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Current Topics in Medicinal Chemistry

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https://www.readbyqxmd.com/read/29998807/antibacterial-activity-and-time-kill-kinetics-of-positive-enantiomer-of-%C3%AE-pinene-against-strains-of-staphylococcus-aureus-and-escherichia-coli
#1
Leticia de Sousa Eduardo, Ticiane Costa Farias, Siluana Benvindo Ferreira, Paula Benvindo Ferreira, Zilka Nanes Lima, Savio Benvindo Ferreira
Research into new antimicrobial agents is needed, as more and more microorganisms that cause antibiotic-resistant diseases are emerging commercially. In this group we can find strains of Staphylococcus aureus and Escherichia coli, which are highly opportunistic species. Faced with this perspective, research using essential oils present in plants is emerging as a therapeutic alternative for the treatment of antimicrobial infections. Many of these oils have, in their composition, monoterpene α-pinene, which shows to have antibacterial activity...
July 11, 2018: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/29998806/obtaining-microbiological-and-pharmacokinetic-highly-predictive-equations
#2
Jose I Bueso-Bordils, Pedro A Aleman-Lopez, Sara Costa-Piles, Maria J Duart, Luis Lahuerta-Zamora, Rafael Martin-Algarra, Gerardo M Anton-Fos
In this paper, a multilinear regression (MLR) analysis has been carried out in order to accurately predict physicochemical properties and biological activities on a group of antibacterial quinolones by means of a set of structural descriptors called topological indices. The aim of this work is to develop prediction equations for these properties after collecting the maximum number of data from the literature on antibacterial quinolones. The five regression functions selected by presenting the best combination of various statistical parameters, subsequently validated by means of internal validation (intercorrelation, Y-randomization and leave-one-out cross-validation tests), allowed the reliable prediction of minimum inhibitory concentration 50 versus Staphylococcus aureus (MIC50Sa), Streptococcus pyogenes (MIC50Spy) and Bacteroides fragilis (MIC50Bf), mean residence time (MRT) after oral administration and volume of distribution (VD)...
July 11, 2018: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/29992885/toward-reproducible-results-from-targeted-metabolomic-studies-perspectives-for-data-pre-processing-and-a-basis-for-analytic-pipeline-development
#3
Thomas Gross, Mark Mapstone, Ricardo Miramontes, Robert Padilla, Amrita K Cheema, Fabio Macciardi, Howard J Federoff, Massimo S Fiandaca
Contemporary metabolomics experiments generate a rich array of complex high-dimensional data. Consequently, there have been concurrent efforts to develop methodological standards and analytical workflows to streamline the generation of meaningful biochemical and clinical inferences from raw data generated using an analytical platform like mass spectrometry. While such considerations have been frequently addressed in untargeted metabolomics (i.e., the broad survey of all distinguishable metabolites within a sample of interest), this methodological scrutiny has seldom been applied to data generated using commercial, targeted metabolomics kits...
July 11, 2018: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/29992884/role-of-morin-in-neurodegenerative-diseases-a-review
#4
Ritu Kataria, Eduardo Sobarzo-Sanchez, Anurag Khatkar
Neurodegenerative diseases are likely to be emerged as the second cause of mortality in the world in coming years. NDDs causes tremendous financial burden on the healthcare system along with profound effect on families and patient. Disease-modifying treatment strategies with proven efficacy for these disorders are still lacking. Documentation proved that oxidative stress plays leading role in the pathophysiology of many neurodegenerative disorders. Molecules with good antioxidant profile could be explored for the doctoring of these conditions...
July 11, 2018: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/29992883/intervention-and-observational-trials-are-complementary-in-metabolomics-diabetes-and-the-oral-glucose-tolerance-test
#5
Alvaro Gonzalez-Dominguez, Alfonso Maria Lechuga-Sancho, Raul Gonzalez-Dominguez
Observational experimental designs are usually employed in metabolomics to elucidate pathological mechanisms underlying disease development and to discover candidate biomarkers for diagnosis. However, intervention trials can also be a suitable starting point before performing a validation study in lager epidemiological cohorts, with a great potential in personalized medicine to investigate how different patients respond to similar stimuli. In the present work, we provide a review of the literature on the application of metabolomics to investigate metabolic alterations associated with diabetes, the diabetes predisposing state of insulin resistance and the oral glucose tolerance test as a case study to demonstrate the complementarity of observational and interventional study designs...
