides showed an [Formula: see text] in the range 2-13 [Formula: see text] against human osteosarcoma cells (HOS) with the most active analog (6g) possessing an [Formula: see text] of [Formula: see text]...
December 13, 2017: Molecular Diversity
https://www.readbyqxmd.com/read/29237375/adhesive-drug-delivery-systems-based-on-polyelectrolyte-complex-nanoparticles-pec-np-for-bone-healing
#8
Martin Muller, David Vehlow, Bernhard Torger, Birgit Urban
BACKGROUND: In this contribution an overview is given on own work concerning drug loaded polyelectrolyte complex (PEC) nanoparticles (NP) used to functionalize bone substitute materials (BSM) for the therapy of bone defects associated with systemic bone diseases. In this context drug loaded PEC NP have certain advantages, which are exemplarily summarized herein. METHODS: Concerning preparative methods PEC NP were fabricated by controlled mixing of polycation and polyanion solutions and integration of charged drugs during and after mixing...
December 12, 2017: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/29236427/sharing-samples-and-generics-an-antitrust-framework
#9
Michael A Carrier
Rising drug prices are in the news. By increasing price, drug companies have placed vital, even life-saving, medicines out of the reach of consumers. In a recent development, brand firms have prevented generics even from entering the market. The ruse for this strategy involves risk-management programs known as Risk Evaluation and Mitigation Strategies ("REMS"). Pursuant to legislation enacted in 2007, the FDA requires REMS when a drug's risks (such as death or injury) outweigh its rewards. Brands have used this regime, intended to bring drugs to the market, to block generic competition...
2017: Cornell Law Review
https://www.readbyqxmd.com/read/29236079/unexpected-binding-mode-of-a-potent-indeno-1-2-b-indole-type-inhibitor-of-protein-kinase-ck2-revealed-by-complex-structures-with-the-catalytic-subunit-ck2%C3%AE-and-its-paralog-ck2%C3%AE
#10
Jennifer Hochscherf, Dirk Lindenblatt, Benedict Witulski, Robin Birus, Dagmar Aichele, Christelle Marminon, Zouhair Bouaziz, Marc Le Borgne, Joachim Jose, Karsten Niefind
Protein kinase CK2, a member of the eukaryotic protein kinase superfamily, is associated with cancer and other human pathologies and thus an attractive drug target. The indeno[1,2-b]indole scaffold is a novel lead structure to develop ATP-competitive CK2 inhibitors. Some indeno[1,2-b]indole-based CK2 inhibitors additionally obstruct ABCG2, an ABC half transporter overexpressed in breast cancer and co-responsible for drug efflux and resistance. Comprehensive derivatization studies revealed substitutions of the indeno[1,2-b]indole framework that boost either the CK2 or the ABCG2 selectivity or even support the dual inhibition potential...
December 13, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/29234968/a-cross-national-analysis-of-the-association-between-years-of-implementation-of-opioid-substitution-treatments-and-drug-related-deaths-in-europe-from-1995-to-2013
#11
Phillip L Marotta, Charlotte A McCullagh
Data at the individual-level provide evidence that opioid substitution treatment (OST) programs protect against mortality for opioid dependent populations. Prior research has not examined the merits of national implementation of opioid substitution programs for reducing mortality at the country-level. This study elucidates longitudinal associations between country-level implementation of opioid substitution treatment programs on mortality rates of drug related deaths (DRD) from 1995 to 2013 in 30 European nations...
