260,683 Works

Record of Leptometopa latipes (Diptera: Milichiidae) from a human cadaver in the Mediterranean area

Giorgia Giordani, Fabiola Tuccia, Silvia Zoppis, Carla Vecchiotti & Stefano Vanin
In forensic entomology, insects are used mainly to obtain information about the time since death. This information is obtained studying the developmental rate of the first colonizers, principally species in the families Calliphoridae, Sarcophagidae, Muscidae, Stratiomyidae and Phoridae. However, species belonging to other families can provide information about body transfer or the season of the death. Among them Milichiidae are flies rarely reported from human cases despite the larvae of some species are known as...

Backup Capacity Coordination with Renewable Energy Certificates in a Regional Electricity Market

Yingjue Zhou, Tieming Liu & Chaoyue Zhao
This paper studies a coordination mechanism between a renewable energy supplier and a conventional supplier in a regional electricity market. The intermittent nature of the renewable supplier results in random power shortage. Though the renewable supplier can buy backup power from a conventional supplier who prepares backup capacity to cover the shortage, there is no commitment that enough backup capacity will be prepared without any incentives to the conventional supplier. We design a coordination mechanism...

Backup capacity coordination with renewable energy certificates in a regional electricity market

Yingjue Zhou, Tieming Liu & Chaoyue Zhao
This article studies a coordination mechanism between a renewable energy supplier and a conventional supplier in a regional electricity market. The intermittent nature of the renewable supplier results in random power shortages. Though the renewable supplier can buy backup power from a conventional supplier who prepares backup capacity to cover the shortage, there is no commitment that enough backup capacity will be prepared without any incentives to the conventional supplier. We design a coordination mechanism...

Backup capacity coordination with renewable energy certificates in a regional electricity market

Yingjue Zhou, Tieming Liu & Chaoyue Zhao
This article studies a coordination mechanism between a renewable energy supplier and a conventional supplier in a regional electricity market. The intermittent nature of the renewable supplier results in random power shortages. Though the renewable supplier can buy backup power from a conventional supplier who prepares backup capacity to cover the shortage, there is no commitment that enough backup capacity will be prepared without any incentives to the conventional supplier. We design a coordination mechanism...

Self-reported occupational blood exposure among paramedics in Poland: a pilot study

Katarzyna Naylor, Anna Torres, Robert Gałązkowski & Kamil Torres
Introduction. Paramedics are at risk of occupational blood exposure, increased by the immediacy of provided treatment. However, the issue has not been acknowledged to date by any research in Europe. Methods. This research aimed at assessing occupational blood exposure among paramedics in Poland. Respondents represented 21 Polish medical institutions. Their participation was voluntary and anonymous. Paramedics were provided with a self-directed job-specific questionnaire adapted to Polish conditions from an original US version. Results. 118 paramedics...

Self-reported occupational blood exposure among paramedics in Poland: a pilot study

Katarzyna Naylor, Anna Torres, Robert Gałązkowski & Kamil Torres
Introduction. Paramedics are at risk of occupational blood exposure, increased by the immediacy of provided treatment. However, the issue has not been acknowledged to date by any research in Europe. Methods. This research aimed at assessing occupational blood exposure among paramedics in Poland. Respondents represented 21 Polish medical institutions. Their participation was voluntary and anonymous. Paramedics were provided with a self-directed job-specific questionnaire adapted to Polish conditions from an original US version. Results. 118 paramedics...

R code for: Secondhand horror: Effects of direct and indirect predator cues on behavior and reproduction of the bank vole

Thorbjörn Sievert, Marko Haapakoski, Rupert Palme, Helinä Voipio & Hannu Ylönen
R code for Sievert et al. 2019 (Secondhand horror: Effects of direct and indirect predator cues on behavior and reproduction of the bank vole)

Data for: Secondhand horror: Effects of direct and indirect predator cues on behavior and reproduction of the bank vole

Thorbjörn Sievert, Marko Haapakoski, Rupert Palme, Helinä Voipio & Hannu Ylönen
Data sets for Sievert et al. 2019 (Secondhand horror: Effects of direct and indirect predator cues on behavior and reproduction of the bank vole)

Enrichment planting to restore degraded tropical forest fragments in Brazil

Julia Raquel S. A. Mangueira, Karen D. Holl & Ricardo R. Rodrigues
In tropical areas with high levels of fragmentation due to agricultural use, forest fragments play an important role for biodiversity conservation at the landscape scale. But these fragments are subject to recurrent disturbances, which lead to arrested succession and loss of functional groups. In such cases, active restoration, such as enrichment planting, could facilitate recovery. We studied enrichment planting methods to restore tropical forest fragments in the Brazilian Atlantic Forest, and we evaluated the costs...

