[HTML][HTML] Thienopyrimidine: A promising Scaffold to access anti-infective agents

P Lagardère, C Fersing, N Masurier, V Lisowski - Pharmaceuticals, 2021 - mdpi.com
Thienopyrimidines are widely represented in the literature, mainly due to their structural
relationship with purine base such as adenine and guanine. This current review presents …

[HTML][HTML] Cysteine proteases: Battling pathogenic parasitic protozoans with omnipresent enzymes

A Rawat, M Roy, A Jyoti, S Kaushik, K Verma… - Microbiological …, 2021 - Elsevier
Millions of people worldwide lie at the risk of parasitic protozoic infections that kill over a
million people each year. The rising inefficacy of conventional therapeutics to combat these …

QSAR, simulation techniques, and ADMET/pharmacokinetics assessment of a set of compounds that target MAO-B as anti-Alzheimer agent

A Ajala, A Uzairu, GA Shallangwa… - Future Journal of …, 2023 - Springer
Background Alzheimer's disease (AD), the most common cause of dementia in the elderly, is
a progressive neurodegenerative disorder that gradually affects cognitive function and …

Antimalarial activity of flavonoid compound isolated from leaves of Artocarpus altilis

AR Hidayati, A Widyawaruyanti, H Ilmi… - Pharmacognosy …, 2020 - phcogj.com
Introduction: Artocarpus altilis leaves extract has previously been reported as a potential
antimalarial drug. Inhibition concentration (IC 50) against P. falciparum and effective dose …

In silico Guided Drug Repurposing: Discovery of New Competitive and Non-competitive Inhibitors of Falcipain-2

LN Alberca, SR Chuguransky, CL Álvarez… - Frontiers in …, 2019 - frontiersin.org
Malaria is among the leading causes of death worldwide. The emergence of Plasmodium
falciparum resistant strains with reduced sensitivity to the first line combination therapy and …

[HTML][HTML] Investigation of some plant stilbenoids and their fragments for the identification of inhibitors of SARS-CoV-2 viral spike/ACE2 protein binding

CT Namba-Nzanguim, CV Simoben, BD Bekono… - The Microbe, 2024 - Elsevier
In silico binding studies were conducted on the known plant-derived polyphenolic tetrameric
stilbenoids,(–)-hopeaphenol (1), vaticanol B (2) and vatalbinoside A (3) and their monomeric …

Tetracycline derivatives inhibit plasmodial cysteine protease falcipain-2 through binding to a distal allosteric site

JE Hernandez Gonzalez, LN Alberca… - Journal of Chemical …, 2021 - ACS Publications
Allosteric inhibitors regulate enzyme activity from remote and usually specific pockets. As
they promise an avenue for less toxic and safer drugs, the identification and characterization …

[HTML][HTML] Three Decades of Targeting Falcipains to Develop Antiplasmodial Agents: What have we Learned and What can be Done Next?

J González, E Salas-Sarduy, L Alvarez… - Current Medicinal …, 2024 - freezetech.ru
Malaria is a devastating infectious disease that affects large swathes of human populations
across the planet s tropical regions. It is caused by parasites of the genus Plasmodium, with …

Virtual design of novel Plasmodium falciparum cysteine protease falcipain-2 hybrid lactone–chalcone and isatin–chalcone inhibitors probing the S2 active site pocket

KNGPG Allangba, M Keita… - Journal of Enzyme …, 2019 - Taylor & Francis
We report computer-aided design of new lactone–chalcone and isatin–chalcone (HLCIC)
inhibitors of the falcipain-2 (Pf FP-2). 3D models of 15 FP-2: HLCIC1-15 complexes with …

In Vitro Antiplasmodium and Chloroquine Resistance Reversal Effects of Andrographolide

ZO Ibraheem, RA Majid, HM Sidek… - Evidence‐Based …, 2019 - Wiley Online Library
The emergence of drug‐resistant strains of Plasmodium falciparum is the worst catastrophe
that has ever confronted the dedicated efforts to eradicate malaria. This urged for searching …