HIV-1 protease inhibitors with a P1 phosphonate modification maintain potency against drug-resistant variants by increased interactions with flap residues

GJ Lockbaum, LN Rusere, M Henes… - European Journal of …, 2023 - Elsevier
Protease inhibitors are the most potent antivirals against HIV-1, but they still lose efficacy
against resistant variants. Improving the resistance profile is key to developing more robust …

Design and synthesis of highly potent HIV-1 protease inhibitors containing tricyclic fused ring systems as novel P2 ligands: structure–activity studies, biological and x …

AK Ghosh, P R. Nyalapatla, S Kovela… - Journal of medicinal …, 2018 - ACS Publications
The design, synthesis, and biological evaluation of a new class of HIV-1 protease inhibitors
containing stereochemically defined fused tricyclic polyethers as the P2 ligands and a …

Design and synthesis of potent HIV-1 protease inhibitors containing bicyclic oxazolidinone scaffold as the P2 ligands: Structure–activity studies and biological and X …

AK Ghosh, JN Williams, RY Ho… - Journal of medicinal …, 2018 - ACS Publications
We have designed, synthesized, and evaluated a new class of potent HIV-1 protease
inhibitors with novel bicyclic oxazolidinone derivatives as the P2 ligand. We have developed …

Metal‐Free Synthesis of 2‐Aminobenzothiazoles via I2‐Catalyzed Tandem Cyclization Reaction of Amines and Carbon Disulfide

T Chen, W Feng, R Yang, S Chen… - Chinese Journal of …, 2024 - Wiley Online Library
Comprehensive Summary A convenient approach for the construction of 2‐
aminobenzothiazoles via I2‐catalyzed tandem cyclization reaction of amines and carbon …

Iodine-catalyzed amination of benzothiazoles with KSeCN in water to access primary 2-aminobenzothiazoles

YS Zhu, L Shi, L Fu, X Chen, X Zhu, XQ Hao… - Chinese Chemical …, 2022 - Elsevier
A facile and sustainable approach for the amination of benzothiazoles with KSeCN using
iodine as the catalyst in water has been disclosed under transition-metal free conditions …

HIV-1 protease inhibitors incorporating stereochemically defined P2′ ligands to optimize hydrogen bonding in the substrate envelope

LN Rusere, GJ Lockbaum, SK Lee… - Journal of medicinal …, 2019 - ACS Publications
A structure-guided design strategy was used to improve the resistance profile of HIV-1
protease inhibitors by optimizing hydrogen bonding and van der Waals interactions with the …

A green aerobic Fe (lll) catalyzed base-free synthesis of 2-aminobenzothiazoles in water

S Radhika, MB Aleena, G Anilkumar - Journal of Catalysis, 2022 - Elsevier
An Fe (III) catalyzed, efficient methodology for the synthesis of 2-aminobenzothiazole
derivatives in water was established. This mild, base-free, one-pot strategy showcases the …

Structure-based design of highly potent HIV-1 protease inhibitors containing new tricyclic ring P2-ligands: design, synthesis, biological, and X-ray structural studies

AK Ghosh, S Kovela, HL Osswald… - Journal of medicinal …, 2020 - ACS Publications
We describe here design, synthesis, and biological evaluation of a series of highly potent
HIV-1 protease inhibitors containing stereochemically defined and unprecedented tricyclic …

Preliminary SAR and biological evaluation of potent HIV-1 protease inhibitors with pyrimidine bases as novel P2 ligands to enhance activity against DRV-resistant HIV …

M Zhu, L Ma, H Zhou, B Dong, Y Wang, Z Wang… - European Journal of …, 2020 - Elsevier
Introducing pyrimidine bases, the basic components of nucleic acid, to P2 ligands might
enhance the potency of Human Immunodeficiency Virus-1 (HIV-1) protease inhibitors …

Design and biological evaluation of cinnamic and phenylpropionic amide derivatives as novel dual inhibitors of HIV-1 protease and reverse transcriptase

M Zhu, Q Shan, L Ma, J Wen, B Dong, G Zhang… - European journal of …, 2021 - Elsevier
Upon the basis of both possible ligand-binding site interactions and the uniformity of key
residues in active sites, a novel class of HIV-1 PR/RT dual inhibitors was designed and …