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1.
PAPER CURRENT
Anti-leishmanial and cytotoxic activities of amino acid-triazole hybrids: Synthesis, biological evaluation, molecular docking and in silico physico-chemical properties (2017)
Elsevier
Publication Date: 2017-03-23
Description: Publication date: Available online 22 March 2017 Source: Bioorganic & Medicinal Chemistry Letters Author(s): Mir Mohammad Masood, Phool Hasan, Shams Tabrez, Md. Bilal Ahmad, Umesh Yadava, Constantin G. Daniliuc, Yogesh A. Sonawane, Amir Azam, Abdur Rub, Mohammad Abid According to WHO, leishmaniasis is a major tropical disease, ranking second after malaria. Significant efforts have been therefore invested into finding potent inhibitors for the treatment. In this work, eighteen novel 1,2,3-triazoles appended with L -amino acid (Phe/Pro/Trp) tail were synthesized via azide-alkyne click chemistry with moderate to good yield, and evaluated for their anti-leishmanial activity against promastigote form of Leishmania donovani (Dd8 strain). Among all, compounds 40 , 43, and 53 were identified with promising anti-leishmanial activity with IC 50 = 88.83 ± 2.93, 96.88 ± 12.88 and 94.45 ± 6.51 μM respectively and displayed no cytotoxicity towards macrophage cells. Moreover, compound 43 showed highest selectivity index (SI = 8.05) among all the tested compounds. Supported by docking studies, the lead inhibitors ( 40 , 43 and 53 ) showed interactions with key residues in the catalytic site of trypanothione reductase. The results of pharmacokinetic parameters suggest that these selected inhibitors can be carried forward for further structural optimization and pharmacological investigation. Graphical abstract
Print ISSN: 0960-894X
Electronic ISSN: 1464-3405
Topics: Chemistry and Pharmacology , Medicine
Published by Elsevier
2.
PAPER CURRENT
Synthesis and biological evaluation of novel selective androgen receptor modulators (SARMs). Part II: Optimization of 4-(pyrrolidin-1-yl)benzonitrile derivatives (2017)
Elsevier
Publication Date: 2017-03-23
Description: Publication date: Available online 21 March 2017 Source: Bioorganic & Medicinal Chemistry Letters Author(s): Moriteru Asano, Takenori Hitaka, Takashi Imada, Masami Yamada, Megumi Morimoto, Hiromi Shinohara, Takahito Hara, Masuo Yamaoka, Takashi Santou, Masaharu Nakayama, Yumi Imai, Noriyuki Habuka, Jason Yano, Keith Wilson, Hisashi Fujita, Atsushi Hasuoka We recently reported a class of novel tissue-selective androgen receptor modulators (SARMs), represented by a naphthalene derivative A . However, their pharmacokinetic (PK) profiles were poor due to low metabolic stability. To improve the PK profiles, we modified the hydroxypyrrolidine and benzonitrile substituents of 4-(pyrrolidin-1-yl)benzonitrile derivative B , which had a comparable potency as that of compound A . This optimization led us to further modifications, which improved metabolic stability while maintaining potent androgen agonistic activity. Among the synthesized compounds, (2 S ,3 S )-2,3-dimethyl-3-hydroxylpyrrolidine derivative 1c exhibited a suitable PK profile and improved metabolic stability. Compound 1c demonstrated significant efficacy in levator ani muscle without increasing the weight of the prostate in an in vivo study. In addition, compound 1c showed agonistic activity in the CNS, which was detected using sexual behavior induction assay. Graphical abstract
Print ISSN: 0960-894X
Electronic ISSN: 1464-3405
Topics: Chemistry and Pharmacology , Medicine
Published by Elsevier
3.
PAPER CURRENT
Transcriptome analysis of pancreatic cells across distant species highlights novel important regulator genes (2017)
BioMed Central
Publication Date: 2017-03-23
Description: Defining the transcriptome and the genetic pathways of pancreatic cells is of great interest for elucidating the molecular attributes of pancreas disorders such as diabetes and cancer. As the function of the d...
Electronic ISSN: 1741-7007
Topics: Biology
Published by BioMed Central
4.
