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 …

Highly resistant HIV-1 proteases and strategies for their inhibition

IT Weber, DW Kneller, A Wong-Sam - Future medicinal chemistry, 2015 - Taylor & Francis
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 …

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 …

Phosphine-catalyzed divergent domino processes between γ-substituted allenoates and carbonyl-activated alkenes

M Wu, Z Han, H Ni, N Wang, K Ding, Y Lu - Chemical Science, 2022 - pubs.rsc.org
Highly enantioselective and chemodivergent domino reactions between γ-substituted
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 …

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 …

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 …

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 …

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 …

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 …