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1.
Avicenna J Med ; 13(1): 49-55, 2023 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-36969351

RESUMO

Background Antibiotic resistance is a global problem, and the World Health Organization has made this problem one of its priorities for solving. Therefore, a survey was carried out to investigate the knowledge, attitude, awareness, and perceptions of antibiotic resistance among physicians and to assess the correlation between the knowledge of antibiotic resistance and their years of experience in some Palestinian hospitals. Methods This was a cross-sectional study that targeted physicians who are working in different healthcare facilities in Hebron and Bethlehem governorates. We used a questionnaire for data collection. The questionnaire consists of 42 questions to measure the knowledge, attitudes, awareness, and perceptions of antibiotic use and resistance. Results The response rate was 91.33% (137 of 150 physicians completed the questionnaire). The participants' ages ranged from 25 to 56 years, and the majority were males ( n = 116, 84.7%) working in governmental hospitals ( n = 83, 60.6%). Of physicians, 69.3% ( n = 95) perceived antibiotic resistance as a very important worldwide problem, while 54.7% ( n = 75) perceived a very important problem in the country, 54.0% ( n = 74) a very important problem in their hospital, and 59.1% ( n = 81) a very important problem in their departments. Methicillin-resistant Staphylococcus aureus was the most known antibiotic-resistant bacteria followed by extended-spectrum beta-lactamases. Only 47 physicians (34.3%) think that antibiotics are not used appropriately in their department. Respondents' physicians showed that the development of antibiotic resistance was due to various factors that include self-medication n= (92, 67.2%), overuse of antibiotics ( n = 83, 60.6%), and uncompleted treatment (n= 87, 63.5). Senior specialists/consultants were found to be more knowledgeable about antibiotic resistance. Conclusion In our survey, physicians showed variable knowledge and perceptions of antibiotic resistance. Introducing educational programs is necessary to improve their understanding and perceptions of antibiotic resistance, as well as their attitude toward antibiotic use.

2.
Avicenna J Med ; 10(4): 135-162, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-33437687

RESUMO

BACKGROUND: Coronavirus disease-2019 (COVID-19) outbreak is a global concern and the World Health Organization (WHO) has declared it as a Public Health Emergency of International Concern. The Palestinian Authority (PA) has quickly and effectively responded to the outbreak of COVID-19, using an internationally and nationally coordinated, to contain the spread of the virus within the borders. The PA approaches are containment and suppression, which is designed to protect the citizens from infection while also mitigating the stress on the health care system. The PA immediately declared a State of Emergency when the first cases in Palestine were diagnosed on 5 March 2020 and launched robust national containment measures to encourage the citizens to protect themselves and follow the guidance. OBJECTIVES: There is currently no vaccine or effective treatment for COVID-19, the treatment is either supportive and/ or the treatment of symptoms. Several strategies in the treatment of the disease were applied including medications. This review aims to summarize the different strategies, guidelines, challenges, and treatments used against COVID-19 worldwide and in Palestine. MATERIALS AND METHODS: Different literature and guidelines among different databases were searched. Literature reviewing was conducted using the following search engines, Google Scholar, Medline, Pub Med, EMBASE, Web of Science, and Science Direct. Data also obtained from WHO and PA reports, and the published peer-reviewed articles of 2019-nCoV. The review focuses on the strategies, guidelines, therapeutics, challenges, and different approaches used in the treatment and management of the disease in Palestine and globally. CONCLUSION: The Palestinian Ministry of Health (MoH) strategies to end the COVID-19 pandemic were; slow and stop transmission; provide optimized care for patients; and minimize the impact of the epidemic on health systems, social services, and economic activity. Thus, proper management, right actions, and effective treatment of the disease should be considered to achieve these strategies. The biggest problem for PA to control and stop the outbreak of the disease is the different challenges which include; the Israeli military and economic control, uncontrol the borders, shortage of medical and financial resources, crowded cities and refugee camps, poverty, food insecurity, and the financial crisis. To date, there are no specific vaccines or medicines for COVID-19; and treatments are under investigation through clinical trials. However, an array of drugs approved for other indications, as well as multiple investigational agents, are being studied for the treatment of COVID-19; in several hundred clinical trials around the World. Treatment is essentially supportive and symptomatic.

