79 research outputs found
Identifying new isatin derivatives with GSK-3 inhibition capacity through molecular docking and bioassays
The semi-synthesis of 11 isatin derivatives was achieved through bimolecular nucleophilic substitution and click chemistry. Seven new compounds were obtained. All chemical structures were determined by infrared spectroscopy (IR), nuclear magnetic resonance spectrometry (NMR) and high-resolution mass spectrometry (HRMS) data. These derivatives were evaluated for their anti-GSK-3 activity and all isatin derivatives (N-alkyl and 1,2,3-triazolic) exhibited strong inhibitory activity, with 2b and 4h exhibiting remarkable potency. In addition, docking studies were performed with 2b and 2e models to unravel the molecular mechanism underlying the polar interactions on the GSK-3 ATP-binding site.This study was funded by the Coordenação de Aperfeiçoamento de Pessoal de Nível Superior, Brasil
(CAPES), Finance Code 001, by the National Council of Scientific and Technological Development (CNPq)
and Foundation of Support to Research and Innovation of Espírito Santo (FAPES PPE-Agro No. 76418880/16). We also would like to acknowledge INCTBioNat (CNPq 465637/2014-0) for additional support and NCQP-UFES, as well as the Portuguese Foundation for Science and Technology (FCT) under the scope of the strategic funding of UID/BIO/04469/2019 unit and BioTecNorte operation (NORTE-01-0145-FEDER-000004) funded
by the European Regional Development Fund under the
scope of Norte2020, Programa Operacional Regional
do Norte. L. R. R. also acknowledges her sabbatical
leave fellowship (SFRH/BSAB/142991/2018) funded
by FCT. D. F. is recipient of a doctoral fellowship (call
NORTE-69-2015-15) funded by the European Social Fund
under the scope of Norte2020, Programa Operacional
Regional do Norte.info:eu-repo/semantics/publishedVersio
Management of MDR-TB in HIV co-infected patients in Eastern Europe: Results from the TB:HIV study
Objectives Mortality among HIV patients with tuberculosis (TB) remains high in Eastern Europe (EE), but details of TB and HIV management remain scarce. Methods In this prospective study, we describe the TB treatment regimens of patients with multi-drug resistant (MDR) TB and use of antiretroviral therapy (ART). Results A total of 105 HIV-positive patients had MDR-TB (including 33 with extensive drug resistance) and 130 pan-susceptible TB. Adequate initial TB treatment was provided for 8% of patients with MDR-TB compared with 80% of those with pan-susceptible TB. By twelve months, an estimated 57.3% (95%CI 41.5\u201374.1) of MDR-TB patients had started adequate treatment. While 67% received ART, HIV-RNA suppression was demonstrated in only 23%. Conclusions Our results show that internationally recommended MDR-TB treatment regimens were infrequently used and that ART use and viral suppression was well below the target of 90%, reflecting the challenging patient population and the environment in which health care is provided. Urgent improvement of management of patients with TB/HIV in EE, in particular for those with MDR-TB, is needed and includes widespread access to rapid TB diagnostics, better access to and use of second-line TB drugs, timely ART initiation with viral load monitoring, and integration of TB/HIV care
Nonlinear characteristics of blood oxygen saturation from nocturnal oximetry for obstructive sleep apnoea detection
Nutritional evaluation of elephant-grass silages with different levels of by-products from the cashew juice industry
Exposição a radiações eletromagnéticas não ionizantes da telefonia celular e sintomas psiquiátricos
Floristic composition and structure of an upper montane cloud forest in the Serra da Mantiqueira Mountain Range of Brazil
Ethylene evolution and endo-beta-mannanase activity during lettuce seed germination at high temperature
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