July 11, 2018: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/29992882/inhibition-of-biofilm-and-virulence-factors-of-candida-albicans-by-partially-purified-secondary-metabolites-of-streptomyces-chrestomyceticus-strain-adp4
#6
Ashok K Dubey, Vartika Srivastava, Rajeev K Singla
BACKGROUND: Despite of several advancements in antifungal drug discovery, fungal diseases like Invasive Candidiasis (IC) still remains associated with high rates of morbidity and mortality worldwide. Thus there is an enormous need for anti-Candida drugs. OBJECTIVE: The main objectives of the work included: 1. To investigate therapeutically significant classes of secondary metabolites produced by S. chrestomyceticus strain ADP4. 2. To investigate and analyze inhibition of significant virulence attributes of C...
July 11, 2018: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/29943703/synthesis-characterization-antimicrobial-and-antioxidant-potential-of-diazenyl-chalcones
#7
Harmeet Kaur, Balasubramanian Narasimhan
A series of diazenyl chalcones was prepared by base catalyzed Claisen-Schmidt condensation of synthesized hydroxy substituted acetophenone azo dye with various substituted aromatic/heteroaromatic aldehydes. The structural conformation of synthesized chalcones was done by a number of physicochemical and spectral means like FTIR, UV-visible, mass, NMR spectroscopy and CHNS/O analysis. These diazenyl chalcones were assessed for their in vitro antimicrobial potential against several Gram-negative, Gram-positive bacterial and fungal strains by serial tube dilution method...
June 25, 2018: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/29895251/ocular-inflammation-and-depression-ophthalmologists-perspective
#8
Hande Taylan Sekeroglu, Mehmet Ali Sekeroglu
Major depression is one of the most common psychiatric disorders in the developed countries, and it is well known that depressive symptoms are more frequently encountered in patients with physical disorders, especially those who have chronic diseases. Although there are numerous study concerning the relationship between ocular inflammatory diseases and depression, the majority of them mainly focus on two diseases: uveitis and dry eye disease (DED). With this review, we aimed to analyze the relation between depression and ocular inflammation, specifically DED and uveitis, in the light of the current literature and to summarize the potential mechanisms regarding this interrelation...
June 12, 2018: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/29886831/improving-the-efficacy-of-anticancer-drugs-via-encapsulation-and-acoustic-release
#9
Salma E Ahmed, Nahid Awad, Vinod Paul, Hesham G Moussa, Ghaleb A Husseini
Conventional chemotherapeutics lack the specificity and controllability, thus may poison healthy cells while attempting to kill cancerous ones. Newly developed nano-drug delivery systems have shown promise in delivering anti-tumor agents with enhanced stability, durability and overall performance; especially when used along with targeting and triggering techniques. This work traces back the history of chemotherapy, addressing the main challenges that have encouraged the medical researchers to seek a sanctuary in nanotechnological-based drug delivery systems that are grafted with appropriate targeting techniques and drug release mechanisms...
June 8, 2018: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/29875003/current-status-and-future-prospects-of-small-molecule-protein-protein-interaction-ppi-inhibitors-of-tumor-necrosis-factor-tnf-and-receptor-activator-of-nf-%C3%AE%C2%BAb-ligand-rankl
#10
Georgia Melagraki, Georgios Leonis, Evangelos Ntougkos, Vagelis Rinotas, Christos Papaneophytou, Thomas Mavromoustakos, George Kontopidis, Eleni Douni, George Kollias, Antreas Afantitis
The overexpression of Tumor Necrosis Factor (TNF) is directly related to the development of several autoimmune diseases, such as rheumatoid and psoriatic arthritis, inflammatory bowel disease, Crohn's disease, refractory asthma, and multiple sclerosis. Receptor activator of nuclear factor kappa-B ligand (RANKL) belongs to the TNF family, and is the primary mediator of osteoclast-induced bone resorption through interaction with its receptor RANK. The function of RANKL is physiologically inhibited by the action of osteoprotegerin (OPG), which is a decoy receptor that binds to RANKL and prevents the process of osteoclastogenesis...
