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https://www.readbyqxmd.com/read/29793211/synthesis-and-evaluation-of-novel-triazolyl-quinoline-derivatives-as-potential-antileishmanial-agents
#1
Akanksha Upadhyay, Pragati Kushwaha, Sampa Gupta, Ranga Prasad Dodda, Karthik Ramalingam, Ruchir Kant, Neena Goyal, Koneni V Sashidhara
The high potential of quinoline containing natural products and their derivatives in medicinal chemistry led us to discover novel series of 25 compounds for the development of new antileishmanial agents. A series of triazolyl 2-methyl-4-phenylquinoline-3-carboxylate derivatives has been synthesized via click chemistry inspired molecular hybridization approach and evaluated against Leishmania donovani. Most of the screened derivatives exhibited significant in vitro anti-leishmanial activity against promastigote (IC50 ranging from 2...
May 12, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29793188/prioritization-of-reproductive-toxicants-in-unconventional-oil-and-gas-operations-using-a-multi-country-regulatory-data-driven-hazard-assessment
#2
Salmaan H Inayat-Hussain, Masao Fukumura, A Muiz Aziz, Chai Meng Jin, Low Wei Jin, Rolando Garcia-Milian, Vasilis Vasiliou, Nicole C Deziel
BACKGROUND: Recent trends have witnessed the global growth of unconventional oil and gas (UOG) production. Epidemiologic studies have suggested associations between proximity to UOG operations with increased adverse birth outcomes and cancer, though specific potential etiologic agents have not yet been identified. To perform effective risk assessment of chemicals used in UOG production, the first step of hazard identification followed by prioritization specifically for reproductive toxicity, carcinogenicity and mutagenicity is crucial in an evidence-based risk assessment approach...
May 21, 2018: Environment International
https://www.readbyqxmd.com/read/29792965/characterization-sulfated-modification-and-bioactivity-of-a-novel-polysaccharide-from-millettia-dielsiana
#3
Zhonghua Wang, Tongqiang Cai, Xipu He
Millettia dielsiana is a traditional herb medicine to treat rheumatic arthritis and gynecological diseases. In this study, a novel polysaccharide (MDP1) with a molecular weight of 139.54 kDa was isolated from Millettia dielsiana by DEAE-52 cellulose chromatography. Its sulfated derivative (S-MDP1) was prepared by the chlorosulfonic acid-pyridine method. Structural analysis indicated that MDP1 was a pectic polysaccharide and did not exhibit a triple helical conformation. In vitro, MDP1 and S-MDP1 had protective effect on H2 O2 -induced PC12 cells death...
May 21, 2018: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/29792906/four-novel-antibacterial-sesquiterpene-%C3%AE-amino-acid-quaternary-ammonium-hybrids-from-the-mycelium-of-mushroom-stereum-hirsutum
#4
Yuan-Chang Duan, Jun Feng, Na Bai, Guo-Hong Li, Ke-Qin Zhang, Pei-Ji Zhao
The mushroom Stereum hirsutum is parasitized by Tremella aurantia to form a heterogeneous basidiocarp Jin'er, which has been used as food and folk medicine in Chinese society. In present work, the S. hirsutum was fermented in YMG broth, and four novel mixed terpenes, stereumamides A-D (1-4), which are sesquiterpenes combined with α-amino acids to form quaternary ammonium hybrids, were isolated from the Stereum hirsutum FP-91666 and their structures were elucidated by spectroscopic data analysis. Stereumamides A and D showed antibacterial activity against Escherichia coli, Staphylococcus aureus, and Salmonella typhimurium, with the minimum inhibitory concentration (MIC) values of 12...
May 21, 2018: Fitoterapia
https://www.readbyqxmd.com/read/29792865/aspirin-restores-abt-737-mediated-apoptosis-in-human-renal-carcinoma-cells
#5
Yen-Chuan Ou, Jian-Ri Li, Jiaan-Der Wang, Wen-Ying Chen, Yu-Hsiang Kuan, Ching-Ping Yang, Su-Lan Liao, Hsi-Chi Lu, Chun-Jung Chen
Aspirin is a novel chemopreventive agent against malignancy. However, outcomes of aspirin monotherapy of renal cell carcinoma (RCC) are inconsistent across studies. ABT-737, an BH3 mimetic inhibitor, is also a promising antitumor drug. Cancer cells including those from RCC, that have high levels of Mcl-1, are refractory to ABT-737-induced apoptosis. We here investigated how aspirin treatment modulates the ABT-737-induced apoptosis. Using the in vitro model of human 786-O cells, we showed that aspirin had sensitized cells to ABT-737 induced apoptosis...
