Read by QxMD icon Read


Beata Powroźnik, Karolina Słoczyńska, Krzysztof Marciniec, Paweł Zajdel, Elżbieta Pękala
Purpose: Determination of the mutagenic potential of new biologically active compounds is of great concern for preliminary toxicity testing and drug development. Methods: The mutagenic and antimutagenic effects of some quinoline- and isoquinolinesulfonamide analogs of aripiprazole (1-8), which display potent antidepressant, anxiolytic, and antipsychotic properties, were evaluated using the Vibrio harveyi assay and OSIRIS Property Explorer software. Additionally, the Ames test was used as the reference. Results: In silico prediction showed that compounds 5 (N-(3-(4-(2,3- dichlorophenyl)piperazin-1-yl)propyl)quinoline-7-sulfonamide) and 6 (N-(4-(4-(2,3- Dichlorophenyl)piperazin-1-yl)butyl)quinoline-7-sulfonamide) trigger a mutagenic structural alert...
September 2016: Advanced Pharmaceutical Bulletin
K Suzuki, G Michael, Y Tamire
OBJECTIVE: Advances in wound treatment have yielded successful approaches to complex wound closure through plastic surgery or other staged surgical methods. However, not all patients or wounds are candidates for such increasingly rigorous levels of interventions. The exploration of non-surgical treatment options that promote anatomical and functional tissue replacement on an outpatient basis without donor site morbidity is necessary to maximise opportunities for patient mobility and rehabilitation...
October 2016: Journal of Wound Care
S Indhavivadhana, M Rattanachaiyanont, S Angsuwathana, K Techatraisak, P Tanmahasamut, P Leerasiri
OBJECTIVES: To validate osteoporosis risk assessment tools in middle-aged Thai women. METHODS: A total of 1038 women who had bone mineral density (BMD) measurements using dual-energy X-ray absorptiometry were reviewed. Clinical data were used to validate the diagnostic test performance of various osteoporosis risk assessment tools, including ABONE, FRAX(®), ORAI, OSIRIS, SCORE, SOFSURF, and OSTA. The following parameters were evaluated: sensitivity, specificity, negative predictive value (NPV), positive predictive value (PPV), and accuracy; those with 95% confidence interval (CI) of the receiver operator characteristics area under the curve (ROC-AUC) > 0...
September 24, 2016: Climacteric: the Journal of the International Menopause Society
Sara S Webb, Karla Hemming, Madhi Y Khalfaoui, Tine Brink Henriksen, Sara Kindberg, Stine Stensgaard, Christine Kettle, Khaled M K Ismail
INTRODUCTION AND HYPOTHESIS: To establish the contribution of maternal, fetal and intrapartum factors to the risk of incidence of obstetric anal sphincter injuries (OASIS) and assess the feasibility of an OASIS risk prediction model based on variables available to clinicians prior to birth. METHODS: This was a population-based, retrospective cohort study using single-site data from the birth database of Aarhus University Hospital, Denmark. The participants were all women who had a singleton vaginal birth during the period 1989 to 2006...
September 2, 2016: International Urogynecology Journal
Renata Maria Ferreira, Marise Teresinha Brenner Affonso da Costa, Osiris Canciglieri Junior, Ângelo Márcio Oliveira Sant'Anna
INTRODUCTION: Human heart valves are used as replacement valves and have satisfactory functional results compared with conventional prostheses. OBJECTIVE: Characterize the profile of effective heart donors from the human valve bank of the santa casa de misericórdia de curitiba and analyze the association between the profile variables. METHODS: It consists of a retrospective and quantitative study of electronic medical records from heart donors for heart valves...
April 2016: Brazilian Journal of Cardiovascular Surgery
Lilly Aswathy, Radhakrishnan S Jisha, Vijay H Masand, Jayant M Gajbhiye, Indira G Shibi
In this work, an attempt was made to propose new leads based on the natural scaffold Thiaplakortone-A active against malaria. The 2D QSAR studies suggested that three descriptors correlate with the anti-malarial activity with an R(2) value of 0.814. Robustness, reliability and predictive power of the model were tested by internal validation, external validation, Y-scrambling and Applicability domain analysis. HQSAR studies were carried out as an additional tool to find the sub-structural fingerprints. The CoMFA and CoMSIA models gave Q(2) values of 0...
August 5, 2016: Journal of Biomolecular Structure & Dynamics
Jian Gao, Li Liang, Yasheng Zhu, Shengzhi Qiu, Tao Wang, Ling Zhang
Peptide deformylase (PDF) is a metalloprotease catalyzing the removal of a formyl group from newly synthesized proteins, which makes it an important antibacterial drug target. Given the importance of PDF inhibitors like actinonin in antibacterial drug discovery, several reported potent PDF inhibitors were used to develop pharmacophore models using the Galahad module of Sybyl 7.1 software. Generated pharmacophore models were composed of two donor atom centers, four acceptor atom centers and two hydrophobic groups...
