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阿维巴坦(Avibactam)是一个与酶可逆性共价结合新型的β-内酰胺酶抑制剂,目前处于Ⅲ期临床试验。阿维巴坦较已上市的3个β-内酰胺酶抑制剂——克拉维酸、舒巴坦、三唑巴坦——作用更强范围更广,对A类、C类和部分D类β-内酰胺酶抑制作用显著。与头孢他啶、头孢洛林等药物联用时,其能够恢复或增强抗生素的活性,耐受性良好,无严重不良事件报道。本文对阿维巴坦的作用机制、药代动力学、联合用药、毒副作用和合成路线等方面作一综述。 相似文献
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细菌耐药问题日益严峻,已经引起了公众的广泛关注。β-内酰胺类抗生素是应用最广的抗生素,但是细菌对此类药物的耐药严重降低了药物的治疗效果,而产生β-内酰胺酶是β-内酰胺类药物耐药的主要机制,研制β-内酰胺酶抑制剂,以此作为增效剂与β-内酰胺类抗生素联用,可有效恢复细菌对β-内酰胺类药物的敏感性。临床上广泛传播的β-内酰胺酶有丝氨酸β-内酰胺酶和金属β-内酰胺酶。目前,在增效剂的研究中,已经获得了多种有效的丝氨酸β-内酰胺酶抑制剂,许多金属β-内酰胺酶抑制剂仍处于研究阶段。此外,为了应对由多种β-内酰胺酶引起的多重感染,研发丝氨酸β-内酰胺酶/金属β-内酰胺酶双重抑制剂也是逆转β-内酰胺类抗生素耐药性的新思路。本文综述了β-内酰胺酶抑制剂的研究进展,为研制新型β-内酰胺酶抑制剂提供借鉴。 相似文献
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目的分析头孢他啶-阿维巴坦药物不良反应(ADR)的一般规律。方法在中国知网、维普数据库、万方数据库、PubMed、ClinicalTrials.gov(网站)中检索2008-01-01至2019-12-31发表的头孢他啶-阿维巴坦ADR的文献以及临床试验,并对头孢他啶-阿维巴坦的ADR进行汇总分析。结果共纳入文献17篇,其中临床试验11篇。共收集头孢他啶-阿维巴坦ADR的例次841例,其中合并用药出现ADRs例次344例,发生ADR涉及全身多个组织器官,主要为消化系统和神经系统等。结论头孢他啶-阿维巴坦所致ADR可累及全身多个器官,应引起临床重视。 相似文献
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目的:分析头孢他啶-阿维巴坦钠对碳青霉烯耐药的革兰阴性菌(carbapenem-resistant gram-negative organisms,CRO)感染患者的临床疗效及其影响因素,为临床头孢他啶-阿维巴坦钠的使用提供参考。方法:选取2019年9月—2022年5月苏州大学附属第二医院收治的48例使用头孢他啶-阿维巴坦钠治疗的CRO感染患者作为研究对象,采集患者的年龄、性别、感染类型及其病原菌状况、抗菌药物使用情况、其他辅助治疗操作、治疗结局等信息,分析头孢他啶-阿维巴坦钠对CRO感染患者的临床疗效和相关影响因素。结果:48例CRO感染患者中,多数患者为多部位感染(28例,占58.33%),感染类型主要为肺部感染(29例,占60.42%),而病原菌主要为肺炎克雷伯菌(39例,占81.25%)和铜绿假单胞菌(21例,占43.75%);在治疗上多数患者存在药物联用情况(29例,占60.42%),而其中联用药物以碳青霉烯类药物为主(17例,占58.62%);头孢他啶-阿维巴坦钠的治疗结果显示,临床有效的有33例(占68.75%),而无效的有15例(占31.25%);回归分析结果显示,CR... 相似文献
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安立生坦(1)是一种内皮素-1受体拮抗药,2-羟基-3-甲氧基-3,3-二苯基丙酸(2)是合成1的关键中间体,本研究报道了合成2的新方法.二苯甲酮(3)与磷酰基乙酸三乙酯经Wittig-Horner反应生成3,3-二苯基丙烯酸乙酯(4).以甲醇为溶剂,4与N-溴代丁二酰亚胺(NBS)亲电加成得到2-溴-3-甲氧基-3,... 相似文献
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依匹哌唑是一种多巴胺和5-羟色胺活性调节剂,非典型抗精神病药物,可作为辅助药物用于重度抑郁症的辅助治疗,也可以用于成人精神分裂症的治疗.本文对依匹哌唑及其关键中间体的合成方法作了详细阐述,并评估了依匹哌唑关键中间体7-羟基喹啉-(1H)-2-酮和4-(1-哌嗪基)苯并[b]噻吩的相关合成工艺,为依匹哌唑的合成及工业化生... 相似文献
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β-内酰胺酶抑制剂复方制剂在临床上被广泛应用于治疗耐药菌所致感染,由于早期β-内酰胺酶抑制剂的抑酶谱较
窄,抑酶谱更广泛的酶抑制剂在不断研发之中。与一般抗菌药物临床前研究不同,β-内酰胺酶抑制剂复方制剂的临床前研究需
明确β-内酰胺类药物或酶抑制剂本身的抗菌谱与抗菌活性,尤其是明确酶抑制剂是否具有抗菌活性。需要确定合适的β-内酰胺
类药物与酶抑制剂复方制剂,以及适用的不同酶型的目标病原菌。本文主要介绍新型β-内酰胺酶抑制剂复方制剂临床前研究方
法。临床前研究阶段的β-内酰胺酶抑制剂复方制剂研究包括体外研究和体内研究两部分,前者主要为体外药效学研究和体外药
动学/药效学(pharmacokinetic/pharmacodynamic, PK/PD)研究,常用研究方法包括β-内酰胺类药物和β-内酰胺酶抑制剂复方制剂最
低抑菌浓度测定、最低杀菌浓度测定、抗生素后效应测定及时间杀菌曲线。后者主要为动物药动学研究、感染动物药效学研究
和感染动物药动学/药效学研究。在动物药动学/药效学研究中,需考虑β-内酰胺类药物与酶抑制剂的相互影响。这些研究方法的
应用旨在阐明β-内酰胺酶抑制剂复方制剂两组分药效学特点、药动学相似与否、PK/PD指数及其临床前PK/PD靶值,为进入临
床试验阶段目标适应症及剂量选择提供依据。 相似文献
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摘要:Wnt/β-catenin信号通路是一条广泛存在于生物体内且在进化上具有高度保守特性的通路。该通路在细 胞生长、发育、迁移及凋亡过程中发挥着重要作用。特异性蛋白-5(Sp5)作为Wnt/β-catenin信号通路的下游靶点,在 发育过程中也有着重要的调控作用,包括细胞分化、组织形成及肿瘤的发生等。本文就Wnt/β-catenin信号通路对其 下游分子Sp5的作用进行综述,明确Wnt/β-catenin-Sp5在疾病发展中的作用。 相似文献
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Establishment and application of the screening model of the Mycobacterium tuberculosis β-lactamase BlaC inhibitors 下载免费PDF全文
