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Current Drug Discovery Technologies

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https://www.readbyqxmd.com/read/29149813/structural-analysis-of-cd59-of-chinese-tree-shrew-a-new-reference-molecule-for-human-immune-system-specific-cd59-drug-discovery
#1
Subhamay Panda, Leena Kumari, Santamay Panda
BACKGROUND: Chinese tree shrews (Tupaia belangeri chinensis) bear several characteristics that are considered to be very crucial for utilizing in animal experimental models in biomedical research. Subsequent to the identification of key aspects and signaling pathways in nervous and immune systems, it is revealed that tree shrews acquires shared common as well as unique characteristics, and hence offers a genetic basis for employing this animal as a prospective model for biomedical research...
November 17, 2017: Current Drug Discovery Technologies
https://www.readbyqxmd.com/read/29149812/architectures-and-mechanical-properties-of-drugs-and-complexes-of-surface-active-compounds-at-air-water-and-oil-water-interfaces
#2
Dipak K Sarker
BACKGROUND: Drugs can represents a multitude of compounds from proteins and peptides, such as growth hormones and insulin and on to simple organic molecules such as flurbiprofen, ibuprofen and lidocaine. Given the chemical nature of these compounds two features are always present. A portion or portions of the molecule that has little affinity for apolar surfaces and media and the opposite a series of part or one large part that has considerable affinity for hydrophilic, polar or charged media and surfaces...
November 17, 2017: Current Drug Discovery Technologies
https://www.readbyqxmd.com/read/29110619/influence-of-antipsychotic-drug-risperidone-on-human-serum-albumin-affinity-to-organic-anions
#3
Tatiana Syrejshchikova, Natalia Smolina, Valentin Kondratyuk, Gennady Dobretsov, Marat Uzbekov
BACKGROUND: Risperidone is an antipsychotic drug. In blood, this drug binds mainly to human serum albumin (HSA) and is also transported by HSA. METHODS: To study certain details of the interaction between risperidone and HSA, a fluorescent dye CAPIDAN was used as a reporter. This dye specifically fluoresces from HSA in serum and is highly sensitive to structural changes in HSA including pathology-induced changes. Interaction of CAPIDAN with HSA has been studied using time-resolved fluorescence techniques...
November 6, 2017: Current Drug Discovery Technologies
https://www.readbyqxmd.com/read/29076430/quantification-of-newly-discovered-anti-cancer-drug-enzalutamide-in-bulk-and-synthetic-mixture-by-stability-indicating-tlc-method
#4
Usmangani K Chhalotiya, Dharmendra J Prajapati, Minesh D Prajapati, Jalpa U Patel, Jaineel Desai
Objective A impressionable, discriminatory and precise stability indicating high performance thin layer chromatographic method has been developed and validated for the estimation of of Enzalutamide in bulk and synthetic mixture. Method The method engaged HPTLC aluminium plates pre-coated with silica gel 60F-254 as the stationary phase while the solvent system was ethyl acetate: toluene (4.5:5.5, v/v). The Rf value of enzalutamide was detected to be 0. 39 ± 0. 005 and the densitometric analysis were carried out in absorbance mode at 246 nm...
October 27, 2017: Current Drug Discovery Technologies
https://www.readbyqxmd.com/read/29065836/stability-indicating-liquid-chromatographic-method-for-simultaneous-determination-of-aspirin-and-omeprazole
#5
Vandana B Patel, Aishwarya D Patel, Dimal A Shah
BACKGROUND: Aspirin combination is prescribed for the its thrombolytic activity where gastric ulceration is the major side effects of aspirin which can be prevented by combining it with proton pump inhibitor omeprazole. Present study describes development of analytical method for the estimation of aspirin and omeprazole in combination. Objective of the present study was to develop and validate chromatographic method for simultaneous analysis of aspirin and omeprazole. METHODS: Isocratic, reversed phase stability indicating liquid chromatographic method was developed for the simultaneous determination of Aspirin and Omeprazole in combination...
October 23, 2017: Current Drug Discovery Technologies
https://www.readbyqxmd.com/read/29046161/inhaled-nitric-oxide-in-preterm-neonates-with-refractory-hypoxemia-associated-to-oligohydramnios
#6
Alvarado Socarras Jorge, Castro M Javier, Fredi Alexander Diaz-Quijano
BACKGROUND: Therapy with inhaled nitric oxide (iNO) is effective in the management of pulmonary hypertension and severe hypoxemia. However, these benefits have not been demonstrated in preterm infants (<34 weeks). The objective of this report is to present the experience of eight cases of preterm neonates with respiratory distress syndrome (RDS) and refractory hypoxemia, with oligohydramnios history. METHODS: We evaluated the clinical feature of 8 preterm neonates with severe hypoxemia who had maternal antecedents of oligoamnios, mainly due to premature rupture of membranes...