2016: International Journal of Molecular Sciences
Rajasekhar Komarla Kumarachari, Sivakumar Peta, Abdrrahman Shemsu Surur, Yenus Tadesse Mekonnen
INTRODUCTION: As pyrimidine is a basic nucleus in DNA and RNA, it has been found to be associated with diverse biological activities. Pyrimidine derivatives were reported to possess anticonvulsant, antimicrobial, anti-inflammatory, antitumor, and antihistaminic. Recently, our team reported the anti-inflammatory and antimicrobial evaluation of some pyrimidines. OBJECTIVE: To synthesize, predict and evaluate biological activity of some 2-(N,N-dimethyl guanidinyl)-4,6-diaryl pyrimidines...
July 2016: Journal of Pharmacy & Bioallied Sciences
Jordan A Berg, Bryan D Merrill, Justin T Crockett, Kyle P Esplin, Marlee R Evans, Karli E Heaton, Jared A Hilton, Jonathan R Hyde, Morgan S McBride, Jordan T Schouten, Austin R Simister, Trever L Thurgood, Andrew T Ward, Donald P Breakwell, Sandra Hope, Julianne H Grose
Brevibacillus laterosporus is a spore-forming bacterium that causes a secondary infection in beehives following European Foulbrood disease. To better understand the contributions of Brevibacillus bacteriophages to the evolution of their hosts, five novel phages (Jenst, Osiris, Powder, SecTim467, and Sundance) were isolated and characterized. When compared with the five Brevibacillus phages currently in NCBI, these phages were assigned to clusters based on whole genome and proteome synteny. Powder and Osiris, both myoviruses, were assigned to the previously described Jimmer-like cluster...
2016: PloS One
David A Hanna, Raven M Harvey, Osiris Martinez-Guzman, Xiaojing Yuan, Bindu Chandrasekharan, Gheevarghese Raju, F Wayne Outten, Iqbal Hamza, Amit R Reddi
Heme is an essential cofactor and signaling molecule. Heme acquisition by proteins and heme signaling are ultimately reliant on the ability to mobilize labile heme (LH). However, the properties of LH pools, including concentration, oxidation state, distribution, speciation, and dynamics, are poorly understood. Herein, we elucidate the nature and dynamics of LH using genetically encoded ratiometric fluorescent heme sensors in the unicellular eukaryote Saccharomyces cerevisiae We find that the subcellular distribution of LH is heterogeneous; the cytosol maintains LH at ∼20-40 nM, whereas the mitochondria and nucleus maintain it at concentrations below 2...
July 5, 2016: Proceedings of the National Academy of Sciences of the United States of America
Osiris A Valdez Banda, Floris Goerlandt, Vladimir Kuzmin, Pentti Kujala, Jakub Montewka
The wintertime maritime traffic operations in the Gulf of Finland are managed through the Finnish-Swedish Winter Navigation System. This establishes the requirements and limitations for the vessels navigating when ice covers this area. During winter navigation in the Gulf of Finland, the largest risk stems from accidental ship collisions which may also trigger oil spills. In this article, a model for managing the risk of winter navigation operations is presented. The model analyses the probability of oil spills derived from collisions involving oil tanker vessels and other vessel types...
July 15, 2016: Marine Pollution Bulletin
Sy-Jou Chen, Yi-Ju Chen, Chui-Hsuan Cheng, Hei-Fen Hwang, Chih-Yi Chen, Mau-Roung Lin
A prospective study was conducted to compare criterion, predictive, and construct validities of 9 fracture/osteoporosis assessment tools, including calcaneal quantitative ultrasonography (QUS), Age Bulk One or Never Estrogens (ABONE), body weight criterion (BWC), Fracture Risk Assessment Tool (FRAX), Garvan fracture risk calculator (GARVAN), Osteoporosis Risk Assessment Instrument (ORAI), Osteoporosis Index of Risk (OSIRIS), Osteoporosis Self-Assessment Tool for Asians (OSTA), and Simple Calculated Osteoporosis Risk Estimation (SCORE), among older men and women in Taiwan...
May 2016: Medicine (Baltimore)
Manathip Osiri, Jongkonnee Wongpiyabovorn, Youwanuch Sattayasomboon, Niramol Thammacharoenrach
The objective of this study was to compare the effects of treatment by combined conventional disease-modifying antirheumatic drugs (cDMARDs) or biologics on cytokines, disease activity, and function in rheumatoid arthritis (RA). Sera from a cohort of 81 patients with long-standing RA treated with combined cDMARDs or biologics were measured for 12 cytokines. Comparisons of serum cytokine concentrations with treatment types (combination 2, 3 cDMARDs or biologics), serologic status (positivity for RF and anti-cyclic citrullinated peptide antibody (anti-CCP Ab)), DAS28-ESR, and function were performed...
July 2016: Clinical Rheumatology
Ayarivan Puratchikody, Dharmaraj Sriram, Appavoo Umamaheswari, Navabshan Irfan
BACKGROUND: Drugs that inhibit cyclooxygenase-2 (COX-2) while sparing cyclooxygenase-1 (COX-1) represent a new attractive therapeutic development and offer new perspective for further use of COX-2 inhibitors. Intention of this work is to develop safer, selective COX-2 inhibitors that do not produce harmful effects. RESULTS: A series of 55 tyrosine derivatives were designed for evaluation as selective COX-2 inhibitors and investigated by in silico for their anti-inflammatory activities using C-Docker...
