共查询到20条相似文献,搜索用时 625 毫秒
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又到人间四月天。每年的愚人节,总会想起一个人。想起他的动人笑脸,想起他离去时的决绝。2003年4月1日,香港文华酒店,张国荣。一个集万千宠爱于一身的人,选择在这样特殊的时间和地点,毫无征兆地离开,让当时还笼罩在SARS阴影中的人们猝不及防。那一夜多少人无心睡眠。还记得他生前的最后一则新闻是这样的: 相似文献
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目的总结汶川地震后过渡期的疾病控制工作措施,保障灾区群众健康。方法根据地震灾区过渡期卫生防疫工作的实践经验,进行回顾性总结分析。结果总结出重点落实的6项防疫措施:①摸底调查,制定灾区防疫工作计划。②大力开展卫生宣教,让村民养成良好的卫生习惯。③搞好环境卫生,认真开展消杀灭等工作。④进行水质检验,确保饮水安全。⑤加强重点疾病的监测防控,防止传染病暴发流行。⑥加强食品卫生管理,防止发生食源性疾病。采取上述措施后,灾区无传染病暴发流行,无发生群体性食物中毒,实现了大灾之后无大疫的目标。结论采取各项预防措施对于预防地震灾后传染病的流行具有重大的意义。 相似文献
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医院里患者最常听到的问候语是:好好休息,祝你早日康复。传统观念中患病总是与休息联系在一起。休息的医学术语叫制动,包括:卧床(各种伤病住院时普遍的措施)、局部固定(骨折或脱位时常用)等。休息的目的是为了保护身体健康。然而休息并不总是有利于康复。这里要谈的就是休息的另一面。先谈谈心血管疾病。许多患者发病时都采用卧床休 相似文献
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介绍了HIV逆转录酶抑制剂和蛋白酶抑制剂、DNA聚合酶抑制剂、肌苷单磷酸(IMP)脱氢酶抑制剂、S-腺苷高半胱氨酸(SAH)水解酶抑制剂以及胞嘧啶三磷酸核苷酸(CTP)合成酶抑制剂的研究进展,并图解说明了这几种抑制剂的作用机制. 相似文献
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Lin MC Lin GZ Shen YF Jian SY Hsieh DK Lin J Lin G 《Chemical research in toxicology》2012,25(7):1462-1471
1,3,5-Tri-N-alkylcarbamylphloroglucinols (1-4) are synthesized as a new series of bulky inhibitors of acetylcholinesterase that may block the catalytic triad, the anionic substrate binding site, and the entrance of the enzyme simultaneously. Among three series of phloroglucinol-derived carbamates, tridentate inhibitors 1,3,5-tri-N-alkylcarbamylphloroglucinols (1-4), bidentate inhibitors 3,5-di-N-n-alkylcarbamyloxyphenols (5-8), and monodentate inhibitors 5-N-n-alkylcarbamyloxyresorcinols (9-12), tridentate inhibitors 1-4 are the most potent inhibitors of mouse acetylcholinesterase. When different n-alkylcarbamyl substituents in tridentate inhibitors 1-4 are compared, n-octylcarbamate 1 is the most potent inhibitor of the enzyme. All inhibitors 1-12 are characterized as the pseudo substrate inhibitors of acetylcholinesterase. Thus, tridentate inhibitors 1-4 are supposed to be hydrolyzed to bidentate inhibitors 5-8 after the enzyme catalysis. Subsequently, bidentate inhibitors 5-8 and monodentate inhibitors 9-12 are supposed to yield monodentate inhibitors 9-12 and phloroglucinol, respectively, after the enzyme catalysis. This means that tridentate inhibitors 1-4 may act as long period inhibitors of the enzyme. Therefore, inhibitors 1-4 may be considered as a new methodology to develop the long-acting drug for Alzheimer's disease. Automated dockings of inhibitor 1 into the X-ray crystal structure of acetylcholinesterase suggest that the most suitable configuration of inhibitor 1 to the enzyme binding is the (1,3,5)- (cis,trans,trans)-tricarbamate rotamer. The cis-carbamyl moiety of this rotamer does not bind into the acetyl group binding site of the enzyme but stretches out itself to the entrance. The other two trans-carbmayl moieties of this rotamer bulkily block the tryptophan 86 residue of the enzyme. 相似文献
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《Expert opinion on therapeutic patents》2013,23(5):617-620
Novel methylsulfoxide analogues, of known selective cyclooxygenase-2 (COX-2) inhibitors, with a methylsulfone moiety are claimed as COX-2 inhibitors. The inhibitors are useful for the treatment of COX-2-mediated disorders comprising inflammation and inflammation-associated disorders. The clinical applicability for development of the claimed sulfoxide analogues as COX-2 inhibitors is eval-uated against the car-diovascular and gastrointestinal safety. 相似文献
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Satoshi Takamatsu 《Journal of natural medicines》2018,72(4):817-835
This paper reviews naturally occurring cell adhesion inhibitors derived from a plant, microbial and marine origin. Plant-derived inhibitors are classified according to a type of structure. Microbially and marine-derived inhibitors were described according to age. In addition, effects of inhibitors on cell proliferation and that of standards on cell adhesion are listed as much as possible. 相似文献
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Various drugs were tested as inhibitors of diamine oxidase on the basis of chemical relationships to the enzyme substrates. It was found that serotonine tryptamine and phenformin are good competitive inhibitors while cimetidine and pheniprazine are non-competitive inhibitors. Other antihistaminic drugs like promethazine are less powerful inhibitors. 相似文献
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Over the past decade, therapeutics that target subsets of the 518 human protein kinases have played a vital role in the fight against cancer. Protein kinases are typically targeted at the adenosine triphosphate (ATP) binding cleft by type I and II inhibitors, however, the high sequence and structural homology shared by protein kinases, especially at the ATP binding site, inherently leads to polypharmacology. In order to discover or design truly selective protein kinase inhibitors as both pharmacological reagents and safer therapeutic leads, new efforts are needed to target kinases outside the ATP cleft. Recent advances include the serendipitous discovery of type III inhibitors that bind a site proximal to the ATP pocket as well as the truly allosteric type IV inhibitors that target protein kinases distal to the substrate binding pocket. These new classes of inhibitors are often selective but usually display moderate affinities. In this review we will discuss the different classes of inhibitors with an emphasis on bisubstrate and bivalent inhibitors (type V) that combine different inhibitor classes. These inhibitors have the potential to couple the high affinity and potency of traditional active site targeted small molecule inhibitors with the selectivity of inhibitors that target the protein kinase surface outside ATP cleft. 相似文献
