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1.
Article in English | MEDLINE | ID: mdl-33498593

ABSTRACT

Scheduled naps in the workplace are an effective countermeasure to drowsiness in safety-sensitive industries. This quasi-experimental study with a one-group, pre- and post-test design aimed to examine the effects of scheduled naps on nurses working 12-h shifts. Nurses in two pediatric intensive care units at a tertiary hospital were provided 30-min scheduled nap opportunities during their shifts. A total of 38 nurses completed pre- and post-test work diaries for sleepiness, fatigue, work demands and pace, and quality of nursing care at the end of each shift. The drowsiness of 13 nurses was continuously assessed during their shifts using infrared reflectance oculography. Nurses who reached naps reported improved levels of fatigue on the first night shift and better quality of nursing care the second night and day shifts post-test, while nurses who did not reach naps showed no significant improvements. The oculography successfully assessed drowsiness during 73% and 61% of the pre- and post-test total work hours, respectively. The total cautionary and cautionary or higher levels of drowsiness decreased. Nurse managers should consider scheduled naps in clinical settings to improve nurses' alertness during their shifts.


Subject(s)
Sleep Disorders, Circadian Rhythm , Sleepiness , Child , Fatigue , Humans , Sleep , Wakefulness , Work Schedule Tolerance
2.
J Korean Med Sci ; 35(28): e255, 2020 Jul 20.
Article in English | MEDLINE | ID: mdl-32686372

ABSTRACT

Quarantine often provokes negative psychological consequences. Thus, we aimed to identify the psychological and behavioral responses and stressors of caregivers quarantined with young patients after a close contact to a coronavirus disease 2019 case at a children's hospital. More than 90% of the caregivers reported feelings of worry and nervousness, while some of them reported suicidal ideations (4.2%), and/or homicidal ideations (1.4%). Fear of infection of the patient (91.7%) and/or oneself (86.1%) were most frequently reported stressors. A multidisciplinary team including infection control team, pediatrician, psychiatrist, nursing staff and legal department provided supplies and services to reduce caregiver's psychological distress. Psychotropic medication was needed in five (6.9%), one of whom was admitted to the psychiatry department due to suicidality. Quarantine at a children's hospital makes notable psychological impacts on the caregivers and a multidisciplinary approach is required.


Subject(s)
Caregivers/psychology , Coronavirus Infections/psychology , Pneumonia, Viral/psychology , Quarantine/psychology , Stress, Psychological/psychology , Anxiety/psychology , COVID-19 , Coronavirus Infections/transmission , Disease Transmission, Infectious/prevention & control , Hospitals, Pediatric , Humans , Pandemics , Pneumonia, Viral/transmission
3.
Med Chem ; 9(3): 410-9, 2013 May.
Article in English | MEDLINE | ID: mdl-22931492

ABSTRACT

A quantitative structure-activity relationship (QSAR) study of aromatic inhibitors against aldose reductase (AR) activity was performed using variable selection from stepwise multiple linear regression (MLR) and genetic algorithm (GA)-MLR. As a result of variable selection, stepwise MLR and GA-MLR gave the same results with one, two, three and five descriptors and different results with four and six descriptors. GA-MLR produced higher values and was better in explanatory and predictive power than stepwise MLR in four variables. AR activity (pIC50) of aromatic derivatives was expressed with acceptable explanatory (74.6-81.2%) and predictive power (68.8-74.4%) in models 3 and 4. The resulting models with the given descriptors illustrate that hydrophobic and electrostatic interactions play a significant role in inhibition of AR activity. This study suggests that the QSAR models can be used as guidelines to predict improved aldose reductase inhibitory activity and to obtain reliable predictions in structurally diverse compounds.


Subject(s)
Aldehyde Reductase/antagonists & inhibitors , Enzyme Inhibitors/chemistry , Enzyme Inhibitors/pharmacology , Lens, Crystalline/enzymology , Models, Biological , Animals , Enzyme Activation/drug effects , Hydrophobic and Hydrophilic Interactions , Inhibitory Concentration 50 , Molecular Structure , Quantitative Structure-Activity Relationship , Rats
4.
Molecules ; 17(9): 10446-58, 2012 Sep 03.
Article in English | MEDLINE | ID: mdl-22945025

ABSTRACT

Simple synthesis of modafinil derivatives and their biological activity are described. The key synthetic strategies involve substitution and coupling reactions. We determined the anti-inflammatory effects of modafinil derivatives in cultured BV2 cells by measuring the inhibition of nitrite production and expression of iNOS and COX-2 after LPS stimulation. It was found that for sulfide analogues introduction of aliphatic groups on the amide part (compounds 11a­d) resulted in lower anti-inflammatory activity compared with cyclic or aromatic moieties (compounds 11e­k). However, for the sulfoxide analogues, introduction of aliphatic moieties (compounds 12a­d) showed higher anti-inflammatory activity than cyclic or aromatic fragments (compounds 12e­k) in BV-2 microglia cells.