December 12, 2017: European Journal of Epidemiology
https://www.readbyqxmd.com/read/29233614/monoterpene-indole-alkaloid-azine-derivatives-as-mdr-reversal-agents
#12
Angela Paterna, Ruttiros Khonkarn, Silva Mulhovo, Alexis Moreno, Patricia Madeira Girio, Hélène Baubichon-Cortay, Pierre Falson, Maria-José U Ferreira
Aiming at generating a library of bioactive indole alkaloid derivatives as multidrug resistance (MDR) reversers, two epimeric indole alkaloids (1 and 2) were submitted to chemical transformations, giving rise to twenty-four derivatives (5-28), bearing new aromatic or aliphatic azine moieties. The structure of the compounds was established by 1D and 2D NMR (COSY, HMBC, HMQC and NOESY) experiments. Two different strategies were employed for assessing their anti-MDR potential, namely through the evaluation of their activity as inhibitors of typical MDR ABC transporters overexpressed by cell transfection, such as ABCB1 (P-gp), ABCC1 (MRP1), and ABCG2 (BCRP), or by evaluating their ability as collateral sensitivity (CS) agents in cells overexpressing MRP1...
December 2, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/29232586/synthesis-and-biological-evaluation-of-coumarin-derivatives-containing-imidazole-skeleton-as-potential-antibacterial-agents
#13
Yang Hu, Yufeng Shen, Xiaohu Wu, Xiao Tu, Gao-Xue Wang
Emergence of multidrug-resistant bacteria causes an urgent need for new generation of antibiotics, which may have a different mechanism of inhibition or killing action from the existing. Here, we report on the design, synthesis, and biological evaluation of thirty-nine coumarin derivatives in order to solve the antibacterial resistance by targeting at the inhibition of biosynthesis pathway of fatty acids. Their antibacterial activities against Escherichia coli, Staphylococcus aureus, Streptococcus agalactiae, and Flavobacterium cloumnare are tested and action mechanism against the key enzyme in bacterial fatty acid synthesis pathway are studied...
December 5, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29231233/access-to-hepatitis-c-treatment-for-patients-in-drug-substitution-programmes-the-fight-is-far-from-over
#14
Francesco Negro, Liudmyla Maistat
No abstract text is available yet for this article.
December 12, 2017: Swiss Medical Weekly
https://www.readbyqxmd.com/read/29229762/multiple-substitutions-lead-to-increased-loop-flexibility-and-expanded-specificity-in-acinetobacter-baumannii-carbapenemase-oxa-239
#15
Thomas M Harper, Cynthia M June, Magdalena A Taracila, Robert A Bonomo, Rachel A Powers, David A Leonard
OXA-239 is a class D carbapenemase isolated from an Acinetobacter baumannii strain found in Mexico.  This enzyme is a variant of OXA-23 with three amino acid substitutions in or near the active site.  These substitutions cause OXA-239 to hydrolyze late-generation cephalosporins and the monobactam aztreonam with greater efficiency than OXA-23.  OXA-239 activity against the carbapenems doripenem and imipenem is reduced approximately 3-fold and 20-fold respectively.  Further analysis demonstrated that two of the substitutions (P225S and D222N) are largely responsible for the observed alteration of kinetic parameters, while the third (S109L) may serve to stabilize the protein...
December 11, 2017: Biochemical Journal
https://www.readbyqxmd.com/read/29229304/functional-characterization-of-the-g162r-and-d216h-genetic-variants-of-human-cyp17a1
#16
C P Capper, J Liu, L R McIntosh, J M Larios, M D Johnson, P F Hollenberg, Y Osawa, R J Auchus, J M Rae
Cytochrome P450 17A1 (CYP17A1) is a dual-function enzyme catalyzing reactions necessary for cortisol and androgen biosynthesis. CYP17A1 is a validated drug target for prostate cancer as CYP17A1 inhibition significantly reduces circulating androgens and improves survival in castration-resistant prostate cancer. Germline CYP17A1 genetic variants with altered CYP17A1 activity manifesting as various endocrinopathies are extremely rare; however, characterizing these variants provides critical insights into CYP17A1 protein structure and function...
