6-Nitro-2,3-dihydro-1H-pyrrolo­[2,1-c][1,4]benzodiazepine-5,11(10H,11aH)-dione

In the two mol­ecules of the asymmetric unit of the title compound, C12H11N3O4, the seven-membered diazepine ring adopts a boat conformation (with the two phenyl­ene C atoms representing the stern and the methine C atom the prow). The five-membered pyrrole ring, which has an envelope conformation, makes dihedral angles of 60.47 (10) and 54.69 (9)° with the benzene ring of the benzodiazepine unit in the two mol­ecules. In the crystal, inter­molecular N—H⋯O hydrogen bonds and π–π stacking inter­actions [centroid–centroid distance = 3.8023 (7)–3.8946 (7) Å] lead to the formation of a three-dimensional framework

2-Methyl-3-(n-octylsulfan­yl)quinoxaline

All the non-H atoms of the title compound, C17H24N2S, lie almost in a common plane (r.m.s. deviation = 0.049 Å). The octyl chain adopts an all-trans conformation

1-Benzyl-3-methyl­quinoxalin-2(1H)-one

The asymmetric unit of the title compound, C16H14N2O, contains three independent mol­ecules. The dihedral angles between the quinoxaline and phenyl planes in the three mol­ecules are 82.58 (8), 85.66 (9) and 85.36 (9)°. The crystal packing is stabilized by C—H⋯O and C—H⋯N hydrogen bonds

rac-(3S,4S)-3-Hy­droxy-4-phenyl-1-[(S)-(3-phenyl-4,5-dihydro-1,2-oxazol-5-yl)meth­yl]-4,5-dihydro-1H-1,5-benzo­diazepin-2(3H)-one

In the title compound, C25H23N3O3, the seven-membered diazepine ring adopts a boat conformation with the hydroxy-substituted C atom at the prow and fused-ring C atoms at the stern. The crystal packing features C—H⋯O, C—H⋯π and N—H ⋯π inter­action

Advances in tetrahydropyrido[1,2-a]isoindolone (valmerins) series: Potent glycogen synthase kinase 3 and cyclin dependent kinase 5 inhibitors.

International audienceAn efficient synthetic strategy was developed to modulate the structure of the tetrahydropyridine isoindolone (Valmerin) skeleton. A library of more than 30 novel final structures was generated. Biological activities on CDK5 and GSK3 as well as cellular effects on cancer cell lines were measured for each novel compound. Additionally docking studies were performed to support medicinal chemistry efforts. A strong GSK3/CDK5 dual inhibitor (38, IC50 GSK3/CDK5 32/84 nM) was obtained. A set of highly selective GSK3 inhibitors was synthesized by fine-tuning structural modifications (29 IC50 GSK3/CDK5 32/320 nM). Antiproliferative effects on cells were correlated with the in vitro kinase activities and the best effects were obtained with lung and colon cell lines

SMOS based high resolution soil moisture estimates for Desert locust preventive management

This paper presents the first attempt to include soil moisture information from remote sensing in the tools available to desert locust managers. The soil moisture requirements were first assessed with the users. The main objectives of this paper are: i) to describe and validate the algorithms used to produce a soil moisture dataset at 1 km resolution relevant to desert locust management based on DisPATCh methodology applied to SMOS and ii) the development of an innovative approach to derive high-resolution (100 m) soil moisture products from Sentinel-1 in synergy with SMOS data. For the purpose of soil moisture validation, 4 soil moisture stations where installed in desert areas (one in each user country). The soil moisture 1 km product was thoroughly validated and its accuracy is amongst the best available soil moisture products. Current comparison with in-situ soil moisture stations shows good values of correlation (R>0.7R>0.7) and low RMSE (below 0.04 m3 m−3). The low number of acquisitions on wet dates has limited the development of the soil moisture 100 m product over the Users Areas. The Soil Moisture product at 1 km will be integrated into the national and global Desert Locust early warning systems in national locust centres and at DLIS-FAO, respectively

Utilisation d’un lit fixe d’origine naturelle pour le traitement biologique d'effluents laitiers

The use of oyster shells as a naturally applied as the media in biomass-fixed biological reactors has been studied in the presence of Aspergillus niger and Penicillium chrysogenum fungi for the treatment of dairy effluents. The objective is to compare the purification performance between several biofilms biological treatments, different by the use of colonization supports and also by their design. The common Kadnes commercial media (Kaldnes K3) was thus studied in the case of biological treatment of the same effluent, and the abatement performances of the organic pollution in both cases were compared. The results show comparable performance after 24 hours of treatment. These yields were better compared to the biological treatment that does not use media of colonization.L’utilisation de coquilles d’huîtres comme support, d’origine naturelle, dans les réacteurs biologiques à biomasse fixe a été étudiée en présence de champignons Aspergillus niger et Penicillium chrysogenum pour le traitement des effluents de laiteries. L’objectif étant de comparer les performances d’épuration entre plusieurs traitements biologiques à biofilms, différents par l’utilisation de supports de colonisation et aussi par leurs conceptions. Le support commercial commun Kadnes (Kaldnes K3) a été ainsi étudié dans le cas de traitements biologiques du même effluent, et les performances d’abattement de la pollution organique dans les deux cas ont été comparées. Les résultats révèlent des performances comparables après 24 heures de traitement. Ces rendements étaient meilleurs comparés au traitement biologique qui n’utilise pas de supports