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Current Drug Discovery Technologies

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https://www.readbyqxmd.com/read/28914189/a-hopeful-prospect-of-riociguat-as-a-soluble-guanylate-cyclase-stimulator-for-management-of-pressure-ulcers
#1
Soha Azadi, Hajar Ashrafi, Amir Azadi
Pressure ulcer remains as a common problem, especially developed in disabled patients and hence, subjected to continuous pressure for prolonged periods of time. Most of the studies investigating the preventive and therapeutic approaches have focused on wound cleansing, dressing and supportive strategies , as well as pharmacological therapy including zinc sulphate, vitamin A or phenytoin. Despite such efforts, pressure ulcer continues to impair the life quality and expectancy. Thus involving in the paradigm shift in biomedical studies, the recent ones focus on biological signaling pathways involving nitric oxide (NO)- soluble guanylatecyclase (sGC)- cyclic guanosine monophosphate (cGMP) contributing in vasodilation, reperfusion and oxygen delivery...
September 15, 2017: Current Drug Discovery Technologies
https://www.readbyqxmd.com/read/28914188/a-retrospect-study-on-thiazole-derivatives-as-the-potential-antidiabetic-agents-in-drug-discovery-amp-developments
#2
Gopal L Khatik, Ashok Kumar Datusalia, Waquar Ahsan, Paranjeet Kaur, Manish Vyas, Amit Mittal, Surendra Kumar Nayak
BACKGROUND: Heterocycles containing thiazole, a moiety with sulfur and nitrogen is a core structure which found in a number of biologically active compounds. The thiazole ring is notable as a component of the certain natural products, such as vitamin B1 (thiamine) and penicillins. Thiazole is also known as wonder nucleus and has versatile in different biological fields. A number of new compounds contain heterocycle thiazole moieties, thus it is one of the important areas of research. METHODS: We searched the scientific database using relevant keywords...
September 15, 2017: Current Drug Discovery Technologies
https://www.readbyqxmd.com/read/28901248/review-on-synthetic-chemistry-and-antibacterial-importance-of-thiazole-derivatives
#3
Ankita Kashyap, Nayana Adhikari, Arpita Das, Anshul Shakya, Surajit Kumar Ghosh, Udaya Pratap Singh, Hans Raj Bhat
The heterocyclic compounds include a vast subject in chemistry and thiazole is one of the leading heterocyclic compounds which have a five-member ring with the molecular formula C3H3NS containing sulphur and nitrogen atoms, occupies an important place in pharmaceutical chemistry. Many natural and synthetic medicinally important compounds contain thiazole as essential moieties with a broad range of therapeutic activities. Diverse modifications of the thiazole ring at various positions led to a variety of novel compounds with a wide spectrum of pharmacological activities such as antibacterial, antioxidant, diuretic, antifungal, antitubercular, anti-inflammatory, anticonvulsant, anti-HIV, antidiabetic, antihypertensive, anti-Alzheimer and anticancer activities...
September 11, 2017: Current Drug Discovery Technologies
https://www.readbyqxmd.com/read/28875855/impurity-profile-of-bronchodilators-used-in-asthma-a-critical-review
#4
Krunal J Prajapati, Charmy Kothari
BACKGROUND: Asthma is defined as a heterogeneous disease usually characterized by chronic airway inflammation (GINA 2016) affecting almost 334 million people worldwide (Global asthma report 2014). Treatment of asthma with a long-acting bronchodilator is important because it reduces the symptoms that occur at night or in the early morning and it is very effective to use as a long term control medication for asthma by preventing asthmatic symptoms. The main objective of this review is to describe the impurity profile and force degradation studies for three major classes of bronchodilators namely β2-adrenoceptor agonists, muscarinic receptor antagonists and xanthine...
August 29, 2017: Current Drug Discovery Technologies
https://www.readbyqxmd.com/read/28875854/cytomegalovirus-infection-the-neurodevelopmental-peptide-signatures
#5
Guglielmo Lucchese, Darja Kanduc
BACKGROUND AND OBJECTIVE: HCMV infection may cause neurodevelopmental disorders, including intellectual disability, hearing loss, cortical malformations, and calcifications. Theorizing about the still unknown molecular basis of HCMV-related diseases, this study analyzes the peptide sharing between HCMV, strains AD169 and Merlin, and human proteins, searching for shared sequences that might lead to crossreactive autoimmune injuries in the brain during immune responses following HCMV infection...
