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https://www.readbyqxmd.com/read/28432943/exploration-of-flexible-phenylpropylurea-scaffold-as-novel-cardiac-myosin-activators-for-the-treatment-of-systolic-heart-failure
#1
Manoj Manickam, Hitesh B Jalani, Thanigaimalai Pillaiyar, Niti Sharma, Pulla Reddy Boggu, Eeda Venkateswararao, You-Jung Lee, Eun-Seok Jeon, Sang-Hun Jung
A series of flexible urea derivatives have been synthesized and demonstrated as selective cardiac myosin ATPase activator. Among them 1-phenethyl-3-(3-phenylpropyl)urea (1, cardiac myosin ATPase activation at 10 μM = 51.1%; FS = 18.90; EF = 12.15) and 1-benzyl-3-(3-phenylpropyl)urea (9, cardiac myosin ATPase activation = 53.3%; FS = 30.04; EF = 18.27) showed significant activity in vitro and in vivo. The change of phenyl ring with tetrahydropyran-4-yl moiety viz., 1-(3-phenylpropyl)-3-((tetrahydro-2H-pyran-4-yl)methyl)urea (14, cardiac myosin ATPase activation = 81...
April 7, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28432813/targeting-on-poly-adp-ribose-polymerase-activity-with-dna-damaging-hybrid-lactam-steroid-alkylators-in-wild-type-and-brca1-mutated-ovarian-cancer-cells
#2
Dimitrios T Trafalis, Aikaterini Polonifi, Panayiotis Dalezis, Nikolaos Nikoleousakos, Sotirios Katsamakas, Vassiliki Sarli
Conjugated lactam-steroid alkylators (LSA), have been shown to exhibit superior activity at controlling cancer models and overlap drug resistance to conventional chemotherapy. Hybrid LSAs combine two active compounds in a single molecule and incorporate modified steroids bearing lactam moiety in one or more steroid rings functioning as vectors for cytotoxic agents. We first describe a novel class of LSAs that generate excellent anticancer activity against UWB1.289 and UWB1.289+BRCA1 human ovarian cancer cell lines...
April 22, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28432808/mechanism-of-the-vasorelaxant-effect-induced-by-trans-4-methyl-%C3%AE-nitrostyrene-a-synthetic-nitroderivative-in-rat-thoracic-aorta
#3
Taylena Maria Teófilo, Loeste Arruda-Barbosa, Jussara Mathyelle Rodrigues-Silva, Joyce Karen Lima Vale, Rosivaldo Dos Santos Borges, Gloria Pinto Duarte, Pedro Jorge Caldas Magalhães, Saad Lahlou
Mechanisms underlying the vasorelaxant effects of trans-4-methyl-β-nitrostyrene (T4MeN) were studied in rat aortic rings. In endothelium-intact preparations, T4MeN fully and similarly relaxed contractions induced by phenylephrine (PHE) (IC50 = 61.41 [35.40-87.42] μM) and KCl (IC50 = 83.50 [56.63-110.50] μM). The vasorelaxant effect of T4MeN was unchanged by endothelium removal, pretreatment with L-NAME, indomethacin, tetraethylammonium, ODQ or MDL-12,330A. Under Ca(2+) -free conditions, T4MeN significantly reduced with a similar potency: (i) phasic contractions induced by PHE, but not by caffeine; (ii) contractions due to CaCl2 in aortic preparations stimulated with PHE (in the presence of verapamil) or high KCl; (iii) contractions evoked by the restoration of external Ca(2+) levels after depletion of intracellular Ca(2+) stores in the presence of thapsigargin...
April 22, 2017: Clinical and Experimental Pharmacology & Physiology
https://www.readbyqxmd.com/read/28432725/synthesis-and-biological-potency-of-anilino-triazine-insecticides
#4
Timothy C Johnson, Annette V Brown, Kristy K Bryan, Katherine K Guenthenspberger, Ricky Hunter, Timothy P Martin, Noormohamed Niyaz, Gene F Tisdell, Tony Trullinger
BACKGROUND: An insecticide screening effort identified N-(4-bromophenyl)-4,6-bis(2,2,2-trifluoroethoxy)-1,3,5-triazine-2-amine as having weak potency against two Lepidopteran species, Helicoverpa zea and Spodoptera exigua. A structure activity relationship study about the trifluoroethoxy substituents and the aniline of this compound was carried out in an effort to improve insecticidal potency. RESULTS: Initially, a series of analogs bearing various substituents on the aniline were prepared and the insecticidal potency was evaluated against Helicoverpa zea and Spodoptera exigua in greenhouse diet feeding assays...
