共查询到17条相似文献,搜索用时 125 毫秒
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本研究改进了洛匹那韦(1)的合成工艺.以[(1S,3S,4S)-4-氨基-3-羟基-5-苯基-1-(苯甲基)戊基]氨基甲酸叔丁酯(2)为起始原料,在苯并三唑-N,N,N',N'-四甲基脲六氟磷酸盐(HBTU)和三乙胺作用下,与2,6-二甲基苯氧乙酸(3)反应制得(2S,3S,5S)-2-(2,6-二甲基苯氧乙酰基)氨基... 相似文献
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目的:近20年来全球多次发生冠状病毒导致的严重危害公众健康的公共卫生事件,其高的传播效率、严重的感染后果以及捉摸不定的流行时间对人类健康构成严重威胁,而针对冠状病毒的治疗目前暂缺乏特效药物。HIV蛋白酶抑制剂复合制剂洛匹那韦/利托那韦广泛用于HIV的治疗,而用于治疗冠状病毒感染则相对少见。本文着重介绍洛匹那韦/利托那韦的药理作用、药动学特点及在冠状病毒感染治疗中的应用。 相似文献
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洛匹那韦/利托那韦是复方制剂,洛匹那韦与病毒蛋白酶催化部位结合干扰病毒装配过程,低剂量利托那韦抑制人体CYP3A介导洛匹那韦代谢,提高生物利用度,提高血浆中洛匹那韦药物浓度。本文对洛匹那韦/利托那韦在病毒感染性疾病的临床应用、不良反应、药物相互作用等进行介绍。 相似文献
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口服抗病毒药洛匹那韦/利托那韦的抗病毒作用受很多因素的影响,如患者性别、种族、合并症、用药依从性等。与其他药物的相互作用也是影响洛匹那韦/利托那韦抗病毒的重要因素之一,其中一些抗菌药物对洛匹那韦/利托那韦的影响较大且机制复杂,作用持续时间也较长,对于联用洛匹那韦/利托那韦合并细菌或真菌感染的患者,抗菌药物的选择与监测更为重要。本文通过综述国内外相关研究,探讨和总结洛匹那韦/利托那韦与抗菌药物的相互作用机制和应对策略,比较不同抗菌药物的药动学特性及与洛匹那韦/利托那韦相互作用的差异,从而为抗菌药物的选择和相应剂量的调整提供参考,降低患者用药风险,提高安全性。 相似文献
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目的:对利托那韦的合成工艺进行优化研究,以获得一条适宜于工业化生产的合成工艺路线。方法使用(2S,3S,5S)-2-胺基-3-羟基-5-(叔丁氧羰基胺基)-1,6-二苯基己烷的丁二酸盐作为起始原料,经过酰胺化、氨基脱保护和再酰胺化三步反应,最终制得目标产物利托那韦。结果经过相应的优化研究之后,最终成功地以较高的收率合成了高纯度的利托那韦产品(总收率57%,纯度>99%)。结论获得了一条较优的利托那韦合成工艺路线,该工艺路线具有高效、简洁以及绿色等特点,能够满足工业化生产的需要,具有广阔的应用前景。 相似文献
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Lei Shi Liping Chen Ryan Chen Liqin Chen 《Journal of labelled compounds & radiopharmaceuticals》2010,53(3):147-151
This study describes the synthesis of deuterium‐labelled fosamprenavir calcium. The stable isotopic‐labelled compound was prepared starting from L ‐phenylalanine in 18 steps with a 9% overall yield. Copyright © 2010 John Wiley & Sons, Ltd. 相似文献
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Therapeutic drug monitoring of lopinavir/ritonavir given alone or with a non-nucleoside reverse transcriptase inhibitor 下载免费PDF全文
Solas C Poizot-Martin I Drogoul MP Ravaux I Dhiver C Lafeuillade A Allegre T Mokhtari M Moreau J Lepeu G Petit N Durand A Lacarelle B 《British journal of clinical pharmacology》2004,57(4):436-440
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YEHUDITH BIRK 《Chemical biology & drug design》1985,25(2):113-131
Four decades of studies on the isolation, characterization, properties, structure, function and possible uses of the Bowman-Birk trypsin- and chymotrypsin-inhibitor from soybeans are reviewed. Starting from Bowman's Acetone Insoluble factor, designated Ai, AA and SBTIAA, the Bowman-Birk inhibitor (BBI) was found to be a protein molecule consisting of a chain of 71 amino acids cross linked by 7 disulfide bonds, with a tendency to self-associate. BBI possesses two independent sites of inhibition, one at Lys 16-Ser 17 against trypsin and the other at Leu 43-Ser 44 against chymotrypsin. It forms a 1:1 complex with either trypsin or chymotrypsin and a ternary complex with both enzymes. Ingestion of BBI by rats, chicks or quails affects the size and protein biosynthesis of the pancreas. Establishment of the full covalent structure of BBI revealed a high homology in the sequences around the two inhibitory sites, suggesting evolutionary gene duplication from a single-headed ancestral inhibitor. Scission of BBI by CNBr followed by pepsin results in two active fragments, one that inhibits trypsin and the other, chymotrypsin. Replacements and substitutions in the reactive sites result in changes in inhibitory activity and in specificity of inhibition. Conformation studies, labeling of BBI with a photoreactive reagent, chemical synthesis of cyclic peptides that include inhibitory sites, in vitro synthesis of BBI, and species specificity regarding the inhibited enzymes are described. The significance of BBI as a prototype of a family of inhibitors present in all legume seeds is discussed. 相似文献