Enrichment planting to restore degraded tropical forest fragments in Brazil

Julia Raquel S. A. Mangueira, Karen D. Holl & Ricardo R. Rodrigues
In tropical areas with high levels of fragmentation due to agricultural use, forest fragments play an important role for biodiversity conservation at the landscape scale. But these fragments are subject to recurrent disturbances, which lead to arrested succession and loss of functional groups. In such cases, active restoration, such as enrichment planting, could facilitate recovery. We studied enrichment planting methods to restore tropical forest fragments in the Brazilian Atlantic Forest, and we evaluated the costs...

Design of selective COX-2 inhibitors in the (aza)indazole series. Chemistry, in vitro studies, radiochemistry and evaluations in rats of a [18F] PET tracer

Jonathan Elie, Johnny Vercouillie, Nicolas Arlicot, Lucas Lemaire, Rudy Bidault, Sylvie Bodard, Christel Hosselet, Jean-Bernard Deloye, Sylvie Chalon, Patrick Emond, Denis Guilloteau, Frédéric Buron & Sylvain Routier
A series of novel derivatives exhibiting high affinity and selectivity towards the COX-2 enzyme in the (aza) indazole series was developed. A short synthetic route involving a bromination/arylation sequence under microwave irradiation and direct C–H activation were established in the indazole and azaindazole series respectively. In vitro assays were conducted and structural modifications were carried out on these scaffolds to furnish compound 16 which exhibited effective COX-2 inhibitory activity, with IC50 values of 0.409 µM...

Design of selective COX-2 inhibitors in the (aza)indazole series. Chemistry, in vitro studies, radiochemistry and evaluations in rats of a [18F] PET tracer

Jonathan Elie, Johnny Vercouillie, Nicolas Arlicot, Lucas Lemaire, Rudy Bidault, Sylvie Bodard, Christel Hosselet, Jean-Bernard Deloye, Sylvie Chalon, Patrick Emond, Denis Guilloteau, Frédéric Buron & Sylvain Routier
A series of novel derivatives exhibiting high affinity and selectivity towards the COX-2 enzyme in the (aza) indazole series was developed. A short synthetic route involving a bromination/arylation sequence under microwave irradiation and direct C–H activation were established in the indazole and azaindazole series respectively. In vitro assays were conducted and structural modifications were carried out on these scaffolds to furnish compound 16 which exhibited effective COX-2 inhibitory activity, with IC50 values of 0.409 µM...

Design, synthesis, in vitro anticancer evaluation, kinase inhibitory effects, and pharmacokinetic profile of new 1,3,4-triarylpyrazole derivatives possessing terminal sulfonamide moiety

Mohammed S. Abdel-Maksoud, Mohammed I. El-Gamal, Mahmoud M. Gamal El-Din & Chang Hyun Oh
The present work describes the design and synthesis of a novel series of 1,3-diaryl-4-sulfonamidoarylpyrazole derivatives 1a–q and 2a–q and their in vitro biological activities. The target compounds were evaluated for antiproliferative activity against NCI-60 cell line panel. Compounds 1c, 1g, 1k–m, 1o, 2g, 2h, 2k–m, 2o, and 2q showed the highest mean inhibition percentages at 10 µM single-dose testing and were selected to be tested at 5-dose mode. The ICs50 of the most potent compounds...

Computer-aided molecular design of pyrazolotriazines targeting glycogen synthase kinase 3

M. Lourdes Sciú, Victor Sebastián-Pérez, Loreto Martinez-Gonzalez, Rocio Benitez, Daniel I. Perez, Concepción Pérez, Nuria E. Campillo, Ana Martinez & E. Laura Moyano
Numerous studies have highlighted the implications of the glycogen synthase kinase 3 (GSK-3) in several processes associated with Alzheimer’s disease (AD). Therefore, GSK-3 has become a crucial therapeutic target for the treatment of this neurodegenerative disorder. Hereby, we report the design and multistep synthesis of ethyl 4-oxo-pyrazolo[4,3-d][1–3]triazine-7-carboxylates and their biological evaluation as GSK-3 inhibitors. Molecular modelling studies allow us to develop this new scaffold optimising the chemical structure. Potential binding mode determination in the enzyme...

