Falcipain-2 and falcipain-3 inhibitors as promising antimalarial agents

R Ettari, S Previti, C Di Chio… - Current Medicinal …, 2021 - ingentaconnect.com
Malaria remains a serious problem in global public health, particularly widespread in South
America and in tropical regions of Africa and Asia. Chemotherapy is actually the only way to …

Design, Synthesis and Preliminary Screening of Some New Conformationally Constrained Falcipain-2 Inhibitors as Potential Antimalarial Agents

AK Shinde, BS Chouhan, S Dasgupta… - Letters in Drug …, 2009 - ingentaconnect.com
Increasing resistance of malaria parasites, P. falciparum in particular, towards existing
antimalarial drugs demands a serious search for novel targets for the development of new …

DESIGN, SYNTHESIS AND BIOLOGICAL EVALUATION OF PEPTIDOMIMETIC FALCIPAIN-2 INHIBITORS AS ANTIMALARIAL AGENTS

N Micale, R Ettari, T Schirmeister, G Grazioso… - Nuove Prospettive in …, 2012 - iris.unime.it
Malaria is currently endemic in 106 countries, with an estimated 216 million clinical cases
and nearly 655000 deaths in 2010 [1]. Five species of a parasite of Plasmodium genus are …

Synthetic compounds from an in house library as inhibitors of falcipain-2 from Plasmodium falciparum

JB Bertoldo, LD Chiaradia-Delatorre… - Journal of Enzyme …, 2015 - Taylor & Francis
Abstract Falcipain-2 (FP-2) is a key cysteine protease from the malaria parasite Plasmodium
falciparum. Many previous studies have identified FP-2 inhibitors; however, none has yet …

Identification of novel class of falcipain-2 inhibitors as potential antimalarial agents

SK Chakka, M Kalamuddin, S Sundararaman… - Bioorganic & medicinal …, 2015 - Elsevier
Falcipain-2 is a papain family cysteine protease and an emerging antimalarial drug target. A
pseudo-tripeptide scaffold I was designed using in silico screening tools and the three …

Design, synthesis and biological evaluation of novel benzothiazole and triazole analogs as falcipain inhibitors

F Shah, Y Wu, J Gut, Y Pedduri, J Legac… - …, 2011 - pubs.rsc.org
We describe the design, combinatorial library synthesis and biological evaluation of
compounds with benzothiazole and triazole cores as inhibitors of falcipain, cysteine …

Development of peptidomimetics with a vinyl sulfone warhead as irreversible falcipain-2 inhibitors

R Ettari, E Nizi, ME Di Francesco… - Journal of medicinal …, 2008 - ACS Publications
This paper describes the synthesis of a new class of peptidomimetic cysteine protease
inhibitors based on a 1, 4-benzodiazepine scaffold and on an electrophilic vinyl sulfone …

Falcipain‐2 inhibitors

R Ettari, F Bova, M Zappalà, S Grasso… - Medicinal research …, 2010 - Wiley Online Library
Malaria, particularly that one caused by Plasmodium falciparum, remains a serious health
problem in Africa, South America, and many parts of Asia where it afflicts about 500 million …

Antimalarial effects in mice of orally administered peptidyl cysteine protease inhibitors

JE Olson, GK Lee, A Semenov, PJ Rosenthal - Bioorganic & medicinal …, 1999 - Elsevier
The Plasmodium falciparum cysteine protease falcipain is required for the degradation of
hemoglobin by erythrocytic malaria parasites. In prior studies, peptidyl inhibitors of falcipain …

A Prodomain Peptide of Plasmodium falciparum Cysteine Protease (Falcipain-2) Inhibits Malaria Parasite Development

R Korde, A Bhardwaj, R Singh… - Journal of medicinal …, 2008 - ACS Publications
Falcipain-2 (FP-2), a papain family cysteine protease of Plasmodium falciparum, is a
promising target for antimalarial chemotherapy. Designing inhibitors that are highly selective …