3.
J Med Chem ; 48(16): 5243-56, 2005 Aug 11.
Artigo em Inglês | MEDLINE | ID: mdl-16078843

RESUMO

Efficient and flexible syntheses of 2-substituted estrone, estradiol and their 3-O-sulfamate (EMATE) derivatives have been developed using directed ortho-lithiation methodology. 2-Substituted EMATEs display a similar antiproliferative activity profile to the corresponding estradiols against a range of human cancer cell lines. 2-Methoxy (3, 4), 2-methylsulfanyl (20, 21) and 2-ethyl EMATEs (32, 33) proved the most active compounds with 2-ethylestradiol-3-O-sulfamate (33), displaying a mean activity over the NCI 55 cell line panel 80-fold greater than the established anticancer agent 2-methoxyestradiol (2). 2-Ethylestradiol-3-O-sulfamate (33) was also an effective inhibitor of angiogenesis using three in vitro markers, and various 2-substituted EMATEs also proved to be inhibitors of steroid sulfatase (STS), a therapeutic target for the treatment of hormone-dependent breast cancer. The potential of this novel class of multimechanism anticancer agents was confirmed in vivo with good activity observed in the NCI hollow fiber assay and in a MDA-MB-435 xenograft mouse model.


Assuntos
Antineoplásicos/síntese química , Estradiol/análogos & derivados , Estradiol/síntese química , Estrona/análogos & derivados , Estrona/síntese química , Ácidos Sulfônicos/síntese química , Inibidores da Angiogênese/síntese química , Inibidores da Angiogênese/farmacologia , Animais , Antineoplásicos/farmacologia , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Cristalografia por Raios X , Ensaios de Seleção de Medicamentos Antitumorais , Estradiol/farmacologia , Estrona/farmacologia , Feminino , Humanos , Camundongos , Estrutura Molecular , Esteril-Sulfatase/antagonistas & inibidores , Relação Estrutura-Atividade , Ácidos Sulfônicos/farmacologia , Transplante Heterólogo
4.
Bioorg Med Chem ; 12(10): 2759-72, 2004 May 15.
Artigo em Inglês | MEDLINE | ID: mdl-15110857

RESUMO

Steroid sulfatase (STS) is an important new therapeutic target in oncology. Attempts to design nonsteroidal STS inhibitors, because of the oestrogenicity of the original lead oestrone 3-O-sulfamate in rodents, have led to the discovery of benzophenone-4,4'-O,O-bis-sulfamate (BENZOMATE, 3). The nonfused bicyclic BENZOMATE is a highly potent STS inhibitor in vitro, inhibiting STS activity in intact MCF-7 breast cancer cells by > 70% at 0.1 microM and in placental microsomes by > 98% at 10 microM. When MCF-7 cells were pre-treated with 3 at 1 microM and then washed to remove unbound inhibitor, the initial 94% inhibition was reduced to 89% suggesting that 3, like other sulfamate-based STS inhibitors, inhibits the enzyme irreversibly. This agent also inhibits rat liver STS activity by 84% and 93% respectively 24 h after a single dose of 1 or 10 mg/kg, demonstrating that BENZOMATE possesses similar in vivo potency to the established potent nonsteroidal inhibitor 667COUMATE. Several modifications were made to BENZOMATE structurally and effects on in vitro activity were examined. These structure-activity relationship studies show that its carbonyl and bis-sulfamate groups are pivotal for activity, although conformational flexibility is not required. Two rigid anthraquinone-based sulfamate derivatives however showed inhibitory activity significantly better than BENZOMATE in the MCF-7 cell assay. BENZOMATE and related analogues therefore represent an important class of non-steroidal STS inhibitor and lead compounds for future drug design.


Assuntos
Benzofenonas/síntese química , Benzofenonas/farmacologia , Inibidores Enzimáticos/síntese química , Inibidores Enzimáticos/farmacologia , Esteril-Sulfatase/antagonistas & inibidores , Animais , Benzofenonas/química , Linhagem Celular Tumoral , Inibidores Enzimáticos/química , Feminino , Humanos , Fígado/enzimologia , Ratos , Ratos Wistar
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