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Current Drug Discovery Technologies

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https://www.readbyqxmd.com/read/28625149/stability-indicating-reverse-phase-hplc-method-for-estimation-of-rifampicin-and-piperine-in-pharmaceutical-dosage-form
#1
Umang H Shah, Shraddha Patel, Manan Raval
BACKGROUND: High performance liquid chromatography is an integral analytical tool in assessing drug product stability. HPLC methods should be able to separate, detect, and quantify the various drug-related degradants that can form on storage or manufacturing, plus detect and any drug-related impurities that may be introduced during synthesis. OBJECTIVE: A simple, economic, selective, precise, and stability-indicating HPLC method has been developed and validated for analysis of Rifampicin (RIFA) and Piperine (PIPE) in bulk drug and in the formulation...
June 18, 2017: Current Drug Discovery Technologies
https://www.readbyqxmd.com/read/28625148/affinity-crystallography-reveals-the-bioactive-compounds-of-industrial-juicing-byproducts-of-punica-granatum-for-glycogen-phosphorylase
#2
George A Stravodimos, Anastassia L Kantsadi, Anna Apostolou, Efthimios Kyriakis, Vassiliki-Nafsika Kafaski-Kanelli, Theodora G A Solovou, Pagona Gatzona, Panagiota Cv Liggri, Stavroula Theofanous, Vyron A Gorgogietas, Apostolia Kissa, Chariklia Psachoula, Demetra S M Chatzileontiadou, Angelos Lemonakis, Anna-Maria G Psarra, Vassiliki T Skamnaki, Serkos Haroutounian, Demetres D Leonidas
BACKGROUND: Glycogen phosphorylase (GP) is a pharmaceutical target for the discovery of new antihyperglycaemic agents. Punica granatum is a well-known plant for its potent antioxidant and antimicrobial activities but so far has not been examined for antihyperglycaemic activity. OBJECTIVE: To examine the inhibitory potency of eighteen polyphenolic extracts obtained from Punica granatum fruits and industrial juicing byproducts against GP and discover their most bioactive ingredients...
June 18, 2017: Current Drug Discovery Technologies
https://www.readbyqxmd.com/read/28578651/immunomodulatory-effect-of-g2013-a-l-guluronic-acid-on-thetlr2-and-tlr4-in-human-mononuclear-cells
#3
Laleh Sharifi, Monireh Mohsenzadegan, Asghar Aghamohammadi, Nima Rezaei, Farzaneh Tofighi Zavareh, Saied Bokaie, Mona Moshiri, Gholamreza Azizi, Abbas Mirshafiey, Zahra Aghazadeh
BACKGROUND: Inhibition of Toll-like receptors (TLRs) signaling have been established as a new method for development of anti-inflammatory drugs instead of NSAIDs (non-steroid anti-inflammatory drugs). Since the immunomodulatory role of G2013 was reported in some recent experiments, we decided to assess the effects of G2013 (a-L-Guluronic acid) on the protein expression of TLR2 and TLR4, their downstream signaling cascade, and the secretion of pro-inflammatory cytokines in human peripheral blood mononuclear cells (PBMCs)...
June 4, 2017: Current Drug Discovery Technologies
https://www.readbyqxmd.com/read/28558629/quinoline-coumarin-and-other-heterocyclic-analogues-based-hiv-1-integrase-inhibitors
#4
Pankaj Wadhwa, Priti Jain, Hemant R Jadhav, Santosh Rudrawar
Human Immunodeficiency Virus Type 1 Integrase or HIV-1 integrase (IN) is a 288 amino acid protein that incorporates the retrotranscribed viral DNA into the host chromosomal DNA. Over the past 30 years, large number of derivatives have been evaluated for their inhibitory potential against IN. There is vast literature available and needs to be collated to help scientists plan the future drug design. This review discusses the reports of past 25 years on analogues of quinoline, coumarin and other related heterocycles, which exhibit low micromolar inhibitory potency against IN...
May 30, 2017: Current Drug Discovery Technologies
https://www.readbyqxmd.com/read/28545350/utilization-of-the-monte-carlo-method-to-build-up-qsar-models-for-hemolysis-and-cytotoxicity-of-antimicrobial-peptides
#5
Alla P Toropova, Andrey A Toropov, Marten Beeg, Marco Gobbi, Mario Salmona
BACKGROUND: Traditional quantitative structure - property / activity relationships (QSPRs/QSARs) are based on representation of molecular structure by molecular graph or simplified molecular input-line entry system (SMILES). It is attractive idea to develop predictive models for large molecules in general and for peptides in particular. However, the representation of these molecules by molecular graph or SMILES is problematic owing to large size of these molecules. A possible alternative of SMILES is representation of peptides via sequence of abbreviations of amino acids...