June 6, 2018: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/29875002/physicochemical-characterization-and-antinociceptive-effect-of-%C3%AE-cyclodextrin-lippia-pedunculosa-essential-oil-in-mice
#11
Paula Dos Passos Menezes, Francielly de Oliveira Araujo, Tatianny Araujo Andrade, Igor Araujo Santos Trindade, Heitor Gomes de Araujo-Filho, Jullyana de Souza Siqueira Quintans, Lucindo Jose Quintans-Junior, Emmanoel Vilaca Costa, Leociley Rocha Alencar Menezes, Reinaldo Nobrega de Almeida, Renan Marinho Braga, Mairim Russo Serafini, Adriano Antunes de Souza Araujo
BACKGROUND: Some researches have been shown that Lippia pedunculosa essential oil (EOLP) has interesting biological activities. However, its low water solubility is the main challenge to achieve its therapeutic potential. In this context, cyclodextrins (CDs) have been widely used in order to overcame this problem due to your capability to improve the physicochemical properties of drugs. OBJECTIVE: In this perspective, the main goal of this study was to investigate how the improvement of the physicochemical properties of inclusion complexes (EOLP and β-CD) enhance the antinociceptive effect in mice...
June 6, 2018: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/29866009/onion-and-garlic-extracts-potentiates-the-efficacy-of-conventional-antibiotics-against-standard-and-clinical-bacterial-isolates
#12
Fawzi Mahomoodally, Simla Ramcharun, Gokhan Zengin
INTRODUCTION: Onion (Allium cepa L.) and garlic (Allium sativum L.) extracts are traditionally used in many cultures as antimicrobial agents. Nonetheless, there is still a dearth of scientific validation pertaining to the antibacterial and possible antibiotic potentiating activity of these plants. METHODS: Decoction as traditionally used and methanol, ethanol, ethyl acetate, and acetone extracts of onion and garlic were evaluated for their antibacterial activity against 15 bacterial strains (6 ATCC strains and 9 clinical isolates) using the broth microdilution method to establish the minimum inhibitory concentration...
June 3, 2018: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/29866008/prediction-and-targeting-of-interaction-interfaces-in-g-protein-coupled-receptor-oligomers
#13
Anke C Schiedel, Meryem Kose, Carlos Barreto, Beatriz Bueschbell, Giulia Morra, Ozge Sensoy, Irina S Moreira
BACKGROUND: Communication within a protein complex is mediated by physical interactions made among the protomers. Evidence for both the allosteric regulation present among the protomers of the protein oligomer and of the direct effect of membrane composition on this regulation has made it essential to investigate the underlying molecular mechanism that drives oligomerization, the type of interactions present within the complex, and to determine the identity of the interaction interface...
June 3, 2018: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/29866007/an-update-on-mdmx-and-dual-mdm2-x-inhibitors
#14
Margarida Espadinha, Valentina Barcherini, Elizabeth A Lopes, Maria M M Santos
The tumor suppressor protein p53 is inactivated in all type of human cancers, either by negative regulation, either by mutation or deletion of its gene. Specifically, in tumors that retain wild-type (wt) p53 status, p53 is inactivated by interaction with negative regulators, such as MDM2 and MDMX. These two proteins are found to be overexpressed in several different types of cancers, and the restoration of p53 activity by inhibition of these proteins is now considered an important approach for cancer treatment...
June 3, 2018: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/29852872/a-structural-perspective-on-the-modulation-of-protein-protein-interactions-with-small-molecules
#15
Habibe Cansu Demirel, Tunca Dogan, Nurcan Tuncbag
Protein-protein interactions (PPIs) are the key components in many cellular processes including signaling pathways, enzymatic reactions and epigenetic regulation. Abnormal interactions of some proteins may be pathogenic and cause various disorders including cancer and neurodegenerative diseases. Although inhibiting PPIs with small molecules is a challenging task, it gained an increasing interest because of its strong potential for drug discovery and design. The knowledge of the interface as well as the structural and chemical characteristics of the PPIs and their roles in the cellular pathways are necessary for a rational design of small molecules to modulate PPIs...