October 17, 2017: Current Drug Discovery Technologies
https://www.readbyqxmd.com/read/29032758/multifaceted-effects-of-delta-opioid-receptors-and-dadle-in-diseases-of-the-nervous-system
#7
Jea-Young Lee, M Grant Liska, Marci Crowley, Kaya Xu, Sandra A Acosta, Cesar V Borlongan, Vivian A Guedes
The opioid system is considered a potential therapeutic target in a variety of neurological disorders. Delta opioid receptors (DOPs) are broadly expressed in the brain, and their activation protects cells from hypoxic/ischemic insults by counteracting disruptions of ionic homeostasis and initiating neuroprotective pathways. The DOP agonist D-Ala2-D-Leu2-Enkephalin (DADLE) promotes neuronal survival, mitigates apoptotic pathways, and protects neurons and glial cells from ischemia-induced cell death, thus making DADLE a promising therapeutic option for stroke...
October 10, 2017: Current Drug Discovery Technologies
https://www.readbyqxmd.com/read/29032757/an-evidence-based-review-of-medicinal-herbs-for-the-treatment-of-gastroesophageal-reflux-disease-gerd
#8
Ayda Hosseinkhani, Kamran Bagheri Lankarani, Abdolali Mohagheghzadeh, Chunlin Long, Mehdi Pasalar
BACKGROUND: Gastroesophageal reflux disease (GERD) is one of the most common diseases in society, affecting up to 40% of the population. It has major impact on the quality of life and a high burden on medical expenditure. In this work, herbs used by ancient Iranians to treat GERD have been introduced. METHODS: Different well-known Persian textbooks and recent electronic databases were searched to explore the treatment of GERD and the pharmacological mechanisms of the identified medicinal plants...
October 10, 2017: Current Drug Discovery Technologies
https://www.readbyqxmd.com/read/28969569/molecular-docking-synthesis-and-biological-evaluation-of-sulphonylureas-guanidine-derivatives-as-promising-antidiabetics-agent
#9
Ishan Panchal, Dhrubo Jyoti Sen, Ashish D Patel, Umang Shah, Mehul Patel, Archana Navle, Vashisth Bhavsar
BACKGROUND: A series of novel sulphonylureas/guanidine derivatives were designed, synthesized, and evaluated for the treatment of diabetes mellitus. In this study, the designed compounds were docked with AKR1C1 complexes by using glide docking program and docking calculations were performed to predict the binding affinity of the designed compounds with the binding pocket of protein 4YVP and QikProp program was used to predict the ADME/T properties of the analogues. METHODS: All the targeted derivatives were synthesized and purified by recrystallization...
October 2, 2017: Current Drug Discovery Technologies
https://www.readbyqxmd.com/read/28969568/in-vitro-and-in-silico-activity-of-iridoids-against-leishmania-amazonensis
#10
Gilsane Lino von Poser, Maria Helena Vendruscolo, Gustavo Machado Neves, Luciano Porto Kagami, Luiz Carlos Rodrigues, Maria Luisa Diehl, Simone Cristina Baggio Gnoatto, Sérgio Augusto de Loreto Bordignon, Pedro Roosevelt Torres Romão, Vera Lucia Eifler Lima
BACKGROUND: Leishmaniasis reaches millions of people around the world. The control of the disease is difficult due to the restricted access to the diagnosis and medication and the low adherence to the treatment. Thus, more efficient drugs are need and natural products are good alternatives. Iridoids, natural products with reported leishmanicidal activity, can be exploited for the development of anti-Leishmania drugs. The aim of this study was to isolate and to investigate the in vitro activity of iridoids against Leishmania amazonensis and to compare the activity in silico of these compounds with those reported as active against this parasite...
October 2, 2017: Current Drug Discovery Technologies
https://www.readbyqxmd.com/read/28914189/a-hopeful-prospect-of-riociguat-as-a-soluble-guanylate-cyclase-stimulator-for-management-of-pressure-ulcers
#11
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
#12
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
#13
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
#14
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
#15
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
#16
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
#17
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
#18
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
#19
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
#20
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
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