Risk factors analysis of nosocomial pneumonia in elderly patients with acute cerebral infraction.

To investigate the risk factors of nosocomial pneumonia (NP) in elderly patients with acute cerebral infarction (ACI).In this study, 324 aged 70 years and over patients with ACI who were admitted to the inpatient department of TianJin First Hospital (China) from January 2012 to February 2018 were retrospectively analyzed. The patients were divided into NP group (80 patients) and non-NP group (244 patients) according to whether NP was occurred 48 hours after hospitalization.

Salvianolate injection in the treatment of acute cerebral infarction: A systematic review and a meta-analysis.

To evaluate the effectiveness and safety of Salvianolate injection (SI) in the treatment of acute cerebral infarction (ACI).We electronically searched databases including PubMed, The Cochrane Library, EMBASE, Chinese Biomedical Literature Database, Chinese National Knowledge Infrastructure, and WanFang Data to collect randomized controlled trials (RCTs) focused on SI treating ACI up to August 2017. Two reviewers independently screened literatures, extracted data, and assessed the risk of bias of included studies.

Pyrrolo[2,3-b]pyridine derivatives as potent Bruton's tyrosine kinase inhibitors.

A series of pyrrolo[2,3-b]pyridine-based derivatives were designed as potent Bruton's tyrosine kinase (BTK) inhibitors by using a scaffold-hopping strategy. Structure-activity relationship studies identified five compounds (3n, 3p, 3q, 3r, and 3s) with IC50 of less than 10nM in BTK enzyme assay and five compounds (3m, 3n, 3o, 3p, and 3t) with IC50 of less than 20 nM in Ramos cell assay. As one of the most potent inhibitors, compound 3p exhibited superior activity to that of compound 1 (RN486) and pyrrolo[2,3-d]pyrimidine derivative 2 in both BTK enzymatic (IC50=6.

Discovery of novel Bruton's tyrosine kinase (BTK) inhibitors bearing a pyrrolo[2,3-d]pyrimidine scaffold.

A series of novel reversible BTK inhibitors was designed based on the structure of the recently reported preclinical drug RN486. Knowledge of the binding mode of RN486 led to the design of new inhibitors that utilized pyrrolo[2,3-d]pyrimidine to conformationally restrain key pharmacophoric groups within the molecule. Comprehensive SAR was disclosed and the most promising compound 4x displayed superior activity both in BTK enzyme (IC50=4.

Design, synthesis and evaluation of novel 5-phenylpyridin-2(1H)-one derivatives as potent reversible Bruton's tyrosine kinase inhibitors.

A series of novel reversible Btk inhibitors has been designed based on the structure of the recently reported preclinical drug RN486. The synthesis and SAR of these compounds are described. Among these derivatives, compound 16b was identified to be a potent and orally available reversible agent with satisfactory Btk enzymatic and cellular inhibition in vitro, as well as favorable PK properties and inhibition of arthritis in vivo.