May 21, 2018: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/29792814/perspectives-of-a-myosin-motor-activator-agent-with-increased-selectivity
#6
Peter Nanasi, Istvan Komaromi, Janos Almassy
Clinical treatment of heart failure is still not fully solved. A novel class of agents, the myosin motor activators, acts directly on cardiac myosin resulting in an increased force generation and prolongation of contraction. Omecamtiv mecarbil, the lead molecule of this group, is now in human 3 phase displaying promising clinical performance. However, omecamtiv mecarbil is not selective to myosin, since it readily binds to and activates cardiac ryanodine receptors (RyR-2), an effect that may cause complications is case of overdose...
May 24, 2018: Canadian Journal of Physiology and Pharmacology
https://www.readbyqxmd.com/read/29792427/native-chemical-ligation-photodesulfurization-in-flow
#7
Timothy S Chisholm, Daniel Clayton, Luke J Dowman, Jessica Sayers, Richard J Payne
Native chemical ligation (NCL) combined with desulfurization chemistry has revolutionized the way in which large polypeptides and proteins are accessed by chemical synthesis. Herein, we outline the use of flow chemistry for the ligation-based assembly of polypeptides. We also describe the development of a novel photodesulfurization transformation that, when coupled with flow NCL, enables efficient access to native polypeptides on time scales up to 2 orders of magnitude faster than current batch NCL-desulfurization methods...
May 24, 2018: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/29792415/two-photon-active-organotin-iv-complexes-for-antibacterial-function-and-superresolution-bacteria-imaging
#8
Lei Hu, Hui Wang, Tingting Xia, Bin Fang, Yu Shen, Qiong Zhang, Xiaohe Tian, Hongping Zhou, Jieying Wu, Yupeng Tian
Antibacterial agents with two-photon absorption are expected to play a significant role in biomedical science. Herein, two novel organotin complexes, HLSn1 and HLSn2, based on coumarin were designed, synthesized, and systematically investigated. It was found that these complexes possessed suitable two-photon-active cross sections in the near-infrared region. Moreover, complex HLSn1 could efficiently inhibit the growth of Gram-negative Escherichia coli and Gram-positive Bacillus subtilis, especially the latter with a minimum inhibitory concentration (MIC; 90%) of 2 ± 0...
May 24, 2018: Inorganic Chemistry
https://www.readbyqxmd.com/read/29792357/synthesis-and-in-vivo-anti-ulcer-evaluation-of-some-novel-piperidine-linked-dihydropyrimidinone-derivatives
#9
Mashooq Ahmad Bhat, Mohamed A Al-Omar, Ahmed M Naglah
Dihydropyrimidinone derivatives containing piperidine moiety were synthesised in a good yield. All the compounds were confirmed by elemental analysis and spectral data. Anti-ulcer activity of novel dihydropyrimidinone-piperidine hybrids (1-18) was evaluated. Among them, four compounds (3, 8, 11 and 15) were found to be most active in 80% ethanol-induced ulcer experimental animal model. All the potent compounds were further evaluated for anti-ulcer activity by different in vivo anti-ulcer models to study the effect of compounds on anti-secretory and cytoprotective activities...
December 2018: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/29792343/plasma-initiated-graft-polymerization-as-an-immobilization-platform-for-metal-free-russian-propolis-ethanol-extracts-designed-specifically-for-biomaterials
#10
Ashwin Ambi, Carolina Vera, Nisharg Parikh, Naidel Perez, Anthony Lopez Rojas, Sanket Kumar, Christopher Stradford, Katherine Borbon, Julia Bryan, Christian Traba
The antibacterial and anti-biofilm activities of propolis have been intensively reported. However, the application of this folk remedy as a means to prevent biomedical implant contamination has yet to be completely evaluated. In response to the significant resistant and infectious attributes of biofilms, biomaterials engineered to possess specific chemical and physical properties were immobilized with metal free Russian propolis ethanol extracts (MFRPEE), a known antibacterial agent. The results obtained from this study begin to examine the application of MFRPEE as a novel alternative method for the prevention of medical and biomedical implant infections...
May 24, 2018: Biofouling
https://www.readbyqxmd.com/read/29792199/nanoparticle-delivery-of-grape-seed-derived-proanthocyanidins-to-airway-epithelial-cells-dampens-oxidative-stress-and-inflammation
#11
S Castellani, A Trapani, A Spagnoletta, L di Toma, T Magrone, S Di Gioia, D Mandracchia, G Trapani, E Jirillo, M Conese
BACKGROUND: Chronic respiratory diseases, whose one of the hallmarks is oxidative stress, are still incurable and need novel therapeutic tools and pharmaceutical agents. The phenolic compounds contained in grape are endowed with well-recognized anti-oxidant, anti-inflammatory, anti-cancer, and anti-aging activities. Considering that natural anti-oxidants, such as proanthocyanidins, have poor water solubility and oral bioavailability, we have developed a drug delivery system based on solid lipid nanoparticles (SLN), apt to encapsulate grape seed extract (GSE), containing proanthocyanidins...
