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1.
Chem Biodivers ; 20(12): e202301271, 2023 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-37806964

RESUMO

According to the fusion technique create effective multi-target-directed ligands, in this study, we designed and synthesized a series of benzo[d]thiazol-2-yl)-3-(pyrrolidin-1-yl) or 3-(morph- olino-1-yl)propanamide derivatives, and evaluated their inhibitory potency against MAOs, AChE, BuChE by in vitro enzyme effect assays. Based on activity results, we found that derivatives N-(5-methylbenzo[d]thiazol-2-yl)-3-(pyrrolidin-1-yl)propanamide (2 c) and N-(6-bromobenzo[d]thiazol-2-yl)-3-(pyrrolidin-1-yl)propanamide (2 h) showed good inhibitory potency against BuChE with IC50 values of 15.12 µM and 12.33 µM, respectively. Besides, 2 c and 2 h also exhibited selective MAO-B inhibitory effects with inhibition rates of 60.10 % and 66.30 % at 100 µM, respectively. In contrast, all designed derivatives were poor active against AChE and MAO-A at a concentration of 100 µM. The toxicity analysis in vitro by MTT and AO/EB fluorescence staining confirmed that 2 c and 2 h were nontoxic up to 100 µM. Molecular modeling studies showed that 2 c and 2 h could bind to the active site of BuChE. This research paves the way for further study aimed at designing MAO-B and BuChE inhibitors for the treatment of neurodegenerative disorders.


Assuntos
Doença de Alzheimer , Butirilcolinesterase , Humanos , Butirilcolinesterase/metabolismo , Inibidores da Monoaminoxidase/farmacologia , Acetilcolinesterase/metabolismo , Inibidores da Colinesterase/química , Monoaminoxidase , Benzotiazóis/farmacologia , Morfolinas , Relação Estrutura-Atividade , Estrutura Molecular , Simulação de Acoplamento Molecular
2.
Zhonghua Yu Fang Yi Xue Za Zhi ; 56(11): 1543-1548, 2022 Nov 06.
Artigo em Chinês | MEDLINE | ID: mdl-36372741

RESUMO

Objective: To evaluate the recognition of acute respiratory infection (ARI) by a pretrained model based on electronic medical records (EMRs). Methods: 38 581 EMRs were obtained from Chongqing University Three Gorges Hospital in December 2021. Bidirectional encoder representation from transformers (BERT) pretrained model was used to identify ARI in EMRs. The results of medical professionals were considered as the gold standard to calculate the sensitivity, specificity, Kappa value, and area under the curve of the receiver operating characteristic (AUC). Results: There were 3 817 EMRs in the test set, with 1 200 ARIs. A total of 1 205 cases were determined as ARI by the model, with a sensitivity of 92.67% (1 112/1 200) and a specificity of 96.45% (2 524/2 617). The model identified ARI with similar accuracy in males and females (AUCs 0.95 and 0.94, respectively), and was more accurate in identifying ARI cases in those aged less than 18 than in adults 18-59 and adults 60 and older (AUCs 0.94, 0.89 and 0.94, respectively). The current model had a better identification of ARIs in outpatient patients than that in hospitalized patients, with AUCs of 0.74 and 0.95, respectively. Conclusion: The use of the BERT pretrained model based on EMRs has a good performance in the recognition of ARI cases, especially for the outpatients and juveniles. It shows a great potential to be applied to the monitoring of ARI cases in medical institutions.


Assuntos
Registros Eletrônicos de Saúde , Infecções Respiratórias , Adulto , Masculino , Feminino , Humanos , Infecções Respiratórias/diagnóstico , Pacientes Ambulatoriais
3.
Zhonghua Yu Fang Yi Xue Za Zhi ; 56(10): 1494-1498, 2022 Oct 06.
Artigo em Chinês | MEDLINE | ID: mdl-36274620

RESUMO

On May 20, 2022, World Health Organization (WHO) Position Paper on Understanding the Behavioural and Social Drivers of Vaccine Uptake (BeSD) was published. This review introduced the BeSD toolkit, interventions to increase vaccine uptake, and offered WHO's position and recommendation. Based on immunization practice, this position paper had some implications for improving the vaccination coverage in China: (1) To promote the BeSD toolkit localization; (2) To integrate the measurement and monitoring of BeSD into multisectoral routine efforts; (3) To enhance the diversity and professionalization of immunization practitioners; (4) To design and carry out implementation research scientifically.


Assuntos
Programas de Imunização , Vacinas , Humanos , Esquemas de Imunização , Política de Saúde , Organização Mundial da Saúde , Vacinação
4.
Zhonghua Yu Fang Yi Xue Za Zhi ; 54(3): 314-319, 2020 Mar 06.
Artigo em Chinês | MEDLINE | ID: mdl-32187938

RESUMO

Objective: To systematically evaluate the quality of gastric cancer screening guidelines/recommendations, and provide a reference for the update of gastric cancer screening guidelines/recommendations in China. Methods: "guidelines/consensus/specifications/standards" , "stomach/gastric tumors" , "screening/diagnosis" , "guideline/recommendation" , "gastric cancer/gastric tumor," "early detection of cancer/screening" were searched as keywords in PubMed, Embase, Web of knowledge, China Knowledge Network, Wanfang, China Biomedical Literature Database, and Cochrane Library, as well as the US Preventive Services Working Group, the American Cancer Society, the International Agency for Research on Cancer, the Australia Cancer Council and the International Guide Collaboration Network at the end of July 2018. The inclusion criteria were independent guidelines/recommendation documents for gastric cancer screening. The exclusion criteria were guideline abstracts, interpretation and evaluation literature, duplicate publications, updated original guidelines, and clinical treatment or practice guidelines for gastric cancer. The language was limited to Chinese and English. The European Guide to Research and Evaluation Tools (AGREE Ⅱ) and Practice Guideline Reporting Standard (RIGHT) for Gastric Cancer Screening Guidelines/Recommendations were used to compare and evaluate the quality and reporting standard of gastric cancer screening guidelines/recommendations. Results: A total of five guides/recommendations were included. The results of the AGREE Ⅱ quality evaluation showed that the overall quality of five guides/recommendations was different, including one recommended for "A", one for "B", and three for "C". Each guide/recommendation scored higher in the scope and purpose, clarity, and scores were more significant in the areas of rigor and independence. In the participants, the application field scores were generally low. The RIGHT evaluation results showed that the quality of five guides/recommendations should be improved. The six items with poor report quality were background, evidence, recommendations, review and quality assurance, funding and conflict of interest statement and management, and other aspects. Conclusion: The quality of the included gastric cancer screening guidelines/recommendations is generally low, and the standardization should be strengthened.


Assuntos
Detecção Precoce de Câncer/normas , Guias de Prática Clínica como Assunto/normas , Neoplasias Gástricas/diagnóstico , China , Consenso , Detecção Precoce de Câncer/métodos , Humanos , Padrões de Referência
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