With the continuous emergence and rapid spread of multidrug-resistant and extensively-drug-resistant Mycobacterium tuberculosis strains, it is imperative to develop novel therapies against this bacterium. The intrinsic β-lactam resistance ofM. tuberculosis is primarily due to the production of an Ambler class-A β-lactamase BlaC, which limits the application of β-lactam antibiotics in the treatment of tuberculosis. Therefore, the inhibitors of BlaC could be novel anti-tuberculosis drug synergistic agents to recover the sensibility of M. Tuberculosis to the β-lactam antibiotics. In the present study, BlaC of M. tuberculosis was expressed and purified to establish a screening model of the BlaC inhibitors. The screening conditions were determined, and the screening model was evaluated to fit for the high throughput screening. A total of 22 BlaC inhibitors were screened out from 26 400 compound samples with a positive rate of 0.083%. Taken together, our findings lay the foundation for the discovery of novel anti-tuberculosis drug synergistic agents in clinic. 相似文献
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A functional divergency oriented synthetic approach to the azoninone (9-membered lactams), key intermediate for the indolizidine alkaloids library, using amide enolate induced aza-Claisen rearrangement has been achieved. 相似文献
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Research progress of synthetic lactacystin and its analogs as β-lactone proteasome inhibitors 下载免费PDF全文
As Bortezomib and Carfilzomib are approved to treat refractory multiple myeloma, 20S proteasome has become a highly interested tumor therapeutic target. Because of drug resistance of Bortezomib and Carfilzomib, β-lactone natural products are used to treat cancer, arthritis, asthma, and Alzheimer’s diseases. Now the second generation drug candidates are developed, eg. Salinosporamide A (1). This review is aiming to encapsulate the synthetic methods of β-lactone proteasome inhibitors, lactacystin (3) and its analogs. 相似文献
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Jae Yeon Cheong Su Hang Choi Nam Tae Woo Jae Young Shin Su Woong Kim Won Tae Jung 《Archives of pharmacal research》1995,18(2):69-74
In order to improve physico-chemical properties and to enhance stability of drugs, amino acid salt has been widely adopted
in pharmaceutical synthesis. Acetylsalicylic acid lysinate is one of the widely used analgesics and it is a good example of
this synthesis. In the case of acetylsalicylic acid lysinate synthesis, racemization of naturally occurred lysine is essential
because the racemic lysine salt of the drug shows better yield, crystallinity and dryness than that of the L-lysine salt.
To establish a simple, practical and economical process for L-lysine racemization, L-lysine treatments with phosphoric acid
and with acetic acid were compared and the optimum conditions for its process and derivatization were investigated by chiral
separation methods using GC-MS spectroscopy. 相似文献
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《中国抗生素杂志》2009,45(5):403-410
Caerulomycins are a kind of natural alkaloids featuring a 2,2'-bipyridine scaffold. Caerulomycins and their analogues exhibited potential bioactivities such as antimicrobial, cytotoxic, and immunosuppressive activities. Synthetic chemists have explored synthetic methods and synthesized these compounds. The synthetic methods and the significance of caerulomycins focusing on caerulomycins A and E were reviewed in this paper. The prospects for the synthesis of such compounds were 相似文献