May 31, 2018: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/29848279/toward-small-molecule-inhibition-of-protein-protein-interactions-general-aspects-and-recent-progress-in-targeting-costimulatory-and-coinhibitory-immune-checkpoint-interactions
#16
Damir Bojadzic, Peter Buchwald
Protein-protein interactions (PPIs) that are part of the costimulatory and coinhibitory (immune checkpoint) signaling are critical for adequate T cell response and are important therapeutic targets for immunomodulation. Biologics targeting them have already achieved considerable clinical success in the treatment of autoimmune diseases or transplant recipients (e.g., abatacept, belatacept, and belimumab) as well as cancer (e.g., ipilimumab, nivolumab, pembrolizumab, atezolizumab, durvalumab, and avelumab). In view of such progress, there have been only relatively limited efforts toward developing small-molecule PPI inhibitors (SMPPIIs) targeting these cosignaling interactions, possibly because they, as all other PPIs, are difficult to target by small molecules and were not considered druggable...
May 30, 2018: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/29807517/evaluation-of-in-vitro-antimicrobial-potential-of-daphne-retusa-hemsl-against-human-pathogenic-bacteria-and-fungi
#17
Jamila Nawab, Shafiq Ahmad Tariq, Naeem Khan, Sadia Nawab, Muhammad Raza Shah, Syed Ashad Haleemi, Haroon Khan
BACKGROUND: Antimicrobial drugs resistance is an emerging problem and leads to failure of control of infectious diseases by adversely affecting patient care and reducing effective management of infectious diseases globally. Thus warranting search for new and more effective alternatives. Daphne retusa Hemsl (Daphne) has medicinal values and is reported to be widely used in curing variety of human ailments. OBJECTIVE: Current study assesses in-vitro antimicrobial activity of the crude extract of D...
May 28, 2018: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/29807516/emerging-virulence-drug-resistance-and-future-anti-fungal-drugs-for-candida-pathogens
#18
Vartika Srivastava, Rajeev Kumar Singla, Ashok Kumar Dubey
Increased incidences of Candida infection have augmented morbidity and mortality in human population, particularly among severely immunocompromised patients and those having long stay in hospitals (nosocomial infections). Many virulence factors and fitness attributes are reported to be associated with the pathogenicity of Candida sp. It can cause infections ranging from easily treatable superficial type to life-threatening invasive infections. Additionally, it has the capability to infect humans of all age groups...
May 28, 2018: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/29807515/multi-target-antitubercular-drugs
#19
Jessika de Oliveira Viana, Hamilton Mitsugu Ishiki, Marcus Tullius Scotti, Luciana Scotti
Tuberculosis is an infectious disease caused by Mycobacterium tuberculosis, which has high levels of mortality worldwide and has already gained resistance to first- and second-line drugs. The study by new chemical entities with promising activities becomes paramount to broaden the therapeutic strategies in the cure of the patients affected with this disease. In this context, in this review we report the discovery of 3 classes of compounds that can simultaneously interact with more than one target of Mycobacterium tuberculosis...
May 28, 2018: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/29793408/recent-development-of-small-molecule-glutaminase-inhibitors
#20
Minsoo Song, Soong-Hyun Kim, Chun Young Im, Hee-Jong Hwang
Glutaminase (GLS) which is responsible for the conversion of glutamine to glutamate plays vital role in up-regulating cell metabolism for tumor cell growth, and is considered as a valuable therapeutic target for cancer treatment. Based on this important function of glutaminase in cancer, several GLS inhibitors have been developed from both academia and industries. Most importantly, Calithera Biosciences Inc. is actively developing glutaminase inhibitor CB-839 for the treatment of various cancers in phase 1 and 2 clinical trials at present...
May 24, 2018: Current Topics in Medicinal Chemistry
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