Subject(s)
Anti-Inflammatory Agents, Non-Steroidal/chemical synthesis , Anti-Inflammatory Agents, Non-Steroidal/pharmacology , Benzhydryl Compounds , Cyclooxygenase 2/metabolism , Nitric Oxide Synthase Type II/metabolism , Nitrites/antagonists & inhibitors , Anti-Inflammatory Agents, Non-Steroidal/chemistry , Antioxidants/chemical synthesis , Antioxidants/chemistry , Antioxidants/pharmacology , Benzhydryl Compounds/chemistry , Benzhydryl Compounds/pharmacology , Cell Line, Tumor , Cell Survival/drug effects , Humans , Lipopolysaccharides/immunology , Modafinil , Nitric Oxide/metabolism , Safrole/analogs & derivatives , Safrole/chemistry , Sulfides/chemistry
5.
Molecules ; 17(2): 2091-102, 2012 Feb 21.
Article in English | MEDLINE | ID: mdl-22354187

ABSTRACT

The total synthesis and structure determination of cis- and trans-flocoumafen was described. The key synthetic steps involve Knoevenagel condensation with p-methoxybenzaldehyde, in situ decarboxylation and intramolecular ring cyclization to construct the tetralone skeleton. Stereospecific reduction of the O-alkylated ketone 13 afforded good yield of precusor alcohol 5. Final coupling of alcohol 5 with 4-hydroxy-coumarin yielded flocoumafen (1). Separation and structure determination of cis- and trans-flocoumafen through 2D NMR analyses-assisted computer simulation techniques for the evaluation of anticoagulant activities are reported for the first time. This method is useful for generating the core tetralone skeleton of 4-hydroxycoumarin derivatives and provides a generalized access to various warfarin type anticoagulants.


Subject(s)
4-Hydroxycoumarins/chemistry , 4-Hydroxycoumarins/chemical synthesis , Biological Products/chemistry , Biological Products/chemical synthesis , Alkylation , Anticoagulants/chemistry , Benzaldehydes/chemistry , Cyclization , Decarboxylation
6.
Molecules ; 16(12): 10409-19, 2011 Dec 15.
Article in English | MEDLINE | ID: mdl-22173334

ABSTRACT

Simple synthesis and biological activities of modafinil derivatives are described. The key reactions include condensation of acid and propargyl alcohol, subsequent 1,3-dipolar cycloaddition reaction of alkynes and (3-azido-propyl)cyclohexane or (4-azido-butyl)benzene in the presence of sodium ascorbate and CuSO4·5H2O in excellent yield. They were then evaluated for the suppression of LPS-induced NO generation in vitro. It was found that all compounds showed moderate effects for suppression of LPS-induced NO generation.


Subject(s)
Benzhydryl Compounds/chemical synthesis , Benzhydryl Compounds/pharmacology , Triazoles/chemical synthesis , Triazoles/pharmacology , Animals , Benzhydryl Compounds/chemistry , Cell Line , Esters/chemical synthesis , Esters/chemistry , Esters/pharmacology , Mice , Microglia/cytology , Microglia/drug effects , Microglia/metabolism , Modafinil , Nitric Oxide/metabolism , Triazoles/chemistry
7.
Molecules ; 16(12): 9886-99, 2011 Nov 28.
Article in English | MEDLINE | ID: mdl-22124203

ABSTRACT

Dimethyl lithosermate B (DLB) is a highly potent natural antioxidant and antidiabetic polyphenol with unknown mode of action. To determine its cellular targets, a photochemical and fluorescent dimethyl lithopermate B probe was designed and efficiently synthesized. The dual-labeled chemical probe for biological application was evaluated by UV and fluorescence to determine its electrochemical absorption and emission properties. This probe could be valuable for investigating ligand-protein interactions and subcellular localization.