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Protein kinases have emerged as the most important class of targets in oncology drug discovery because of their major roles in regulating cellular growth and survival. At least, 11 kinase inhibitors have received FDA approval to be used as cancer treatments, and there are continuous efforts to bring more candidates from laboratory benches to the clinic. Although many protein kinase inhibitors directly interact with the ATP binding site, other can alter the kinase conformation to prevent productive ATP binding. Herein we discuss the different mechanisms of action of kinase inhibitors and provide classification of the inhibitors according to their binding sites. Some of these are allosteric inhibitors, ATP competitive inhibitors, protein substrate competitive inhibitors, and covalent bond forming inhibitors. This review provides a broad overview of the relation between mechanism of action and the issues of target selectivity and resistance. Special attention was given to the kinase inhibitors currently in clinical trials. 相似文献
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There are two types of anti-obesity agents which are classified as inhibitors of absorption: inhibitors of lipid and carbohydrate absorption. Inhibitors of lipid absorption consist of lipase inhibitor (orlistat, Nomma Herb's extract (CT-II) and fat substitute (olestra, sucrose polyester). Orlistat is now available as an anti-obesity drug in the USA and Europe. CT-II may be useful as a functional diet. Application of fat substitute is still limited in snack food. As for inhibitors of carbohydrate absorption, alpha-glucosidase inhibitors are now available as anti-diabetic drugs. To develop these agents for anti-obesity drug, solution of adverse effects on the gastrointestinal tract are necessary. 相似文献
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Nzila A 《Drug discovery today》2006,11(19-20):939-944
Antifolates, inhibitors of folate synthesis or folate conversion, are used for malaria treatment. They are developed as synergistic combinations of inhibitors of dihydrofolate reductase (DHFR) and of dihydropteroate synthase (DHPS). DHPS inhibitors are sulfur-based drugs, analogs of sulfanilamide. These compounds compete with para-aminobenzoic acid in the active site of DHPS. The discovery of new antifolates is based on the identification of DHFR inhibitors; little work has been done on sulfur-based drugs because of their toxicity. As a result, only a few sulfur-based drugs are available. In this review, the hypothesis that compounds that compete with pteridine derivatives in active sites of de novo folate enzymes can be used as synergizers of DHFR inhibitors is discussed. If correct, this could lead to the identification of a new family of synergizers of DHFR inhibitors. 相似文献
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Anand-Krishna Singh Rameshwar Jatwa Ashok Purohit 《Journal of Asian natural products research》2017,19(10):1036-1045
Currently antidiabetic therapeutic strategies are mainly based on synthetic hypoglycemic agent. Antidiabetic drugs are associated with significant adverse effects of hypoglycemia, dysfunction of insulin and weight gain. Nowadays, the novel Dipeptidyl peptidase-IV (DPP-IV) inhibitors unique approach for the management of diabetes has been considered to be safe, as DPP-IV inhibitors reduce blood glucose level by monitoring hyperglycemia including positive effects on body weight as it remains neutral, improves glycated hemoglobin levels and do not induce hypoglycemia. Inhibitors help to protect degradation of Glucagon-like peptide-1 (GLP-1) and gastric inhibitory peptide (GIP), gut hormones which helps to suppresses postprandial glucagon release, delay gastric emptying and regulate satiety. Therefore, the innovation of DPP-IV inhibitor based drugs regulates activity of incretin hormones such as GLP-1 and GIP. Commercially available DPP-IV inhibitors are chemically synthesized with good therapeutic value. However, the durability and long-term safety of DPP-IV inhibitors remains to be established. On the other hand, phytocompounds-based DPP-IV inhibitors are alternative and safe to use as compared to synthetic. Numerous novel antidiabetic compounds and group of compounds emerging in clinical development are through DPP-IV inhibition. This review summarized recent progress made on DPP-IV inhibitors from both synthetic as well as from natural sources. 相似文献