Computer-aided molecular design of pyrazolotriazines targeting glycogen synthase kinase 3

M. Lourdes Sciú, Victor Sebastián-Pérez, Loreto Martinez-Gonzalez, Rocio Benitez, Daniel I. Perez, Concepción Pérez, Nuria E. Campillo, Ana Martinez & E. Laura Moyano
Numerous studies have highlighted the implications of the glycogen synthase kinase 3 (GSK-3) in several processes associated with Alzheimer’s disease (AD). Therefore, GSK-3 has become a crucial therapeutic target for the treatment of this neurodegenerative disorder. Hereby, we report the design and multistep synthesis of ethyl 4-oxo-pyrazolo[4,3-d][1–3]triazine-7-carboxylates and their biological evaluation as GSK-3 inhibitors. Molecular modelling studies allow us to develop this new scaffold optimising the chemical structure. Potential binding mode determination in the enzyme...

Design, synthesis, in vitro anticancer evaluation, kinase inhibitory effects, and pharmacokinetic profile of new 1,3,4-triarylpyrazole derivatives possessing terminal sulfonamide moiety

Mohammed S. Abdel-Maksoud, Mohammed I. El-Gamal, Mahmoud M. Gamal El-Din & Chang Hyun Oh
The present work describes the design and synthesis of a novel series of 1,3-diaryl-4-sulfonamidoarylpyrazole derivatives 1a–q and 2a–q and their in vitro biological activities. The target compounds were evaluated for antiproliferative activity against NCI-60 cell line panel. Compounds 1c, 1g, 1k–m, 1o, 2g, 2h, 2k–m, 2o, and 2q showed the highest mean inhibition percentages at 10 µM single-dose testing and were selected to be tested at 5-dose mode. The ICs50 of the most potent compounds...

iVS analysis to evaluate the impact of scaffold diversity in the binding to cellular targets relevant in cancer

Agostino Cilibrizzi, Giuseppe Floresta, Vincenzo Abbate & Maria Paola Giovannoni
This study reports the application of inverse virtual screening (iVS) methodologies to identify cellular proteins as suitable targets for a library of heterocyclic small-molecules, with potential pharmacological implications. Standard synthetic procedures allow facile generation of these ligands showing a high degree of core scaffold diversity. Specifically, we have computationally investigated the binding efficacy of the new series for target proteins which are involved in cancer pathogenesis. As a result, nine macromolecules demonstrated efficient binding interactions...

iVS analysis to evaluate the impact of scaffold diversity in the binding to cellular targets relevant in cancer

Agostino Cilibrizzi, Giuseppe Floresta, Vincenzo Abbate & Maria Paola Giovannoni
This study reports the application of inverse virtual screening (iVS) methodologies to identify cellular proteins as suitable targets for a library of heterocyclic small-molecules, with potential pharmacological implications. Standard synthetic procedures allow facile generation of these ligands showing a high degree of core scaffold diversity. Specifically, we have computationally investigated the binding efficacy of the new series for target proteins which are involved in cancer pathogenesis. As a result, nine macromolecules demonstrated efficient binding interactions...

Design, synthesis and biological evaluation of novel 4-anlinoquinazoline derivatives as EGFR inhibitors with the potential to inhibit the gefitinib-resistant nonsmall cell lung cancers

Caolin Wang, Shan Xu, Liang Peng, Bingliang Zhang, Hong Zhang, Yingying Hu, Pengwu Zheng & Wufu Zhu
A series of quinazoline derivatives with benzylidene hydrazine carboxamide were designed and synthesised as EGFR inhibitors. Most compounds exhibited exceptional anti-proliferative activity against A549, HepG2, MCF-7 and H1975 cells. Furthermore, six compounds demonstrated excellent inhibition activity against EGFRWT with the IC50 value both less than 2 nM. Among the six compounds, 44 exhibited the strongest activity (0.4 nM) and potently inhibited EGFRL858R/T790M (0.1 μM). Excitingly, the most potent compound 14 showed excellent enzyme inhibitory activity...

Synthesis and biological evaluation of 3-arylcoumarin derivatives as potential anti-diabetic agents

Yuheng Hu, Bing Wang, Jie Yang, Teng Liu, Jie Sun & Xiaojing Wang
A variety of substituted 3-arylcoumarin derivatives were synthesised through microwave radiation heating. The method has characteristics of environmental friendliness, economy, simple separation, and purification process, less by-products and high reaction yield. Those 3-arylcoumarin derivatives were screened for antioxidant, α-glucosidase inhibitory and advanced glycation end-products (AGEs) formation inhibitory. Most compounds exhibited significant antioxidant and AGEs formation inhibitory activities. Anti-diabetic activity studies showed that compounds 11 and 17 were equipotent to the standard drug glibenclamide in vivo....

