Integrated approach to structure-based enzymatic drug design: molecular modeling, spectroscopy, and experimental bioactivity

B Honarparvar, T Govender, GEM Maguire… - Chemical …, 2014 - ACS Publications
Analysis of the literature involving computational modeling of diseases and drug design with
the aid of experimental spectroscopic techniques reveals that this specific combination of …

Novel series of benzo [d] thiazolyl substituted-2-quinolone hybrids: Design, synthesis, biological evaluation and in-silico insights

G Bolakatti, M Palkar, M Katagi, G Hampannavar… - Journal of Molecular …, 2021 - Elsevier
Abstract A novel series of 3-(2-(4-(substituted-benzo [d] thiazol-2-yl) phenylamino) acetyl)-4‑
hydroxy-1-methyl/phenyl quinolin-2 (1H)-one (7a-f and 8a-f) were synthesized. Reaction of …

Binding free energy calculations of nine FDA‐approved protease inhibitors against HIV‐1 subtype C I36T↑ T containing 100 amino acids per monomer

HA Lockhat, JRA Silva, CN Alves… - Chemical biology & …, 2016 - Wiley Online Library
In this work, have investigated the binding affinities of nine FDA‐approved protease inhibitor
drugs against a new HIV‐1 subtype C mutated protease, I36T↑ T. Without an X‐ray crystal …

Comparison of the molecular dynamics and calculated binding free energies for nine FDA‐approved HIV‐1 PR drugs against subtype B and C‐SA HIV PR

SM Ahmed, HG Kruger, T Govender… - Chemical biology & …, 2013 - Wiley Online Library
We report the first account of a comparative analysis of the binding affinities of nine FDA‐
approved drugs against subtype B as well as the South African subtype C HIV PR (C‐SA). A …

Pentacycloundecane lactam vs lactone norstatine type protease HIV inhibitors: binding energy calculations and DFT study

B Honarparvar, SA Pawar, CN Alves, J Lameira… - Journal of Biomedical …, 2015 - Springer
Background Novel pentacycloundecane (PCU)-lactone-CO-EAIS peptide inhibitors were
designed, synthesized, and evaluated against wild-type C-South African (C-SA) HIV-1 …

Identification of binding mode and prospective structural features of novel Nef protein inhibitors as potential anti-HIV drugs

S Moonsamy, S Bhakat, M Ramesh… - Cell biochemistry and …, 2017 - Springer
Human immunodeficiency virus (HIV)-negative factor (Nef) protein is an accessory
pathogenic factor, which plays a significant role in acquired immune deficiency syndrome …

Identification of irreversible protein splicing inhibitors as potential anti-TB drugs: insight from hybrid non-covalent/covalent docking virtual screening and molecular …

L Blake, MES Soliman - Medicinal Chemistry Research, 2014 - Springer
Tuberculosis is responsible for~ 3 million deaths annually and is one of the most prevalent
infectious diseases known to mankind. Despite ongoing developments in medicine, the …

Investigation of the binding free energies of FDA approved drugs against subtype B and C-SA HIV PR: ONIOM approach

ZK Sanusi, T Govender, GEM Maguire… - Journal of Molecular …, 2017 - Elsevier
Human immune virus subtype C is the most widely spread HIV subtype in Sub-Sahara Africa
and South Africa. A profound structural insight on finding potential lead compounds is …

An insight to the molecular interactions of the FDA approved HIV PR drugs against L38L↑ N↑ L PR mutant

ZK Sanusi, T Govender, GEM Maguire… - Journal of Computer …, 2018 - Springer
The aspartate protease of the human immune deficiency type-1 virus (HIV-1) has become a
crucial antiviral target in which many useful antiretroviral inhibitors have been developed …

Pentacycloundecane‐diol‐Based HIV‐1 Protease Inhibitors: Biological Screening, 2D NMR, and Molecular Simulation Studies

B Honarparvar, MM Makatini, SA Pawar… - …, 2012 - Wiley Online Library
Novel compounds incorporating a pentacycloundecane (PCU) diol moiety were designed,
synthesized, and evaluated as inhibitors of the wild‐type C‐South African (C‐SA) HIV‐1 …