PAPER CURRENT
Corrigendum to “Synthesis and biological activity of 2,5-diaryl-3-methylpyrimido[4,5-c]quinolin-1(2H)-one derivatives” [Bioorg. Med. Chem. 15 (2007) 2434–2440] (2017)
Elsevier
Publication Date: 2017-03-23
Description: Publication date: Available online 22 March 2017 Source: Bioorganic & Medicinal Chemistry Author(s): Kamel Metwally, Omar Aly, Enayat Aly, Abhijit Banerjee, Rudravajhala Ravindra, Susan Bane
Print ISSN: 0968-0896
Electronic ISSN: 1464-3391
Topics: Chemistry and Pharmacology , Medicine
Published by Elsevier
5.
PAPER CURRENT
Genome-wide expression profiling in leaves and roots of date palm (Phoenix dactylifera L.) exposed to salinity (2017)
BioMed Central
Publication Date: 2017-03-23
Description: Date palm, as one of the most important fruit crops in North African and West Asian countries including Oman, is facing serious growth problems due to salinity, arising from persistent use of saline water for ...
Electronic ISSN: 1471-2164
Topics: Biology
Published by BioMed Central
6.
PAPER CURRENT
Optical and molecular-level characterization of fluvial organic matter biodegradation in a highly urbanized river system (2017)
Copernicus
Publication Date: 2017-03-23
Description: Optical and molecular-level characterization of fluvial organic matter biodegradation in a highly urbanized river system Most Shirina Begum, Hyojin Jin, Inae Jang, Jung-Min Lee, Han Bin Oh, and Ji-Hyung Park Biogeosciences Discuss., doi:10.5194/bg-2017-93,2017 Manuscript under review for BG (discussion: open, 0 comments) A basin-scale field survey was combined with two laboratory incubation experiments to explore human impacts on organic matter biodegradation and CO 2 emission in a highly urbanized river system in South Korea. The results suggest that river impoundment and pollution can alter the optical properties and biodegradability of both dissolved and particulate organic matter in the modified river system to such a degree that can induce a priming effect on biodegradation and CO 2 emission.
Print ISSN: 1810-6277
Electronic ISSN: 1810-6285
Topics: Biology , Geosciences
7.
PAPER CURRENT
Local Magnitude Discrepancies for Near-Event Receivers: Implications for the U.K. Traffic-Light Scheme (2017)
Seismological Society of America (SSA)
Publication Date: 2017-03-23
Description: Local seismic magnitudes provide a practical and efficient scale for the implementation of regulation designed to manage the risk of induced seismicity, such as Traffic-Light Schemes (TLS). We demonstrate that significant magnitude discrepancies (up to a unit higher) occur between seismic events recorded on nearby stations (<5 km) compared with those at greater distances. This is due to the influence of sedimentary layers, which are generally lower in velocity and more attenuating than the underlying crystalline basement rocks, and requires a change in the attenuation term of the M L scale. This has a significant impact on the United Kingdom’s (U.K.) hydraulic fracturing TLS, whose red light is set at M L  0.5. Because the nominal detectability of the U.K. network is M L  2, this scheme will require the deployment of monitoring stations in close proximity to well sites. Using data collected from mining events near New Ollerton, Nottinghamshire, we illustrate the effects that proximity has on travel path velocities and attenuation, then perform a damped least-squares inversion to determine appropriate constants within the M L scale. We show that the attenuation term needs to increase from 0.00183 to 0.0514 and demonstrate that this higher value is representative of a ray path within a slower more attenuating sedimentary layer compared with the continental crust. We therefore recommend that the magnitude scale M L =log( A )+1.17log( r )+0.0514 r –3.0 should be used when local monitoring networks are within 5 km of the event epicenters.
Print ISSN: 0037-1106
Electronic ISSN: 1943-3573
Topics: Geosciences , Physics
8.