Subject(s)
Drugs, Chinese Herbal/chemical synthesis , Molecular Probes/chemical synthesis , Photoaffinity Labels/metabolism , Photochemical Processes , Drugs, Chinese Herbal/chemistry , Spectrometry, Fluorescence , Spectrophotometry, Ultraviolet , Ultraviolet Rays
8.
Chem Biol Drug Des ; 78(4): 725-9, 2011 Oct.
Article in English | MEDLINE | ID: mdl-21791008

ABSTRACT

Here, we describe the practical synthesis and biological properties of bergenin and its structural analogs. Synthetic bergenin compounds were prepared by acylation of bergenin. These compounds were then evaluated for suppression of lipopolysaccharide-induced nitric oxide (NO) generation in cultured cells and anti-narcotic effects on morphine-dependent mice. We found that bergenin derivatives showed potent anti-inflammatory activity (suppression of NO generation) at concentrations ranging from 20 to 30 µmin vitro, and bergenin derivatives (10-20 mg/kg) exhibited significant anti-narcotic effects on morphine dependence in mice. These results suggest the potential utility of bergenin and its analogs as anti-narcotic agents and the design of more potent anti-inflammatory compounds.


Subject(s)
Anti-Inflammatory Agents/chemistry , Anti-Inflammatory Agents/pharmacology , Benzopyrans/chemistry , Benzopyrans/pharmacology , Morphine Dependence/drug therapy , Nitric Oxide/metabolism , Acylation , Animals , Anti-Inflammatory Agents/chemical synthesis , Benzopyrans/chemical synthesis , Cell Line , Chemistry Techniques, Synthetic , Lipopolysaccharides/metabolism , Mice , Mice, Inbred C57BL , Microglia/cytology , Substance-Related Disorders
9.
J Appl Behav Anal ; 44(1): 121-6, 2011.
Article in English | MEDLINE | ID: mdl-21541107

ABSTRACT

Pedestrian safety is a serious concern at busy intersections and pedestrian campuses across the nation. Although crosswalks and signs inform pedestrians where to cross, there is no standard protocol for pedestrians to signal drivers that they wish to use the crosswalks, except to stand in or at the crosswalk. We examined the effects of two pedestrian prompts, a raised hand and extended arm, on motorist yielding at uncontrolled crosswalks. The two prompts were effective at increasing yielding.


Subject(s)
Accidents, Traffic/prevention & control , Automobile Driving/psychology , Conflict, Psychological , Walking/psychology , Accidents, Traffic/psychology , Accidents, Traffic/statistics & numerical data , Humans
10.
Eur J Med Chem ; 44(8): 3166-74, 2009 Aug.
Article in English | MEDLINE | ID: mdl-19375195

ABSTRACT

A convenient synthesis and the biological properties of new amides, esters and other derivatives of trans-stilbene are described. The key synthetic strategies involve the Wittig-Horner reaction of a phosphonium salt 9 and an aldehyde 10 to generate (E)- or (Z)-olefins and a coupling reaction of an acid 12 and various amines 13a-n to give trans-stilbene derivatives 15a-n in high yields. A amide derivative 15g showed three times more in vitro free radical-scavenging activity than resveratrol, while another 15d exhibited strong inhibitory activity against lipopolysaccharide (LPS)(a)-induced NO generation. Allylamide analogue 15a showed the most potent neuroprotective activity in glutamate-induced primary cortical neuron cells.


Subject(s)
Drug Design , Free Radical Scavengers/chemical synthesis , Free Radical Scavengers/pharmacology , Neuroprotective Agents/chemical synthesis , Neuroprotective Agents/pharmacology , Stilbenes/chemical synthesis , Stilbenes/pharmacology , Animals , Cell Line , Cerebral Cortex/cytology , Free Radical Scavengers/chemistry , Kinetics , L-Lactate Dehydrogenase/metabolism , Mice , Mice, Inbred ICR , Microglia/cytology , Microglia/drug effects , Microglia/metabolism , Neurons/drug effects , Neurons/metabolism , Neuroprotective Agents/chemistry , Nitric Oxide/metabolism , Stereoisomerism , Stilbenes/chemistry
11.
Chem Biol Drug Des ; 73(3): 346-54, 2009 Mar.
Article in English | MEDLINE | ID: mdl-19207471

ABSTRACT

A series of benzamide-containing stilbene derivatives was synthesized through the incorporation of short basic side-chains in the B-ring hydroxy position of resveratrol. Their antiplasmodial activity was evaluated in vitro against the chloroquine resistant Plasmodium falciparum D10 strain, showing IC(50) values between 1.5 and 80 microM, while their cytotoxicity was assessed using an human myeloid leukemia (U-937) cell line. With a selectivity ratio of > 51.02, the most selective of these derivatives, 29, also had the most lowest cytotoxic activity of the series.


