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2.
Pharmaceuticals (Basel) ; 15(10)2022 Oct 11.
Artigo em Inglês | MEDLINE | ID: mdl-36297362

RESUMO

Chalcones are a class of privileged scaffolds with high medicinal significance due to the presence of an α,ß-unsaturated ketone functionality. Numerous functional modifications of chalcones have been reported, along with their pharmacological behavior. The present review aims to summarize the structures from natural sources, synthesis methods, biological characteristics against infectious and non-infectious diseases, and uses of chalcones over the past decade, and their structure-activity relationship studies are detailed in depth. This critical review provides guidelines for the future design and synthesis of various chalcones. In addition, this could be highly supportive for medicinal chemists to develop more promising candidates for various infectious and non-infectious diseases.

3.
Artigo em Inglês | MEDLINE | ID: mdl-32755815

RESUMO

The Household Air Pollution Intervention Network (HAPIN) trial is evaluating health benefits of a liquefied petroleum gas (LPG) stove intervention in biomass cook-fuel using homes (n = 3200) in four low-and middle-income countries (LMICs) that include Peru, Guatemala, Rwanda and India. Longitudinal urine samples (n = 6000) collected from enrolled pregnant women, infants and older women will be analyzed for biomarkers associated with exposure and health outcomes. We report results from cross-validation of a lower cost high-performance liquid chromatography with fluorescence detection (HPLC-FLD) method with a higher resolution liquid chromatography-tandem mass spectrometry (LC-MS/MS) method for the measurement of 1-hydroxypyrene (1PYR) and 2-naphthol (2NAP). Twenty-five split urine samples were analyzed by HPLC-FLD method at the India trial site in Chennai, India and by LC-MSMS method at the trial wide Biomarker Coordinating Center, Emory University, USA. The limits of detection (LOD) for the HPLC-FLD method were 0.02 ng/mL and 0.07 ng/mL for 2NAP and 1PYR, respectively. Bland-Altman analysis estimated a bias of 2.98 ng/ml for 2NAP (95% CI: -5.22, -0.75) and 0.09 ng/mL for 1PYR (95% CI: -0.02, 0.21) with HPLC-FLD levels being lower than LC-MSMS levels at higher concentrations. Analyses of additional urine samples (n = 119) collected during the formative phase of the HAPIN trial in India, showed 2NAP and 1PYR levels to be consistently above the limit of quantification (LOQ) and demonstrated the applicability of the method. The HPLC-FLD method can serve as a cost-effective and reliable analytical method to measure 2NAP and 1PYR in human urine in LMICs, within and beyond the HAPIN trial.


Assuntos
Poluentes Atmosféricos/urina , Monitoramento Biológico/métodos , Exposição Ambiental/análise , Hidrocarbonetos Policíclicos Aromáticos/urina , Adulto , Poluentes Atmosféricos/metabolismo , Cromatografia Líquida de Alta Pressão , Culinária , Feminino , Humanos , Índia , Lactente , Recém-Nascido , Limite de Detecção , Modelos Lineares , Hidrocarbonetos Policíclicos Aromáticos/metabolismo , Gravidez , Reprodutibilidade dos Testes , Espectrometria de Massas em Tandem
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