PAPER CURRENT
Apparent Late Quaternary Fault-Slip Rate Increase in the Southern Lower Rhine Graben, Central Europe (2017)
Seismological Society of America (SSA)
Publication Date: 2017-03-23
Description: In regions of low strain, long earthquake recurrence intervals (10 4 –10 6 yrs) and erosive processes limit preservation of Quaternary markers suitable for distinguishing whether faults slip at uniform or secularly varying rates. The Lower Rhine graben in the border region of Germany, The Netherlands, and Belgium provides a unique opportunity to explore Quaternary slip-rate variations in a region of low strain using the basal (2.29±0.29 Ma) and surface (700±80 ka) contacts of the regionally extensive main terrace ("Hauptterrasse"), deposited by the Rhine and Maas Rivers. These surfaces are vertically offset 3–140 m and 0–68 m, respectively, across individual fault strands within a distributed network of northwest-trending, slow-slipping (<0.1 mm/yr) normal faults. In this investigation, we construct Quaternary slip histories for the southern Lower Rhine graben faults using new main terrace surface vertical offset measurements made from light detection and ranging (lidar)-derived bare-earth digital terrain models, which we synthesize with existing constraints on the offset basal contact of this fluvial deposit ( n =91 collocated sites with displacement constraints). We find that >80% of the sites record an apparent increase in slip rate for the more recent interval from 700 ka to present, which corresponds to a period of increased uplift of the nearby Rhenish Massif and regional volcanism. However, the apparent increase in slip rate could result, in part, from erosion of the footwall surface below the main terrace, leading to an apparent displacement that is smaller than the total vertical offset since the start of the Quaternary. Prior work focused on characterization of these faults as seismic sources in the Lower Rhine graben has preferentially relied on the average fault-slip rate constrained using the base of the main terrace. We suggest that average fault-slip rates calculated using the ~700 ka main terrace surface are subjected to fewer uncertainties and sample a time interval that is more relevant for seismic-hazard analysis. Electronic Supplement: Table of main terrace surface and basal contact offset measurements, figure describing an unrealistic faulting scenario, and a KML file with the fault-trace mapping spanning the Lower Rhine graben.
Print ISSN: 0037-1106
Electronic ISSN: 1943-3573
Topics: Geosciences , Physics
9.
PAPER CURRENT
Properties of Noise Cross-Correlation Functions Obtained from a Distributed Acoustic Sensing Array at Garner Valley, California (2017)
Seismological Society of America (SSA)
Publication Date: 2017-03-23
Description: A field test that was conducted at Garner Valley, California, on 11 and 12 September 2013 using distributed acoustic sensing (DAS) to sense ground vibrations provided a continuous overnight record of ambient noise. The energy of ambient noise was concentrated between 5 and 25 Hz, which falls into the typical traffic noise frequency band. A standard procedure ( Bensen et al. , 2007 ) was adopted to calculate noise cross-correlation functions (NCFs) for 1-min intervals. The 1-min-long NCFs were stacked using the time–frequency domain phase-weighted-stacking method, which significantly improves signal quality. The obtained NCFs were asymmetrical, which was a result of the nonuniform distributed noise sources. A precursor appeared on NCFs along one segment, which was traced to a strong localized noise source or a scatterer at a nearby road intersection. NCF for the radial component of two surface accelerometers along a DAS profile gave similar results to those from DAS channels. We calculated the phase velocity dispersion from DAS NCFs using the multichannel analysis of surface waves technique, and the result agrees with active-source results. We conclude that ambient noise sources and the high spatial sampling of DAS can provide the same subsurface information as traditional active-source methods.
Print ISSN: 0037-1106
Electronic ISSN: 1943-3573
Topics: Geosciences , Physics
10.
PAPER CURRENT
Stable and Transportable Seismic Yield Estimation from Local Full-Envelope Template Matching (2017)
Seismological Society of America (SSA)
Publication Date: 2017-03-23
Description: We developed a multifrequency, full-envelope template approach to estimate surface explosion yield from seismic stations in the 5–50 km distance range. The new method is empirically based, transportable, and unlike other methods, it is designed to work for short-duration coda that a simple exponential single-scattering formulation in a homogeneous space does not model well. Our empirical full-envelope template-matching approach produces close fits to complicated short-duration and high-frequency waveforms observed at near-field distances. Moreover, because the envelope templates capture the nuances of the initial P and S waves and their scattered counterparts, the method is robust and provides roughly a factor of three times less scatter in yield measurement than peak P -wave and integrated first P -wave estimates. In this article, we demonstrate that our improved empirical template matching achieves accurate explosive yield estimates that are within 50% of the design yields at 95% confidence for a set of chemical explosions ranging in yield from 50 kg to 45 tonnes.
Print ISSN: 0037-1106
Electronic ISSN: 1943-3573
Topics: Geosciences , Physics