April 22, 2017: Pest Management Science
https://www.readbyqxmd.com/read/28432702/tunable-porous-coordination-polymers-for-the-capture-recovery-and-storage-of-inhalation-anesthetics
#5
Brendan Francis Abrahams, David Dharma, Paul Stephen Donnelly, Timothy Adam Hudson, Cameron J Kepert, Richard Robson, Peter D Southon, Keith Forrest White
The uptake of inhalation anesthetics by three topologically identical frameworks is described. The 3D network materials, which possess square channels of different dimensions, are formed from the relatively simple combination of Zn(II) centres and dianionic ligands that contain a phenolate and a carboxylate group at opposite ends. All three framework materials are able to adsorb N2O, Xe and isoflurane. Whilst the framework with the widest channels is able to adsorb large quantities of the various guests from the gas phase, the frameworks with the narrower channels have superior binding enthalpies and exhibit higher levels of retention...
April 22, 2017: Chemistry: a European Journal
https://www.readbyqxmd.com/read/28432632/tryptophan-fluorescence-yields-and-lifetimes-as-a-probe-of-conformational-changes-in-human-glucokinase
#6
Bogumil Zelent, Chris Bialas, Ignacy Gryczynski, Pan Chen, Rahul Chib, Karina Lewerissa, Maria G Corradini, Richard D Ludescher, Jane M Vanderkooi, Franz M Matschinsky
Five variants of glucokinase (ATP-D-hexose-6-phosphotransferase, EC 2.7.1.1) including wild type and single Trp mutants with the Trp residue at positions 65, 99, 167 and 257 were prepared. The fluorescence of Trp in all locations studied showed intensity changes when glucose bound, indicating that conformational change occurs globally over the entire protein. While the fluorescence quantum yield changes upon glucose binding, the enzyme's absorption spectra, emission spectra and fluorescence lifetimes change very little...
April 22, 2017: Journal of Fluorescence
https://www.readbyqxmd.com/read/28432424/variations-of-isovaline-structure-related-to-activity-in-the-formalin-foot-assay-in-mice
#7
Timothy Fung, Yahya I Asiri, Richard Wall, Stephan K W Schwarz, Ernest Puil, Bernard A MacLeod
Current centrally acting analgesics such as opioids are associated with adverse effects that limit their use and threaten patient safety. Isovaline is a novel prototype analgesic that produces peripheral antinociception in several pain models with little or no effect on the central nervous system. The aim of this study was to establish a preliminary structure-activity relationship for isovaline derivatives by assaying efficacy in the formalin foot assay and central adverse effect profile in mice. Selected compounds were tested using the formalin foot assay to determine efficacy in reducing formalin-induced behaviors...
April 21, 2017: Amino Acids
https://www.readbyqxmd.com/read/28432317/psiguajadials-a-k-unusual-psidium-meroterpenoids-as-phosphodiesterase-4-inhibitors-from-the-leaves-of-psidium-guajava
#8
Gui-Hua Tang, Zhen Dong, Yan-Qiong Guo, Zhong-Bin Cheng, Chu-Jun Zhou, Sheng Yin
Bioassay-guided fractionation of the ethanolic extract of the leaves of Psidium guajava led to the isolation of 11 new Psidium meroterpenoids, psiguajadials A-K (1-11), along with 17 known ones (12-28). Their structures and absolute configurations were elucidated by spectroscopic methods and comparison of experimental and calculated ECD. Compounds 1 and 2 represent two unprecedented skeletons of 3,5-diformyl-benzyl phloroglucinol-coupled sesquiterpenoid, while 3 is the first example of Psidium meroterpenoids coupling via an oxepane ring...
April 21, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28432309/fano-resonance-with-high-local-field-enhancement-under-azimuthally-polarized-excitation
#9
Wuyun Shang, Fajun Xiao, Weiren Zhu, Hongsen He, Malin Premaratne, Ting Mei, Jianlin Zhao
Being an enabling technology for applications such as ultrasensitive biosensing and surface enhanced spectroscopy, enormous research interests have been focused on further boosting the local field enhancement at Fano resonance. Here, we demonstrate a plasmonic Fano resonance resulting from the interference between a narrow magnetic dipole mode and a broad electric dipole mode in a split-ring resonator (SRR) coupled to a nanoarc structure. Strikingly, when subjected to an azimuthally polarized beam (APB) excitation, the intensity enhancement becomes more than 60 times larger than that for a linearly polarized beam (LPB)...