Subject(s)
Antimalarials/chemistry , Antimalarials/pharmacology , Stilbenes/chemistry , Stilbenes/pharmacology , Animals , Antimalarials/chemical synthesis , Cell Line, Tumor , Humans , Inhibitory Concentration 50 , Plasmodium falciparum/drug effects , Stilbenes/chemical synthesis
12.
J Enzyme Inhib Med Chem ; 24(2): 328-36, 2009 Apr.
Article in English | MEDLINE | ID: mdl-18608762

ABSTRACT

In the present study we report the simple synthesis and antitumour activity of novel stilbene derivatives 13-22. The key synthetic strategies involved Wadsworth-Horner-Emmons condensation and coupling reactions in high yields. All compounds showed significant growth inhibition on human tumour cell lines, with the most potent compound (19) exhibiting an IC(50) of 5.7 microM-11.4 microM in vitro.


Subject(s)
Antineoplastic Agents, Phytogenic/chemical synthesis , Antineoplastic Agents, Phytogenic/pharmacology , Stilbenes/chemistry , Antineoplastic Agents, Phytogenic/chemistry , Cell Line, Tumor , Drug Screening Assays, Antitumor , Humans , Inhibitory Concentration 50 , Resveratrol , Stilbenes/chemical synthesis , Stilbenes/pharmacology
13.
J Med Chem ; 51(13): 4054-8, 2008 Jul 10.
Article in English | MEDLINE | ID: mdl-18517185

ABSTRACT

An efficient synthesis involving a key aldol reaction and biological properties of 1,3-diphenyl-2-propen-1-ones 8- 20 is described. The in vitro activity for 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging of 10 and 11 was 2 times higher than that for resveratrol. Compounds 9 and 11 were the strongest in suppression of in vitro nitric oxide (NO) generation and antiexcitotoxicity. Molecular modeling proposes an electron-donating group at the para position of acetophenones that leads to a dramatic increase in the suppression of NO production.


Subject(s)
Chalcone/chemical synthesis , Chalcone/pharmacology , Neuroprotective Agents/chemical synthesis , Neuroprotective Agents/pharmacology , Aldehydes/chemistry , Animals , Cell Line , Cell Survival/drug effects , Chalcone/chemistry , Glutarates/pharmacology , Lipopolysaccharides/pharmacology , Mice , Models, Molecular , Molecular Structure , Neurons/drug effects , Neurons/metabolism , Neuroprotective Agents/chemistry , Nitric Oxide/biosynthesis , Structure-Activity Relationship , Tissue Culture Techniques
14.
Bioorg Med Chem Lett ; 17(16): 4481-6, 2007 Aug 15.
Article in English | MEDLINE | ID: mdl-17596944

ABSTRACT

Dihydroxy stilbene derivatives were designed based on lithospermic acid B and were prepared from 4-(chloromethyl)benzoic acid. The inhibitory activities of the novel compounds against protein tyrosine phosphatase 1B (PTP1B) were evaluated. 3,4-Dihydroxy stilbene carbonyl compounds (7, 11b, 27b) inhibited PTP1B with IC50 values comparable to molybdate, while the conjugation-extended compound (15b) showed inhibition 3-fold better than preclinical RK682. The introduction of electron withdrawing groups or amides into the second phenyl ring, or extension of the conjugation into the stilbene molecule may increase stability of the generated radicals.


Subject(s)
Benzofurans/chemistry , Depsides/chemistry , Drug Design , Protein Tyrosine Phosphatase, Non-Receptor Type 1/antagonists & inhibitors , Stilbenes/chemical synthesis , Stilbenes/pharmacology , Antioxidants/chemistry , Antioxidants/pharmacology , Benzofurans/pharmacology , Depsides/pharmacology , Models, Molecular , Molecular Structure , Structure-Activity Relationship
15.
Cancer ; 104(12 Suppl): 2955-8, 2005 Dec 15.
Article in English | MEDLINE | ID: mdl-16276533

ABSTRACT

Hepatocellular cancer occurs more frequently among Koreans, Vietnamese, and Chinese than other racial/ethnic groups in the U.S. This excess risk can be attributed to high rates of chronic hepatitis B viral (HBV) infection and low rates of HBV vaccination among Asian immigrants. However, there is little available information regarding the hepatitis B knowledge, beliefs, and practices among Koreans, the fifth-largest Asian population in the U.S. This brief report summarizes results from 30 qualitative interviews and two focus groups investigating hepatitis and liver cancer prevention, behavior, and beliefs among first-generation Korean immigrant adults ages 18-64 years residing in the Seattle-Tacoma metropolitan area of Washington State. The report concludes with suggestions for future investigations to address the high rates of chronic HBV infection and hepatocellular cancer in this vulnerable population.


Subject(s)
Asian/ethnology , Culture , Health Knowledge, Attitudes, Practice , Hepatitis B/ethnology , Liver Neoplasms/virology , Adult , Emigration and Immigration , Female , Focus Groups , Humans , Korea/ethnology , Male , Middle Aged , Washington
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