May 23, 2018: Journal of Translational Medicine
https://www.readbyqxmd.com/read/29792190/novel-insights-into-neuroinflammation-bacterial-lipopolysaccharide-tumor-necrosis-factor-%C3%AE-and-ureaplasma-species-differentially-modulate-atypical-chemokine-receptor-3-responses-in-human-brain-microvascular-endothelial-cells
#12
Christine Silwedel, Christian P Speer, Axel Haarmann, Markus Fehrholz, Heike Claus, Mathias Buttmann, Kirsten Glaser
BACKGROUND: Atypical chemokine receptor 3 (ACKR3, synonym CXCR7) is increasingly considered relevant in neuroinflammatory conditions, in which its upregulation contributes to compromised endothelial barrier function and may ultimately allow inflammatory brain injury. While an impact of ACKR3 has been recognized in several neurological autoimmune diseases, neuroinflammation may also result from infectious agents, including Ureaplasma species (spp.). Although commonly regarded as commensals of the adult urogenital tract, Ureaplasma spp...
May 23, 2018: Journal of Neuroinflammation
https://www.readbyqxmd.com/read/29792150/synthesis-and-biological-evaluation-of-novel-2-3-disubstituted-benzofuran-analogues-of-gaba-as-neurotropic-agents
#13
Arturo Coaviche-Yoval, Hector Luna, Ricardo Tovar-Miranda, Marvin Antonio Soriano-Ursua, Jose G Trujillo-Ferrara
BACKGROUND: Benzofurans are heterocyclic compounds with neurotropic activity. Some have been developed for the treatment of acute and degenerative neuronal injuries. OBJECTIVE: To evaluate the in silico binding of some promising benzofurans on the GABA receptors, and the in vivo neurotropic activity of benzofuran analogues (BZF 6-10) of gamma-aminobutyric acid (GABA) on a seizure model. METHODS: The ligands with the best physicochemical attributes were docked on two GABA receptors (the alpha-1 subunit of GABAA-R and GBR1 subunit of GABAB-R)...
May 23, 2018: Medicinal Chemistry
https://www.readbyqxmd.com/read/29792149/inhibition-of-mutated-isocitrate-dehydrogenase-1-in-cancer
#14
Fangrui Wu, Gang Cheng, Yuan Yao, Mari Kogiso, Hong Jiang, Xiao-Nan Li, Yongcheng Song
BACKGROUND: R132H mutation of isocitrate dehydrogenase 1 (IDH1) are found in ~75% of low-grade gliomas and secondary glioblastomas as well as in several other types of cancer. More chemotypes of inhibitors of IDH1(R132H) are therefore needed. OBJECTIVE: To develop a new class of IDH1(R132H) inhibitors as potent antitumor agents. METHOD: A biochemical assay was developed to find inhibitors of IDH1(R132H) mutant enzyme. Chemical synthesis and structure activity relationship studies were used to find compounds with improved potency...
May 23, 2018: Medicinal Chemistry
https://www.readbyqxmd.com/read/29792143/recent-updates-on-novel-approaches-in-insulin-drug-delivery-a-review-of-challenges-and-pharmaceutical-implications
#15
Manisha Pandey, Hira Choudhury, Cheah Xiao Yi, Chen Wei Mun, Goh Khang Ping, Guee Xin Rou, Bhalqish Jeet Kaur A/P Ambar Jeet Singh, Angel Ng Ann Jhee, Lee Kai Chin, Prashant Kesharwani, Bapi Gorain, Zahid Hussain
Diabetes mellitus, a metabolic disorder of glucose metabolism, is mainly associated with insulin resistance to the body cells, or impaired production of insulin by the pancreatic β-cells. Insulin is mainly required to regulate glucose metabolism in type 1 diabetes mellitus patients; however, many patients with type 2 diabetes mellitus also require insulin, especially when their condition cannot be controlled solely by oral hypoglycemic agents. Hence, major researches are ongoing attempting to improve the delivery of insulin in order to make it more convenient to patients who experience side effects from the conventional treatment procedure or non-adherence to insulin regimen due to multiple comorbid conditions...
