Indinavir analogues with blocked metabolism sites as HIV protease inhibitors with improved pharmacological profiles and high potency against PI-Resistant viral strains.

Cheng Y; Zhang F; Rano T; Lu Z; Schleif W; Gabryelski L; Olsen D; Stahlhut M; Rutkowski C; Lin J; Jin L; Emini E; Chapman K; Tata J

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Indinavir analogues with blocked metabolism sites as HIV protease inhibitors with improved pharmacological profiles and high potency against PI-Resistant viral strains.

机译：具有受阻代谢位点的茚地那韦类似物作为HIV蛋白酶抑制剂，具有改善的药理作用和对PI耐药病毒株的高效力。

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Indinavir analogues with blocked metabolism sites show highly improved pharmacokinetic profiles in animals. The cis-aminochromanol substituted analogues exhibited excellent potency against both the wild-type (NL4-3) virus and protease inhibitor-resistant HIV strains.

机译：具有受阻代谢位点的茚地那韦类似物在动物中显示出大大改善的药代动力学特征。顺式氨基苯并二氢苯并二氢吡喃取代的类似物对野生型（NL4-3）病毒和耐蛋白酶抑制剂的HIV菌株均表现出优异的效力。

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《Bioorganic and Medicinal Chemistry Letters 》 |2002年第17期| 共1页
作者
Cheng Y; Zhang F; Rano T; Lu Z; Schleif W; Gabryelski L; Olsen D; Stahlhut M; Rutkowski C; Lin J; Jin L; Emini E; Chapman K; Tata J;
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正文语种 eng
中图分类药学 ; 生物化学 ;
关键词
Indinavir; metabolic aspects; S-Phase Fraction; Viral; 英地纲韦;

机译：茚地那韦;代谢方面;S相分数;病毒;英地纲韦;

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专利

1. Indinavir analogues with blocked metabolism sites as HIV protease inhibitors with improved pharmacological profiles and high potency against PI-Resistant viral strains. [J] . Cheng Y, Zhang F, Rano T, Bioorganic and Medicinal Chemistry Letters . 2002 ,第17期

机译：具有受阻代谢位点的茚地那韦类似物作为HIV蛋白酶抑制剂，具有改善的药理作用和对PI耐药病毒株的高效力。
2. Synthesis and activity of novel HIV protease inhibitors with improved potency against multiple PI-resistant viral strains. [J] . Duffy J, Kevin N, Kirk B, Bioorganic and Medicinal Chemistry Letters . 2002 ,第17期

机译：新型HIV蛋白酶抑制剂的合成与活性，具有改善多种PI抗性病毒菌株的效力。
3. The design, synthesis and evaluation of novel HIV-1 protease inhibitors with high potency against PI-resistant viral strains. [J] . Zhang F, Chapman KT, Schleif WA, Bioorganic and Medicinal Chemistry Letters . 2003 ,第15期

机译：新型HIV-1蛋白酶抑制剂对PI耐药病毒株具有高效力的设计，合成和评估。
4. P -glycoprotein mediated efflux and CYP3A4 mediated metabolism of HIV -protease inhibitor, ritonavir, and its interaction with pure herbal constituents [D] . Patel, Jignesh 2004

机译：P-糖蛋白介导的外排和CYP3A4介导的HIV-蛋白酶抑制剂利托那韦的代谢及其与纯草药成分的相互作用
5. A Conserved Hydrogen-Bonding Network of P2 bis-Tetrahydrofuran-Containing HIV-1 Protease Inhibitors (PIs) with a Protease Active-Site Amino Acid Backbone Aids in Their Activity against PI-Resistant HIV [O] . Ravikiran S. Yedidi, Harisha Garimella, Manabu Aoki, 2014

机译：含P2双四氢呋喃的HIV-1蛋白酶抑制剂（PIs）的保守氢键网络与蛋白酶活性位点氨基酸骨干的活性可抵抗PI抵抗的HIV。
6. Improved cyclic urea inhibitors of the HIV-1 protease: synthesis, potency, resistance profile, human pharmacokinetics and X-ray crystal structure of DMP 450 [O] . Hodge C. Nicholas, Aldrich Paul E., Bacheler Lee T., 1996

机译：改进的HIV-1蛋白酶环状脲抑制剂：DMP 450的合成，效价，耐药性，人药代动力学和X射线晶体结构

Indinavir analogues with blocked metabolism sites as HIV protease inhibitors with improved pharmacological profiles and high potency against PI-Resistant viral strains.

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