May 24, 2017: Current Drug Discovery Technologies
https://www.readbyqxmd.com/read/28474554/flavonoid-enriched-fraction-of-campylandra-aurantiaca-attenuates-carbon-tetrachloride-induced-oxidative-dna-damage-in-mouse-peritoneal-macrophages-in-animal-model
#6
Mainak Chakraborty, Asis Bala, Pallab K Haldar
The aim of the present study was to evaluate the effect of flavonoid enriched fraction of Campylandra aurantiaca (FEFCA) on in vitro and in vivo antioxidant and DNA protective effect in mouse peritoneal macrophages cells. FEFCA was characterized by HPLC analysis. The in vitro antioxidant activities of FEFCA was measured by different in vitro assays like 1, 1-diphenyl-2-picrylhydrazil radical (DPPH), superoxide anions, nitric oxide and hydroxyl radicals scavenging methods. Isolated mouse peritoneal macrophages were oxidized by carbon tetra chloride (CCl4) in animal model; subsequently the protective effect of FEFCA was determined in terms of estimation of antioxidant enzyme and the damage to DNA of the cells...
May 3, 2017: Current Drug Discovery Technologies
https://www.readbyqxmd.com/read/28443514/compound-libraries-recent-advances-and-their-applications-in-drug-discovery
#7
Zhen Gong, Guoping Hu, Qiang Li, Zhiguo Liu, Fei Wang, Xuejin Zhang, Jian Xiong, Peng Li, Yan Xu, Rujian Ma, Shuhui Chen, Jian Li
Hit identification is the starting point of small-molecule drug discovery and is therefore very important to the pharmaceutical industry. One of the most important approaches to identify a new hit is to screen a compound library using an in vitro assay. High-throughput screening has made great contributions to drug discovery since the 1990s but requires expensive equipment and facilities, and its success depends on the size of the compound library. Recent progress in the development of compound libraries has provided more efficient ways to identify new hits for novel drug targets, thereby helping to promote the development of the pharmaceutical industry, especially for first-in-class drugs...
April 25, 2017: Current Drug Discovery Technologies
https://www.readbyqxmd.com/read/28412913/anti-carcinogenic-effects-of-carnosol-an-updated-review
#8
Saeed Samarghandian, Mohsen Azimi-Nezahad, Tahereh Farkhondeh
BACKGROUND: Despite the newly treatment procedures, cancer is considered as the main health threat nowadays and, therefore, new therapeutic options such as traditional medicine should be investigated. Rosemary (Rosmarinus officinalis L.) has been found to possess antitumor effects due to its major ingredients, including carnosic acid, carnosol, ursolic acid, and rosmarinic acid. OBJECTIVE: This study was designed to gather the recent literature findings from 2010 to 2016 on the cancer anti-tumor activities of carnosol and probably involved mechanisms...
April 13, 2017: Current Drug Discovery Technologies
https://www.readbyqxmd.com/read/28382857/prediction-of-human-intestinal-absorption-of-compounds-using-artificial-intelligence-techniques
#9
Rajnish Kumar, Anju Sharma, Mohammed Haris Siddiqui, Rajesh Kumar Tiwari
Information about Pharmacokinetics of compounds is an essential component of drug design and development. Modeling the pharmacokinetic properties require identification of the factors effecting absorption, distribution, metabolism and excretion of compounds. There have been continuous attempts in the prediction of absorption of compounds using various Artificial intelligence methods in the effort to reduce the attrition rate of drug candidates entering to preclinical and clinical trials. Currently, there are large numbers of individual predictive models available for absorption using machine learning approaches...
April 4, 2017: Current Drug Discovery Technologies
https://www.readbyqxmd.com/read/28359232/identification-and-characterization-of-a-chemical-compound-that-inhibits-methionyl-trna-synthetase-from-pseudomonas-aeruginosa
#10
Sara Robles, Yanmei Hu, Tahyra Resto, Frank Dean, James M Bullard
Pseudomonas aeruginosa is an opportunistic pathogen problematic in causing nosocomial infections and is highly susceptible to development of resistance to multiple antibiotics. The gene encoding methionyl-tRNA synthetase (MetRS) from P. aeruginosa was cloned and the resulting protein characterized. MetRS was kinetically evaluated and the KM for its three substrates, methionine, ATP and tRNAMet were determined to be 35, 515, and 29 μM, respectively. P. aeruginosa MetRS was used to screen two chemical compound libraries (1690) and a natural product compound was identified that inhibited the aminoacylation function...
