Geminal diheteroatomic motifs: some applications of acetals, ketals, and their sulfur and nitrogen homologues in medicinal chemistry and drug design
YJ Wu, NA Meanwell - Journal of Medicinal Chemistry, 2021 - ACS Publications
Acetals and ketals and their nitrogen and sulfur homologues are often considered to be
unconventional and potentially problematic scaffolding elements or pharmacophores for the …
unconventional and potentially problematic scaffolding elements or pharmacophores for the …
Highly resistant HIV-1 proteases and strategies for their inhibition
The virally encoded protease is an important drug target for AIDS therapy. Despite the
potency of the current drugs, infections with resistant viral strains limit the long-term …
potency of the current drugs, infections with resistant viral strains limit the long-term …
Beyond Members of the Flaviviridae Family, Sofosbuvir Also Inhibits Chikungunya Virus Replication
AC Ferreira, PA Reis, CS de Freitas… - Antimicrobial agents …, 2019 - Am Soc Microbiol
Chikungunya virus (CHIKV) causes a febrile disease associated with chronic arthralgia,
which may progress to neurological impairment. Chikungunya fever (CF) is an ongoing …
which may progress to neurological impairment. Chikungunya fever (CF) is an ongoing …
Phosphine-catalyzed divergent domino processes between γ-substituted allenoates and carbonyl-activated alkenes
Highly enantioselective and chemodivergent domino reactions between γ-substituted
allenoates and activated alkenes have been developed. In the presence of NUSIOC-Phos …
allenoates and activated alkenes have been developed. In the presence of NUSIOC-Phos …
Joint X-ray/neutron crystallographic study of HIV-1 protease with clinical inhibitor amprenavir: insights for drug design
IT Weber, MJ Waltman, M Mustyakimov… - Journal of medicinal …, 2013 - ACS Publications
HIV-1 protease is an important target for the development of antiviral inhibitors to treat AIDS.
A room-temperature joint X-ray/neutron structure of the protease in complex with clinical …
A room-temperature joint X-ray/neutron structure of the protease in complex with clinical …
Highly Potent HIV-1 Protease Inhibitors with Novel Tricyclic P2 Ligands: Design, Synthesis, and Protein–Ligand X-ray Studies
AK Ghosh, GL Parham, CD Martyr… - Journal of medicinal …, 2013 - ACS Publications
The design, synthesis, and biological evaluation of a series of HIV-1 protease inhibitors
incorporating stereochemically defined fused tricyclic P2 ligands are described. Various …
incorporating stereochemically defined fused tricyclic P2 ligands are described. Various …
Aureonitol, a fungi-derived tetrahydrofuran, inhibits influenza replication by targeting its surface glycoprotein hemagglutinin
CQ Sacramento, A Marttorelli, N Fintelman-Rodrigues… - PLoS …, 2015 - journals.plos.org
The influenza virus causes acute respiratory infections, leading to high morbidity and
mortality in groups of patients at higher risk. Antiviral drugs represent the first line of defense …
mortality in groups of patients at higher risk. Antiviral drugs represent the first line of defense …
Computational studies of a mechanism for binding and drug resistance in the wild type and four mutations of HIV-1 protease with a GRL-0519 inhibitor
G Hu, A Ma, X Dou, L Zhao, J Wang - International journal of molecular …, 2016 - mdpi.com
Drug resistance of mutations in HIV-1 protease (PR) is the most severe challenge to the long-
term efficacy of HIV-1 PR inhibitor in highly active antiretroviral therapy. To elucidate the …
term efficacy of HIV-1 PR inhibitor in highly active antiretroviral therapy. To elucidate the …
Drug resistance mutation L76V alters nonpolar interactions at the flap–core interface of HIV-1 protease
A Wong-Sam, YF Wang, Y Zhang, AK Ghosh… - Acs Omega, 2018 - ACS Publications
Four HIV-1 protease (PR) inhibitors, clinical inhibitors lopinavir and tipranavir, and two
investigational compounds 4 and 5, were studied for their effect on the structure and activity …
investigational compounds 4 and 5, were studied for their effect on the structure and activity …
Extreme multidrug resistant HIV-1 protease with 20 mutations is resistant to novel protease inhibitors with P1′-pyrrolidinone or P2-tris-tetrahydrofuran
J Agniswamy, CH Shen, YF Wang… - Journal of medicinal …, 2013 - ACS Publications
Extreme drug resistant mutant of HIV-1 protease (PR) bearing 20 mutations (PR20) has
been studied with the clinical inhibitor amprenavir (1) and two potent antiviral investigational …
been studied with the clinical inhibitor amprenavir (1) and two potent antiviral investigational …