Design of Highly Potent, Dual‐Acting and Central‐Nervous‐System‐Penetrating HIV‐1 Protease Inhibitors with Excellent Potency against Multidrug‐Resistant HIV‐1 Variants - Ghosh, Arun K.; Rao, Kalapala Venkateswara; Nyalapatla, Prasanth R.; Kovela, Satish; Brindisi, Margherita; Osswald, Heather L.; Sekhara Reddy, Bhavanam; Agniswamy, Johnson; Wang, Yuan‐Fang; Aoki, Manabu; Hattori, Shin‐ichiro; Weber, Irene T.; et al. (ChemMedChem, 2018)
Keywords: Animals; antiviral agents; BASIC BIOLOGICAL SCIENCES; Brain - metabolism; brain penetration; Carbamates - chemistry; Carbamates - pharmacokinetics; Carbamates - pharmacology; Cell Line; Central nervous system; Chemistry, Medicinal; Crystal structure; Crystallography, X-Ray; Design; Dimerization; Drug Design; Drug resistance; Halogenation; HIV; HIV Infections - drug therapy; HIV Infections - virology; HIV Protease - chemistry; HIV Protease - metabolism; HIV Protease Inhibitors - chemistry; HIV Protease Inhibitors - pharmacokinetics; HIV Protease Inhibitors - pharmacology; HIV-1 - chemistry; HIV-1 - drug effects; HIV-1 - enzymology; HIV-1 protease; Human immunodeficiency virus; Humans; Life Sciences & Biomedicine; Ligands; Models, Molecular; Multidrug resistant organisms; Penetration resistance; Pharmacology & Pharmacy; Protease; Protease inhibitors; Proteinase inhibitors; Rats; Science & Technology; structure-based design; DIMERIZATION INHIBITION; DARUNAVIR; CCP4 SUITE; antiviral agents; brain penetration; COMPLEXES; DRUG-RESISTANCE; structure-based design; IN-VITRO; RESOLUTION CRYSTAL-STRUCTURES; REPLICATION; ASYMMETRIC EPOXIDATION; FLUORINE; drug resistance; HIV-1 protease