March 30, 2017: Current Drug Discovery Technologies
https://www.readbyqxmd.com/read/28359233/in-vivo-hypoglycemic-studies-of-polyherbal-phytoceuticals-their-pharmacokinetic-studies-and-dose-extrapolation-by-allometric-scaling
#11
Baishakhi De, Koushik Bhandari, Prakash Katakam, Analava Mitra
BACKGROUND: This work reports the safety profiling, in vivo hypoglycemic and pharmacokinetic studies of three phytoceuticals viz. conventional and sustained release tablets and microspheres each containing a polyherbal product phytocomposite (PHC) as the active ingredient. PHC is prepared from the leaf extracts of Ficus benghalensis: Syzigium cumini: Ocimum sanctum mixed in the weight ratio of 1:1:2. Further no observed adverse effect level (NOAEL), maximum recommended starting dose (MRSD) in human and prediction of human pharmacokinetic parameters have been accomplished by allometric equations...
March 29, 2017: Current Drug Discovery Technologies
https://www.readbyqxmd.com/read/28325148/the-potent-inhibitory-effect-of-%C3%AE-d-mannuronic-acid-m2000-as-a-novel-nsaid-with-immunosuppressive-property-on-anti-cyclic-citrullinated-peptide-antibodies-rheumatoid-factor-and-anti-dsdna-antibodies-in-patients-with-rheumatoid-arthritis
#12
Hossein Ahmadi, Ahmad Reza Jamshidi, Mahdi Mahmoudi, Salvatore Cuzzocrea, Mohammad Javad Fattahi, Anis Barati, Bernd H A Rehm, Hidenori Matsou, Abbas Mirshafiey
OBJECTIVE: To investigate the inhibitory effect of β-D-mannuronic acid (M2000) on anti-cyclic citrullinated peptide antibodies (anti-CCP), rheumatoid factor (RF), anti-double strand DNA (anti-dsDNA) and acute phase reactants in rheumatoid arthritis (RA) patients. METHODS: The study included 40 patients with RA who had an inadequate response to conventional therapy (identifier: IRCT2014011213739N2). The patients were permitted to continue the conventional therapy excluding NSAIDs...
March 21, 2017: Current Drug Discovery Technologies
https://www.readbyqxmd.com/read/28240185/design-synthesis-and-molecular-docking-of-1-cyclopropyl-6-fluoro-4-oxo-7-4-2-4-substituted-phenyl-2-substituted-ethyl-1-piperazinyl-1-4-dihydroquinoline-3-carboxylic-acid-as-an-antimicrobial-agents
#13
Mehul M Patel, Laxman J Patel
BACKGROUND: Quinolone scaffold are widely used for synthesis of number of medicinal compounds with variety of biological activity. In view of the reported antimicrobial activity of various fluoroquinolones, the structure activity studies of various substituted quinolones, which proved the importance of the C-7 substituents to exhibit potent antimicrobial activities. OBJECTIVE: Based on the structural activity relationship at C-7 position it was rationalized to design and synthesize new quinolone derivatives with increasing bulk at C-7 position of the main 6-fluoroquinolone scaffold...
February 24, 2017: Current Drug Discovery Technologies
https://www.readbyqxmd.com/read/28176631/grid-based-continual-analysis-of-molecular-interior-for-drug-discovery-qsar-and-qspr
#14
A V Potemkin, M A Grishina, V A Potemkin
BACKGROUND: In 1979, R.D.Cramer and M.Milne made a first realization of the above mentioned principles attempting to compare molecules by aligning them in space and by mapping their molecular fields to a 3D grid. Further, this approach was developed as the DYLOMMS (DYnamic Lattice-Oriented Molecular Modelling System) approach. In 1984, H.Wold and S.Wold proposed the use of partial least squares (PLS) analysis, instead of principal component analysis, to correlate the field values with biological activities...
February 7, 2017: Current Drug Discovery Technologies
https://www.readbyqxmd.com/read/28155594/pbpk-modeling-a-predictive-eco-friendly-bio-waiver-tool-for-drug-research
#15
Baishakhi De, Koushik Bhandari, Ranjan Mukherjee, Prakash Katakam, Shanta K Adiki, Rohit Gundamaraju, Analava Mitra
BACKGROUND: The world has witnessed growing complexities in disease scenario influenced by the drastic changes in host-pathogen- environment triadic relation. Pharmaceutical R&Ds are in constant search of novel therapeutic entities to hasten transition of drug molecules from lab bench to patient bedside. Extensive animal studies and human pharmacokinetics are still the "gold standard" in investigational new drug research and bio-equivalency studies. Apart from cost, time and ethical issues on animal experimentation, burning questions arise relating to ecological disturbances, environmental hazards and biodiversity issues...