April 21, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28432304/decreasing-temperature-enhances-the-formation-of-sixfold-hydrogen-bonded-rings-in-water-rich-water-methanol-mixtures
#10
Imre Bakó, László Pusztai, László Temleitner
The evolution of the structure of liquid water-methanol mixtures as a function of temperature has been studied by molecular dynamics simulations, with a focus on hydrogen bonding. The combination of the OPLS-AA (all atom) potential model of methanol and the widely used SPC/E water model has provided excellent agreement with measured X-ray diffraction data over the temperature range between 298 and 213 K, for mixtures with methanol molar fractions of 0.2, 0.3 and 0.4. Hydrogen bonds (HB-s) have been identified via a combined geometric/energetic, as well as via a purely geometric definition...
April 21, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28432121/the-lon-protease-like-domain-in-the-bacterial-reca-paralog-rada-is-required-for-dna-binding-and-repair
#11
Masao Inoue, Kenji Fukui, Yuki Fujii, Noriko Nakagawa, Takato Yano, Seiki Kuramitsu, Ryoji Masui
Homologous recombination (HR) plays an essential role in the maintenance of genome integrity. RecA/Rad51 paralogs have been recognized as an important factor of HR. Among them, only one bacterial RecA/Rad51 paralog - RadA - is involved in HR as an accessory factor of RecA recombinase. RadA has a unique Lon protease-like domain (LonC) at its C-terminus, in addition to a RecA-like ATPase domain. Unlike Lon protease, RadA's LonC domain does not show protease activity but is still essential for RadA-mediated DNA repair...
April 21, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/28431937/structural-modifications-in-the-sugar-moiety-as-a-key-to-improving-the-anticancer-effectiveness-of-doxorubicin
#12
REVIEW
Marta Denel-Bobrowska, Agnieszka Marczak
Doxorubicin (DOX) is one of the most commonly used and effective chemotherapeutic agents. Despite its clinical benefits, the use of DOX is often limited by serious adverse effects, such as severe cardiotoxicity and myelosuppression. Recent progress in chemical synthesis has enabled the design of modified anthracyclines with a sugar moiety being a desirable subject of research. A series of new analogues of DOX has been synthesised, in which the amino group in the daunosamine moiety was replaced by a formamidine system containing the rest of the cyclic secondary amine with gradually increased ring size...
April 18, 2017: Life Sciences
https://www.readbyqxmd.com/read/28431743/opportunistic-sampling-to-quantify-plastics-in-the-diet-of-unfledged-black-legged-kittiwakes-rissa-tridactyla-northern-fulmars-fulmarus-glacialis-and-great-cormorants-phalacrocorax-carbo
#13
Heidi Acampora, Stephen Newton, Ian O'Connor
Seabirds can interact with marine litter, mainly by entanglement or ingestion. The ingestion of plastics can lead to starvation or physical damage to the digestive tract. For chicks, it could additionally lead to reduced growth, affecting survival and fledging. This study quantified the ingestion of plastics by seabird chicks via an opportunistic sampling strategy. When ringing is carried out at colonies, birds may spontaneously regurgitate their stomach contents due to the stress or as a defence mechanism...
April 18, 2017: Marine Pollution Bulletin
https://www.readbyqxmd.com/read/28431477/duration-of-orthognathic-surgical-treatment
#14
Jaakko Paunonen, Mika Helminen, Timo Peltomäki
OBJECTIVE: The objective of this study was to determine the duration of orthognathic-surgical treatment conducted with conventional pre- and post-surgical orthodontic treatment phases. MATERIAL AND METHODS: The study material was comprised of the files of 185 consecutive patients treated in Oral and Maxillofacial Unit, Tampere University Hospital, Finland, in 2007-2014. The files were reviewed and the following data was obtained: gender and age of patients, ICD-10 diagnosis, type of malocclusion, duration of pre- and post-surgical orthodontic treatment and type of operation...
April 21, 2017: Acta Odontologica Scandinavica
https://www.readbyqxmd.com/read/28431352/degradation-of-sulfamethoxazole-by-uv-uv-h2o2-and-uv-persulfate-pds-formation-of-oxidation-products-and-effect-of-bicarbonate
#15
Yi Yang, Xinglin Lu, Jin Jiang, Jun Ma, Guanqi Liu, Ying Cao, Weili Liu, Juan Li, Suyan Pang, Xiujuan Kong, Congwei Luo
The frequent detection of sulfamethoxazole (SMX) in wastewater and surface waters gives rise of concerns about their ecotoxicological effects and potential risks to induce antibacterial resistant genes. UV/hydrogen peroxide (UV/H2O2) and UV/persulfate (UV/PDS) advanced oxidation processes have been demonstrated to be effective for the elimination of SMX, but there is still a need for a deeper understanding of product formations. In this study, we identified and compared the transformation products of SMX in UV, UV/H2O2 and UV/PDS processes...
