Discovery of low‐molecular‐weight phenylalanine derivatives as novel HIV capsid modulators with improved antiretroviral activity and metabolic stability
Xiangyi Jiang,
Zhen Gao,
Prem Prakash Sharma
et al.
Abstract:The HIV capsid (CA) protein is a promising target for anti‐AIDS treatment due to its critical involvement in viral replication. Herein, we utilized the well‐documented CA inhibitor PF74 as our lead compound and designed a series of low‐molecular‐weight phenylalanine derivatives. Among them, compound 7t exhibited remarkable antiviral activity with a high selection index (EC50 = 0.040 µM, SI = 2815), surpassing that of PF74 (EC50 = 0.50 µM, SI = 258). Furthermore, when evaluated against the HIV‐2 strain, 7t (EC5… Show more
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