February 1, 2017: Current Drug Discovery Technologies
https://www.readbyqxmd.com/read/28124597/pimping-up-drugs-recovered-superannuated-and-under-exploited-drugs-an-introduction-to-the-basics-of-drug-reprofiling
#16
Suzanne Jane Dilly, George Stephen Morris
Drug development has moved along way forward from the days of with doctors peddling cauldrons of herbs and spices, however the process can still miss opportunities for full exploitation of a drug's potential. Drug reprofiling provides a chance for an established or a forgotten drug to move into a new area of therapy, whether related to the known effects or in a completely new area. In an era of environmental awareness and spiraling costs for traditional drug development, a strategy to squeeze every benefit out of drugs with known safety, tolerability and pharmacological parameters must be a strategically sound desire...
January 17, 2017: Current Drug Discovery Technologies
https://www.readbyqxmd.com/read/28056731/molecularly-imprinted-polymer-of-colocynthin-an-effective-tool-for-quality-control-of-citrullus-colocynthis-extracts
#17
Farid Ramezany, Mahnaz Khanavi, Mohammad Reza Shams Ardakani, Börje Sellegren, Mahdieh Eftekhari, Hossein Rastegar, Maryam Shekarchi
BACKGROUND: Different parts of Colocynth, Citrullus colocynthis (L.) Schrad., are used in traditional phytotherapy and homeopathy. OBJECTIVE: In our new approach, a molecularly imprinted polymer was synthesized to absorb colocynthin, the major plant marker, and its capability was evaluated using HPLC-UV. METHOD: A new method was considered to achieve optimal conditions. FT-infrared, N2 adsorption porosimetry, fluorescent and scanning electron microscopy and thermo gravimetric profile of the polymers were studied...
January 4, 2017: Current Drug Discovery Technologies
https://www.readbyqxmd.com/read/28042769/discovery-of-an-unexplored-protein-structural-scaffold-of-serine-protease-from-big-blue-octopus-octopus-cyanea-a-new-prospective-lead-molecule
#18
Subhamay Panda, Leena Kumari
BACKGROUND: Serine proteases are a group of enzymes that hydrolyses the peptide bonds in proteins. In mammals, these enzymes help in the regulation of several major physiological functions such as digestion, blood clotting, responses of immune system, reproductive functions and the complement system. OBJECTIVE: Serine proteases obtained from the venom of Octopodidae family is a relatively unexplored area of research. In the present work, we tried to effectively utilize comparative composite molecular modeling technique...
January 2, 2017: Current Drug Discovery Technologies
https://www.readbyqxmd.com/read/28003007/icp-ms-analytical-method-for-identification-and-detection-of-elemental-impurities
#19
Mohini Mittal, Kapil Kumar, Durgadas Anghore, Ravindra Kumar Rawal
Aim of this article is to review and discuss the currently used quantitative analytical method ICP-MS, which is used for quality control of pharmaceutical products. ICP-MS technique has several applications such as determination of single elements, multi element analysis in synthetic drugs, heavy metals in environmental water, trace element content of selected fertilizers and dairy manures. ICP-MS is also used for determination of toxic and essential elements in different varieties of food samples and metal pollutant present in the environment...
December 21, 2016: Current Drug Discovery Technologies
https://www.readbyqxmd.com/read/28000555/physicochemical-characteristics-of-brazilian-green-propolis-evaluated-during-a-six-year-period
#20
Sônia M De Figueiredo, Nancy Scardua Binda, Sidney AugustoVieira-Filho, Bruno de Moura Almeida, Sheila Rago Lemos Abreu, Niraldo Paulino, Gláucia Maria Pastore, HéliaHarumi Sato, Viviane Cristina Toreti Theodoropoulos, Eulália Vargas Tapia, Yong Kun Park, Raquel Basques Caligiorne
BACKGROUND: Propolis has been used as a natural health product mainly due to the presence of polyphenols, flavonoids, phenolic aldehydes, amino acids, vitamins and others bioactive constituents. To this natural substance are attributed different biological and pharmacological properties which are influenced by its chemical composition and organoleptic properties. The aim of this work was to evaluate the physicochemical properties and parameters of green propolis collected during a period of six years (2008-2013) in the state of Minas Gerais, located at the southeastern region of Brazil...
December 20, 2016: Current Drug Discovery Technologies
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