2016: Chemistry Central Journal
Laura de Andrade Moura, Ana Carolina Marqui de Almeida, Andreza Vieira da Silva, Vivian Rodrigues de Souza, Vitor Francisco Ferreira, Michel Vieira Menezes, Carlos Roland Kaiser, Sabrina Baptista Ferreira, André Lopes Fuly
BACKGROUND: Cardiovascular diseases, such as thrombosis and stroke, represent the major cause of disability and death worldwide; and dysfunctions in platelet aggregation and blood coagulation processes are involved. The regular antithrombotic drugs have unsatisfactory results and may produce side effects. Therefore, alternative therapies have been extensively investigated. OBJECTIVE: The anticoagulant and antiplatelet aggregation potential of a series of six synthetic 1,2,3-triazole derivatives were investigated through in vitro models...
May 2, 2016: Medicinal Chemistry
Ramya Sugumar, Abhinand Ponneri Adithavarman, Anusha Dakshinamoorthi, Darling Chellathai David, Padmavathi Kannan Ragunath
INTRODUCTION: Pneumocystis jirovecii is a fungus that causes Pneumocystis pneumonia in HIV and other immunosuppressed patients. Treatment of Pneumocystis pneumonia with the currently available antifungals is challenging and associated with considerable adverse effects. There is a need to develop drugs against novel targets with minimal human toxicities. Histone Acetyl Transferase (HAT) Rtt109 is a potential therapeutic target in Pneumocystis jirovecii species. HAT is linked to transcription and is required to acetylate conserved lysine residues on histone proteins by transferring an acetyl group from acetyl CoA to form e-N-acetyl lysine...
March 2016: Journal of Clinical and Diagnostic Research: JCDR
Andreas Vilcinskas, Heiko Vogel
The European map butterfly (Araschnia levana) is a classic example of seasonal polyphenism because the spring and summer imagoes display two distinct morphological phenotypes. The light regime and temperature during larval and prepupal development determine whether or not the pupae commit to diapause and overwintering and thus whether spring or summer imagoes emerge. We used suppression subtractive hybridization to experimentally screen for genes that are differentially expressed in prepupae committed either to accelerated metamorphosis and egg production or diapause and overwintering...
April 20, 2016: Ecology and Evolution
Rashmi Shukla, Ajeet Pal Singh, Pankaj K Sonar, Mudita Mishra, Shailendra K Saraf
A series of Schiff bases of benzothiazol-2-ylamine/thiazolo [5, 4-b] pyridin-2-ylamine was synthesized. Aniline/4-aminopyridine was converted to the corresponding thiourea derivatives, which were cyclized to obtain benzothiazol-2-ylamine/thiazolo [5, 4-b] pyridin-2-ylamine. Finally, these were condensed with various aromatic and heteroaromatic aldehydes to obtain twelve (I-XII) novel Schiff bases of benzothiazol-2-ylamine and thiazolo [5, 4-b] pyridin-2-ylamine. The synthesized compounds were characterized by spectral analysis and screened for their anticonvulsant activity using maximal electroshock (MES) test and isoniazid (INH) induced convulsions test, with phenytoin and diazepam, respectively, as the standard drugs...
April 28, 2016: Central Nervous System Agents in Medicinal Chemistry
Marius-Ionuţ Iuraşcu, Osiris Marroquin Belaunzanar, Claudia Cozma, Ulf Petrausch, Christoph Renner, Michael Przybylski
HLA-B27 homodimer formation is believed to be a hallmark of HLA-B27 associated spondyloarthritides. Recently, we have generated a homodimer-specific monoclonal antibody (HD6) and have demonstrated that HLA-B27 homodimer complexes are present on monocytes of healthy HLA-B27 gene carriers at low levels, with significantly increased levels at active disease. The capability of the HD6 antibody to discriminate between correctly formed HLA-B27 heterotrimers and pathology-associated homodimers is striking and cannot be explained by the primary structure of HLA-B27...
June 2016: Journal of the American Society for Mass Spectrometry
Naveen Polkam, Venkat Ragavan Ramaswamy, Parsharamulu Rayam, Tejeswara Rao Allaka, Hasitha Shilpa Anantaraju, Sriram Dharmarajan, Yogeeswari Perumal, Durgaiah Gandamalla, Narsimha Reddy Yellu, Sridhar Balasubramanian, Jaya Shree Anireddy
A series of new edaravone derivatives 3-7 have been synthesized, characterised using various spectroscopic techniques and screened for their in vitro anti-cancer, antioxidant activities. Structure of 5d was further substantiated through single crystal X-ray diffraction. Among the tested, 5l exhibited pronounced activity against PC3 cancer cells. Compounds 5i, 5l, 7c showed potent activity against A549 cancer cells. Products 5k, 6, 7c demonstrated good antioxidant activity with MIC values of 18.60, 16.27, 16...
May 15, 2016: Bioorganic & Medicinal Chemistry Letters
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"