Design and synthesis of HIV-1 protease inhibitors for a long-acting injectable drug application

B Kesteleyn, K Amssoms, W Schepens, G Hache…

文献索引：Kesteleyn, Bart; Amssoms, Katie; Schepens, Wim; Hache, Geerwin; Verschueren, Wim; Van De Vreken, Wim; Rombauts, Klara; Meurs, Greet; Sterkens, Patrick; Stoops, Bart; Baert, Lieven; Austin, Nigel; Wegner, Joerg; Masungi, Chantal; Dierynck, Inge; Lundgren, Stina; Joensson, Daniel; Parkes, Kevin; Kalayanov, Genadiy; Wallberg, Hans; Rosenquist, Asa; Samuelsson, Bertil; Van Emelen, Kristof; Thuring, Jan Willem Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 1 p. 310 - 317

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被引用次数: 4

摘要

The design and synthesis of novel HIV-1 protease inhibitors (PIs)(1–22), which display high potency against HIV-1 wild-type and multi-PI-resistant HIV-mutant clinical isolates, is described. Lead optimization was initiated from compound 1, a Phe–Phe hydroxyethylene peptidomimetic PI, and was directed towards the discovery of new PIs suitable for a long- acting (LA) injectable drug application. Introducing a heterocyclic 6-methoxy-3-pyridinyl or ...