March 28, 2017: Water Research
https://www.readbyqxmd.com/read/28431326/incidentally-detected-splenogonadal-fusion-in-a-laparoscopic-transabdominal-preperitoneal-hernia-repair-operation-a-case-report
#16
Yuichi Akama, Kimiyoshi Shimanuki, Shuji Asahi, Yohei Watanabe, Kazuhide Ko, Ryotaro Takano, Hodaka Amano, Takanori Kawaguchi, Eiji Uchida
INTRODUCTION: Splenogonadal fusion (SGF) is a rare congenital malformation in which the spleen is connected to the gonad. Few SGF cases have been reported in the English scientific literature, and we are unaware of any previous case reports of SGF with inguinal hernia by laparoscopic transabdominal preperitoneal hernia repair (TAPP). Here, we report a case of SGF that was incidentally detected during a TAPP procedure, with an uneventful postoperative course without complications. PRESENTATION OF CASE: A 76-year-old male presented with a 10-year history of left inguinal swelling...
April 5, 2017: International Journal of Surgery Case Reports
https://www.readbyqxmd.com/read/28431285/two-benzoyl-coumarin-amide-fluorescence-chemosensors-for-cyanide-anions
#17
Zian Wang, Qianqian Wu, Jiale Li, Shuang Qiu, Duxia Cao, Yongxiao Xu, Zhiqiang Liu, Xueying Yu, Yatong Sun
Two new benzoyl coumarin amide derivatives with ortho hydroxyl benzoyl as terminal group have been synthesized. Their photophysical properties and recognition properties for cyanide anions in acetonitrile have also been examined. The influence of electron donating diethylamino group in coumarin ring and hydroxyl in benzoyl group on recognition properties was explored. The results indicate that the compounds can recognize cyanide anions with obvious absorption and fluorescence spectral change and high sensitivity...
April 13, 2017: Spectrochimica Acta. Part A, Molecular and Biomolecular Spectroscopy
https://www.readbyqxmd.com/read/28431217/reduced-graphene-oxide-as-an-effective-adsorbent-for-removal-of-malachite-green-dye-plausible-adsorption-pathways
#18
Kanika Gupta, Om P Khatri
Efficient removal of malachite green (MG) dye from simulated wastewater is demonstrated using high surface area reduced graphene oxide (rGO). The plausible interaction pathways between MG dye and rGO are deduced from nanostructural features (HRTEM) of rGO and spectroscopic analyses (FTIR and Raman). The high surface area (931m(2)⋅gm(-1)) of rGO, π-π interaction between the aromatic rings of MG dye and graphitic skeleton, and electrostatic interaction of cationic centre of MG dye with π-electron clouds and negatively charged residual oxygen functionalities of rGO collectively facilitate the adsorption of MG dye on the rGO...
April 12, 2017: Journal of Colloid and Interface Science
https://www.readbyqxmd.com/read/28431136/c1-lateral-mass-displacement-and-transverse-atlantal-ligament-failure-in-jefferson-s-fracture-a-biomechanical-study-of-the-rule-of-spence
#19
Rafeek O Woods, Serkan Inceoglu, Yusuf T Akpolat, Wayne K Cheng, Brice Jabo, Olumide Danisa
BACKGROUND: Jefferson's fracture, first described in 1927, represents a bursting fracture of the C1 ring with lateral displacement of the lateral masses. It has been determined that if the total lateral mass displacement (LMD) exceeds 6.9 mm, there is high likelihood of transverse atlantal ligament (TAL) rupture, and if LMD is less than 5.7 mm TAL injury is unlikely. Several recent radiographic studies have questioned the accuracy and validity of the "rule of Spence" and it lacks biomechanical support...
April 20, 2017: Neurosurgery
https://www.readbyqxmd.com/read/28431053/occurrence-of-simultaneous-cathodal-anodal-capture-with-left-ventricular-quadripolar-leads-for-cardiac-resynchronization-therapy-an-electrocardiogram-evaluation
#20
Eraldo Occhetta, Gabriele Dell'Era, Ailia Giubertoni, Andrea Magnani, Francesco Rametta, Alessandro Blandino, Vincenzo Magnano, Maurizio Malacrida, Paolo Marino
Aims: The occurrence of left ventricular (LV) anodal activation during pacing with modern multipolar cardiac resynchronization therapy (CRT) systems has never been reported. The aim of our study was to demonstrate, by means of electrocardiogram (ECG) analysis, the occurrence of simultaneous cathodal-anodal LV capture with quadripolar LV leads. Methods and Results: We studied 10 first-time recipients of a CRT device equipped with a quadripolar LV lead. During follow-up, standard supine 12-lead ECGs were obtained in available cathode-to-anode LV pacing configurations with a pulse amplitude equal to twice the pacing threshold...
April 1, 2017: Europace: European Pacing, Arrhythmias, and Cardiac Electrophysiology
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