Synthesis and structure-activity relationship studies of cruzain and rhodesain inhibitors

DA Rocha, EB Silva, IS Fortes, MS Lopes… - European Journal of …, 2018 - Elsevier
Abstract Chagas disease and Human African trypanosomiasis (HAT) are important public
health issues in Latin American and sub-Saharan African countries, respectively, and are …

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 …

Covalent inhibition by a natural product-inspired latent electrophile

DP Byun, J Ritchie, Y Jung, R Holewinski… - Journal of the …, 2023 - ACS Publications
Strategies to target specific protein cysteines are critical to covalent probe and drug
discovery. 3-Bromo-4, 5-dihydroisoxazole (BDHI) is a natural product-inspired, synthetically …

Development of novel peptide-based Michael acceptors targeting rhodesain and falcipain-2 for the treatment of Neglected Tropical Diseases (NTDs)

S Previti, R Ettari, S Cosconati… - Journal of Medicinal …, 2017 - ACS Publications
This paper describes the development of a class of peptide-based inhibitors as novel
antitrypanosomal and antimalarial agents. The inhibitors are based on a characteristic …

Development of Urea-Bond-Containing Michael Acceptors as Antitrypanosomal Agents Targeting Rhodesain

S Previti, R Ettari, E Calcaterra, C Di Chio… - ACS Medicinal …, 2022 - ACS Publications
Human African Trypanosomiasis (HAT) is a neglected tropical disease widespread in sub-
Saharan Africa. Rhodesain, a cysteine protease of Trypanosoma brucei rhodesiense, has …

Development of novel dipeptide nitriles as inhibitors of rhodesain of Trypanosoma brucei rhodesiense

C Di Chio, S Previti, G Amendola… - European Journal of …, 2022 - Elsevier
In this paper, we developed a new series of dipeptide nitriles that were demonstrated to be
reversible rhodesain inhibitors at nanomolar level, with EC 50 values against cultured T. b …

Discovery of covalent inhibitors of glyceraldehyde-3-phosphate dehydrogenase, a target for the treatment of malaria

S Bruno, A Pinto, G Paredi, L Tamborini… - Journal of Medicinal …, 2014 - ACS Publications
We developed a new class of covalent inhibitors of Plasmodium falciparum glyceraldehyde-
3-phosphate dehydrogenase, a validated target for the treatment of malaria, by screening a …

Optimization strategy of novel peptide-based Michael acceptors for the treatment of Human African Trypanosomiasis

R Ettari, S Previti, S Maiorana… - Journal of Medicinal …, 2019 - ACS Publications
This paper describes an optimization strategy of the highly active vinyl ketone 3 which was
recognized as a strong inhibitor of rhodesain of Trypanosoma brucei rhodesiense, endowed …

The inhibition of cysteine proteases rhodesain and TbCatB: A valuable approach to treat Human African Trypanosomiasis

R Ettari, S Previti, L Tamborini, G Cullia… - Mini reviews in …, 2016 - ingentaconnect.com
Human African Trypanosomiasis (HAT) is an endemic parasitic disease of sub-Saharan
Africa, caused by two subspecies of protozoa belonging to Trypanosoma genus: T. brucei …