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Current Drug Discovery Technologies

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https://www.readbyqxmd.com/read/28799486/development-and-validation-of-chemometric-spectrophotometric-methods-for-simultaneous-determination-of-simvastatin-and-nicotinic-acid-in-binary-combinations
#1
Shoeb Alahmad, Hamed M Elfatatry, Mokhtar M Mabrouk, Sherin F Hammad, Fotouh R Mansour
BACKGROUND: The development and introduction of combined therapy represent a challenge for analysis due to severe overlapping of their UV spectra in case of spectroscopy or the requirement of a long tedious and high cost separation technique in case of chromatography. Quality control laboratories have to develop and validate suitable analytical procedures in order to assay such multi component preparations. METHOD: New spectrophotometric methods for the simultaneous determination of simvastatin (SIM) and nicotinic acid (NIA) in binary combinations were developed...
August 10, 2017: Current Drug Discovery Technologies
https://www.readbyqxmd.com/read/28748751/update-on-nitazoxanide-a-multifunctional-chemotherapeutic-agent
#2
Anshul Shakya, Hans Raj Bhat, Surjit Kumar Ghosh
Background: The thiazolide nitazoxanide (NTZ) is a broad-spectrum anti-infective drug that adversely affects viability, growth, and proliferation of a range of extracellular and intracellular protozoan, helminths, anaerobic and microaerophilic bacteria, and viruses. Methods: Current review compiled the potential chemotherapeutic efficacy of NTZ against a variety of such disease-causing macro and/or micro-organisms as well as neoplastic cells, using various search engines viz...
July 27, 2017: Current Drug Discovery Technologies
https://www.readbyqxmd.com/read/28745209/thiazole-containing-heterocycles-with-antimalarial-activity
#3
Mukesh Kumar Kumawat
BACKGROUND: Heterocyclic compounds are the main class of medicinally important compounds. Many heterocyclic compounds bearing a five member ring in their structure have a good spectrum of biological activities. Thiazole is an important class of five membered heterocyclic compounds. Thiazole and its derivatives exhibited a broad range of biological activities due to the presence of various reaction posses. Thiazole, heterocyclic nucleus is present in several potent pharmacologically active molecules such as Sulfathiazole (antimicrobial drug), Ritonavir (antiretroviral drug), Tiazofurin (antineoplastic drug) and Abafungin (antifungal drug) etc...
July 25, 2017: Current Drug Discovery Technologies
https://www.readbyqxmd.com/read/28745208/thiazole-containing-heterocycles-with-cns-activity
#4
Priyanka Kalal, Divyani Gandhi, Prakash Prajapat, Shikha Agarwal
BACKGROUND: Thiazoles are promising scaffolds in the area of medicinal and pharmaceutical chemistry and have accounted to show different pharmacophoric properties. For the last years, thiazole derivatives have focused too much attention to develop different new CNS active agents. It has been broadly used to generate diverse therapeutic agents against various CNS targets. Histamine H3 receptors are seriously involved in the pathophysiology of numerous disorders of the central nervous system...
July 24, 2017: Current Drug Discovery Technologies
https://www.readbyqxmd.com/read/28707600/a-new-potent-ns5a-inhibitor-in-the-management-of-hepatitis-c-virus-ravidasvir
#5
Enas Hafez, Tamer Elbaz, Mohamed El Kassas, Gamal Esmat
Background: Chronic hepatitis C virus (HCV) is a worldwide health problem that can lead to liver cirrhosis, liver cell failure and numerous subsequent complications such as hepatocellular carcinoma. Till the near past, pegylated interferon was the standard of care therapy. However, it was associated with suboptimal success rates and many side effects. Thereafter, direct antiviral agents (DAA) appeared and played the key role in management of HCV. One of those recent DAA is ravidasvir. Summary: It is a potent NS5A inhibitor that was formerly known as PPI-668...
July 13, 2017: Current Drug Discovery Technologies
https://www.readbyqxmd.com/read/28707599/designing-of-selective-%C3%AE-secretase-inhibitory-benzenesulfonamides-through-comparative-in-vitro-and-in-silico-analysis
#6
Neeraj Masand, Satya P Gupta, Ratan Lal Khosa
BACKGROUND: In Alzheimer's disease (AD), the gene mutations have been identified in the amyloid precursor protein (APP), the presenilin-1 (PS1) and -2 (PS2) genes. APP is a transmembrane protein which gets cleaved by α- and β-secretase enzymes and releases Aβ peptides which forms senile plaques in brain tissue. It contributes for local inflammatory response, subsequent oxidative stress, biochemical changes and neuronal death. Targeting the development of Aβ aggregates in the senile plaques is an important strategy in the treatment of AD...
July 13, 2017: Current Drug Discovery Technologies
https://www.readbyqxmd.com/read/28625149/stability-indicating-reverse-phase-hplc-method-for-estimation-of-rifampicin-and-piperine-in-pharmaceutical-dosage-form
#7
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
#8
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
#9
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
#10
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
#11
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
#12
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
#13
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
#14
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
#15
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
#16
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
#17
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
#18
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
#19
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
#20
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
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