Synthesis and biological evaluation of 3-arylcoumarin derivatives as potential anti-diabetic agents

Yuheng Hu, Bing Wang, Jie Yang, Teng Liu, Jie Sun & Xiaojing Wang
A variety of substituted 3-arylcoumarin derivatives were synthesised through microwave radiation heating. The method has characteristics of environmental friendliness, economy, simple separation, and purification process, less by-products and high reaction yield. Those 3-arylcoumarin derivatives were screened for antioxidant, α-glucosidase inhibitory and advanced glycation end-products (AGEs) formation inhibitory. Most compounds exhibited significant antioxidant and AGEs formation inhibitory activities. Anti-diabetic activity studies showed that compounds 11 and 17 were equipotent to the standard drug glibenclamide in vivo....

Design, synthesis and biological evaluation of novel 4-anlinoquinazoline derivatives as EGFR inhibitors with the potential to inhibit the gefitinib-resistant nonsmall cell lung cancers

Caolin Wang, Shan Xu, Liang Peng, Bingliang Zhang, Hong Zhang, Yingying Hu, Pengwu Zheng & Wufu Zhu
A series of quinazoline derivatives with benzylidene hydrazine carboxamide were designed and synthesised as EGFR inhibitors. Most compounds exhibited exceptional anti-proliferative activity against A549, HepG2, MCF-7 and H1975 cells. Furthermore, six compounds demonstrated excellent inhibition activity against EGFRWT with the IC50 value both less than 2 nM. Among the six compounds, 44 exhibited the strongest activity (0.4 nM) and potently inhibited EGFRL858R/T790M (0.1 μM). Excitingly, the most potent compound 14 showed excellent enzyme inhibitory activity...

Phosphonate inhibitors of West Nile virus NS2B/NS3 protease

Marcin Skoreński, Aleksandra Milewska, Krzysztof Pyrć, Marcin Sieńczyk & Józef Oleksyszyn
West Nile virus (WNV) is a member of the flavivirus genus belonging to the Flaviviridae family. The viral serine protease NS2B/NS3 has been considered an attractive target for the development of anti-WNV agents. Although several NS2B/NS3 protease inhibitors have been described so far, most of them are reversible inhibitors. Herein, we present a series of α-aminoalkylphosphonate diphenyl esters and their peptidyl derivatives as potent inhibitors of the NS2B/NS3 protease. The most potent inhibitor identified was...

Synthesis and biological assessment of KojoTacrines as new agents for Alzheimer’s disease therapy

Youssef Dgachi, Hélène Martin, Rim Malek, Daniel Jun, Jana Janockova, Vendula Sepsova, Ondrej Soukup, Isabel Iriepa, Ignacio Moraleda, Emna Maalej, M. Carmo Carreiras, Bernard Refouvelet, Fakher Chabchoub, José Marco-Contelles & Lhassane Ismaili
In view of the multifactorial nature of Alzheimer’s disease (AD), multitarget small molecules (MTSM) represent the most potent and attractive therapeutic strategy to design new drugs for Alzheimer’s disease therapy. The new MTSM KojoTacrines (KTs) were designed and synthesized by juxtaposition of selected pharmacophoric motifs from kojic acid and tacrine. Among them, 11-amino-2-(hydroxymethyl)-12-(3-methoxyphenyl)-7,9,10,12-tetrahydropyrano [2',3':5,6] pyrano[2,3-b]quinolin-4(8H)-one (KT2d) was identified as less-hepatotoxic than tacrine, at higher concentration, a moderate, but selective human acetylcholinesterase inhibitor (IC50 = 4.52...

Synthesis and biological assessment of KojoTacrines as new agents for Alzheimer’s disease therapy

Youssef Dgachi, Hélène Martin, Rim Malek, Daniel Jun, Jana Janockova, Vendula Sepsova, Ondrej Soukup, Isabel Iriepa, Ignacio Moraleda, Emna Maalej, M. Carmo Carreiras, Bernard Refouvelet, Fakher Chabchoub, José Marco-Contelles & Lhassane Ismaili
In view of the multifactorial nature of Alzheimer’s disease (AD), multitarget small molecules (MTSM) represent the most potent and attractive therapeutic strategy to design new drugs for Alzheimer’s disease therapy. The new MTSM KojoTacrines (KTs) were designed and synthesized by juxtaposition of selected pharmacophoric motifs from kojic acid and tacrine. Among them, 11-amino-2-(hydroxymethyl)-12-(3-methoxyphenyl)-7,9,10,12-tetrahydropyrano [2',3':5,6] pyrano[2,3-b]quinolin-4(8H)-one (KT2d) was identified as less-hepatotoxic than tacrine, at higher concentration, a moderate, but selective human acetylcholinesterase inhibitor (IC50 = 4.52...

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