May 22, 2018: Current Drug Targets
https://www.readbyqxmd.com/read/29792136/zinc-dependent-histone-deacetylase-inhibitors-in-cancer-therapeutics-recent-update
#16
Panagiotis I Georgianos, Maria Divani, Theodoros Eleftheriadis, Peter R Mertens, Vassilios Liakopoulos
BACKGROUND: Despite optimal management of diabetic kidney disease (DKD) with intensive glycemic control and administration of agents blocking the renin-angiotensin-aldosterone-system, the residual risk for nephropathy progression to end-stage-renal-disease (ESRD) remains high. Sodium-glucose co-transporter type 2 (SGLT-2)-inhibitors represent a newly-introduced anti-diabetic drug class with pleiotropic actions extending above their glucose-lowering efficacy. Herein, we provide an overview of preclinical and clinical-trial evidence supporting a protective effect of SGLT-2 inhibitors on DKD...
May 23, 2018: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/29792038/downregulation-of-cancer-stemness-by-novel-diterpenoid-ovatodiolide-inhibits-hepatic-cancer-stem-cell-like-traits-by-repressing-wnt-formula-see-text-catenin-signaling
#17
Mingche Liu, Oluwaseun Adebayo Bamodu, Kuang-Tai Kuo, Wei-Hwa Lee, Yen-Kuang Lin, Alexander T H Wu, Hsiao M, Yew-Min Tzeng, Chi-Tai Yeh, Jo-Ting Tsai
The hierarchical tumor propagation or cancer stem cells (CSCs) model of carcinogenesis postulates that like physiologic adult stem cell (ASC), the CSCs positioned at the apex of any tumor population form the crux of tumor evolution with a constitutive regenerative capacity and differentiation potential. The propagation and recurrence of the characteristically heterogeneous and therapy-resistant hepatocellular carcinoma (HCC), adds to accumulating evidence to support this CSCs model. Based on the multi-etiologic basis of HCC formation which among others, focuses on the disruption of the canonical Wnt signaling pathway, this study evaluated the role of cembrane-type phytochemical, Ovatodiolide, in the modulation of the Wnt/[Formula: see text]-catenin pathway, and its subsequent effect on liver CSCs' activities...
May 24, 2018: American Journal of Chinese Medicine
https://www.readbyqxmd.com/read/29791869/ghrelin-and-the-heart
#18
Takeshi Tokudome, Kentaro Otani, Mikiya Miyazato, Kenji Kangawa
Ghrelin, a growth hormone-releasing peptide that was first discovered in the stomach of rats in 1999, is an endogenous ligand of growth hormone secretagogue receptor. Ghrelin exerts its potent growth hormone-releasing and orexigenic activities by binding to specific receptors in the brain. Subsequent studies showed that ghrelin participates in the regulation of diverse processes, including energy balance, body weight maintenance, and glucose and fat metabolism, and demonstrated that ghrelin is beneficial for treatment of cardiac diseases...
May 20, 2018: Peptides
https://www.readbyqxmd.com/read/29791237/the-future-of-chronic-lymphocytic-leukemia-potential-directions-from-ash-2017
#19
Stefano Molica
Novel targeted therapies - including ibrutinib, venetoclax and idelalisib - have revolutionized the treatment landscape of chronic lymphocytic leukemia (CLL). Therefore, studying combinations of novel agents (NAs) with distinct mechanism of action and non-overlapping toxicities is challenging. Area covered: The 2017 American Society Hematology (ASH) Annual Meeting, has represented a showcase for several trials combining NAs. These studies are currently evaluating the efficacy NA plus anti-CD20 monoclonal antibody, NA plus NA (with or without anti-CD20 monoclonal antibody) and NA plus chemo-immunotherapy...
May 23, 2018: Expert Review of Hematology
https://www.readbyqxmd.com/read/29790931/gsk3%C3%AE-modulates-timing-dependent-long-term-depression-through-direct-phosphorylation-of-kv4-2-channels
#20
Giuseppe Aceto, Agnese Re, Andrea Mattera, Lucia Leone, Claudia Colussi, Marco Rinaudo, Federico Scala, Katia Gironi, Saviana Antonella Barbati, Salvatore Fusco, Thomas Green, Fernanda Laezza, Marcello D'Ascenzo, Claudio Grassi
Spike timing-dependent plasticity (STDP) is a form of activity-dependent remodeling of synaptic strength that underlies memory formation. Despite its key role in dictating learning rules in the brain circuits, the molecular mechanisms mediating STDP are still poorly understood. Here, we show that spike timing-dependent long-term depression (tLTD) and A-type K+ currents are modulated by pharmacological agents affecting the levels of active glycogen-synthase kinase 3 (GSK3) and by GSK3β knockdown in layer 2/3 of the mouse somatosensory cortex...
February 23, 2018: Cerebral Cortex
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