August 29, 2017: Current Drug Discovery Technologies
https://www.readbyqxmd.com/read/28875853/effectiveness-of-cicer-arietinum-in-cutaneous-problems-viewpoint-of-avicenna-and-razi
#6
Marjan Mahjour, Arash Khoushabi, MohammadReza Noras, Shokouhsadat Hamedi
BACKGROUND: Cicer arietinum is one of the popular legumes in the most parts of the world. It's known for a long time in Asia because of the many possibilities of its application. Cicer arietinum has benefits for the skin regarding safe ingredients. Some of these ingredients are recommended in skin care. METHODS: This study aimed to introduce the benefits of Cicer arietinum by reviewing of traditional literature from 10th to 21th century and also conventional medicine for its safe ingredients by searching the electronic data banks such as ISI, Pub Med and Scopus...
August 29, 2017: Current Drug Discovery Technologies
https://www.readbyqxmd.com/read/28875852/molecular-modeling-studies-of-novel-fluoroquinolone-molecules
#7
Naresh Kumar Katari, Tejeswara Rao Allaka, Venkataramireddy Veeramreddy, Jaya Shree Anireddy
BACKGROUND: Fluoroquinolones have been the centre of considerable scientific and clinical interest due to their broad spectrum pharmacological activities. Pefloxacin is an analogue of norfloxacin, which is a 3rd generation of fluoroquinolone [5] antibiotic similar to ciprofloxacin. Pefloxacin is used to treat a variety of bacterial infections like respiratory tract, ear, nose and throat (ENT) infections, skin infections, urinary tract infections. Hydrazone as a pharmacophore unit that attract the medicinal chemists because of structure activity relationship (SAR) studies of fluoroquinolones especially the functionality at C-3 position...
August 29, 2017: Current Drug Discovery Technologies
https://www.readbyqxmd.com/read/28814239/homology-modeling-and-molecular-docking-studies-of-bacillomycin-and-iturin-synthetases-with-novel-ligands-for-the-production-of-therapeutic-lipopeptides
#8
Jujjavarapu Satya Eswari, Swasti Dhagat, Shubham Kaser, Anoop Tiwari
BACKGROUND: Lipopeptide synthetases play an important role in the production of lipopeptides. Lipopeptides are molecules made up of peptides and fatty acid moieties and have shown to have a broad range of antimicrobial activity. As infectious diseases have caused severe health problems mainly resulting from the development of antibiotic resistant strains of disease causing microorganisms there is a need of alternatives to antibiotics. The lipopeptide synthetase of the corresponding lipopeptides can be used as templates to design these as drugs using computational techniques...
August 15, 2017: Current Drug Discovery Technologies
https://www.readbyqxmd.com/read/28814238/structural-insights-for-drugs-developed-for-phospholipase-d-enzymes
#9
Kimberly Stieglitz
BACKGROUND: In recent years human phospholipase D enzymes (PLD1 and PLD2 isozymes) have emerged as drug targets for various diseases such as cardiovascular disease, cancer, infectious diseases and neurodegenerative conditions such as Alzheimer's and Parkinson's disease. The interest in PLD as a drug target is due to the fact that PLD enzymes belong to a superfamily of phospholipases that are essential to intracellular and extracellular signaling. Many bioactive lipid signaling molecules are generated by these enzymes including phosphatidic and lysophosphatidic acid, arachidonic acid, and diacylglycerol (DAG)...
August 15, 2017: Current Drug Discovery Technologies
https://www.readbyqxmd.com/read/28799486/development-and-validation-of-chemometric-spectrophotometric-methods-for-simultaneous-determination-of-simvastatin-and-nicotinic-acid-in-binary-combinations
#10
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
#11
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
#12
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
#13
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
#14
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
#15
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
#16
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
#17
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
#18
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
#19
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
#20
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
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