December 8, 2017: Journal of Steroid Biochemistry and Molecular Biology
https://www.readbyqxmd.com/read/29229225/design-synthesis-and-pharmacological-evaluation-of-new-acyl-sulfonamides-as-potent-and-selective-bcl-2-inhibitors
#17
Xiaohua Liu, Yu Zhang, Wenjing Huang, Wenfu Tan, Ao Zhang
The antiapoptotic protein Bcl-2, overexpressed in many tumor cells, is an attractive target for potential small molecule anticancer drug discovery. Herein, we report a different structural modification approach on ABT-263 by merging the piperazinyl-phenyl fragment into a bicyclic framework leading to a series of novel analogues, among which tetrahydroisoquinoline 13 was nearly equally potent against Bcl-2 as ABT-263. Further SAR in the P4-interaction pocket affored the difluoroazetidine substituted analogue 55, which retained good Bcl-2 activity with improved Bcl-2/Bcl-xL selectivity...
December 5, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/29227930/synthesis-and-in%C3%A2-vitro-evaluation-of-novel-substituted-isatin-propylene-1h-1-2-3-triazole-4-methylene-moxifloxacin-hybrids-for-their-anti-mycobacterial-activities
#18
Xinjia Yan, Zaosheng Lv, Jing Wen, Shijia Zhao, Zhi Xu
Twelve novel substituted isatin-propylene-1H-1,2,3-triazole-4-methylene-moxifloxacin hybrids 5a-l were designed, synthesized and screened for their in vitro anti-mycobacterial activities against drug-sensitive and multidrug-resistant Mycobacterium tuberculosis as well as cytotoxicity in VERO cell line. All hybrids exhibited excellent activities against two Mycobacterium tuberculosis strains with minimum inhibitory concentration in the range from 0.05 to 2.0 μg/mL. The most active hybrid 5i was 2-8 times more potent than the reference agents (moxifloxacin and rifampicin) in vitro against Mycobacterium tuberculosis H37Rv, while 2->2048 times more potent than the reference agents (moxifloxacin, rifampicin and isoniazid) in vitro against multidrug-resistant Mycobacterium tuberculosis...
December 2, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29227917/design-synthesis-molecular-docking-of-new-lipophilic-acetamide-derivatives-affording-potential-anticancer-and-antimicrobial-agents
#19
Hany E A Ahmed, Saleh K Ihmaid, Abdelsattar M Omar, Ahmed M Shehata, Heba S Rateb, Mohammed F Zayed, Sahar Ahmed, Mahmoud M Elaasser
Fifteen new substituted N-2-(2-oxo-3-phenylquinoxalin-1(2H)-yl) acetamides 5a-f, 6a-f, and 8a-c were synthesized by reacting ethyl 2-(2-oxo-3-phenylquinoxalin-1(2H)-yl)acetate with various primary amines including benzylamines, sulfonamides, and amino acids. The in vitro antimicrobial screening of the target compounds was screened to assess their antibacterial and antifungal activity. As a result, seven compounds namely; 5a, 5c, 5d, 6a, 6c, 8b and 8c showed a promising broad spectrum antibacterial activity against both Gram-positive and Gram-negative strains...
December 2, 2017: Bioorganic Chemistry
https://www.readbyqxmd.com/read/29224996/cost-effectiveness-of-the-non-laboratory-based-framingham-algorithm-in-primary-prevention-of-cardiovascular-disease-a-simulated-analysis-of-a-cohort-of-african-american-adults
#20
Jacob K Kariuki, Philimon Gona, Suzanne G Leveille, Eileen M Stuart-Shor, Laura L Hayman, Jerry Cromwell
The non-lab Framingham algorithm, which substitute body mass index for lipids in the laboratory based (lab-based) Framingham algorithm, has been validated among African Americans (AAs). However, its cost-effectiveness and economic tradeoffs have not been evaluated. This study examines the incremental cost-effectiveness ratio (ICER) of two cardiovascular disease (CVD) prevention programs guided by the non-lab versus lab-based Framingham algorithm. We simulated the World Health Organization CVD prevention guidelines on a cohort of 2690 AA participants in the Atherosclerosis Risk in Communities (ARIC) cohort...
December 7, 2017: Preventive Medicine
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