Chemotherapy for human schistosomiasis: how far have we come? What's new? Where do we go from here?

GA Dziwornu, HD Attram, S Gachuhi… - RSC Medicinal …, 2020 - pubs.rsc.org
Globally, schistosomiasis threatens more than 700 million lives, mostly children, in poor
localities of tropical and sub-tropical areas with morbidity due to acute and chronic …

Simple inorganic base promoted polycyclic construction using mucohalic acid as a C 3 synthon: synthesis and AIE probe application of benzo [4, 5] imidazo [1, 2-a] …

K Yang, ZX Chen, YJ Zhou, Q Chen, SW Yu… - Organic Chemistry …, 2022 - pubs.rsc.org
A transition metal-free and efficient synthesis of fused azapolycycles via a multicomponent
reaction has been developed using mucohalic acid as a C3 synthon. The reaction promoted …

Improving translational power in antischistosomal drug discovery

A Probst, S Biendl, J Keiser - Advances in parasitology, 2022 - Elsevier
Schistosomiasis is a poverty-associated tropical disease caused by blood dwelling
trematodes that threaten approximately 10% of the world population. Praziquantel, the sole …

Antimalarial Pyrido[1,2-a]benzimidazole Derivatives with Mannich Base Side Chains: Synthesis, Pharmacological Evaluation, and Reactive Metabolite Trapping …

J Okombo, C Brunschwig, K Singh… - ACS infectious …, 2019 - ACS Publications
A novel series of pyrido [1, 2-a] benzimidazoles bearing Mannich base side chains and their
metabolites were synthesized and evaluated for in vitro antiplasmodium activity, microsomal …

Simple inorganic base promoted C–N and C–C formation: synthesis of benzo [4, 5] imidazo [1, 2-a] pyridines as functional AIEgens used for detecting picric acid

K Yang, SH Luo, SH Chen, XY Cao, YJ Zhou… - Organic & …, 2021 - pubs.rsc.org
Metal-free catalyzed intermolecular tandem Michael addition/cyclization has been
developed for the synthesis of benzo [4, 5] imidazo [1, 2-a] pyridines from α …

Drug discovery and development for schistosomiasis

CR Caffrey, N El‐Sakkary, P Mäder… - … : drug discovery and …, 2019 - Wiley Online Library
Schistosomiasis is a neglected disease of poverty that is caused by several species of the
trematode flatworm, Schistosoma. Treatment relies on just one drug, the …

Expanding the activity profile of pyrido [1, 2-a] benzimidazoles: Synthesis and evaluation of novel N 1-1-phenylethanamine derivatives against Schistosoma mansoni

A Probst, K Chisanga, GA Dziwornu… - ACS infectious …, 2020 - ACS Publications
Praziquantel is the only widely available drug to treat schistosomiasis. With very few
candidates currently in the drug development pipeline, there is an urgent need to discover …

Structure–Activity Relationship and in Vitro Absorption, Distribution, Metabolism, Excretion, and Toxicity (ADMET) Studies of N-aryl 3-Trifluoromethyl Pyrido[1,2-a] …

G Mayoka, J Keiser, C Haberli… - ACS infectious …, 2018 - ACS Publications
We have previously reported on the antischistosomal activity of pyrido [1, 2-a] benzimidazole
(PBI) derivatives. As a follow-up, we designed and prosecuted further structure–activity …

[HTML][HTML] Benzimidazole analogues active against adult Schistosoma mansoni: SAR analyses, In vivo efficacy in mice, and preliminary mechanistic studies as potential …

GA Dziwornu, HD Attram, C Haeberli, K Masike… - European Journal of …, 2025 - Elsevier
For over three decades, praziquantel (PZQ) has been the mainstay chemotherapy for
prevention and treatment of schistosomiasis. The excessive use of PZQ, coupled with the …

Dealing with schistosomiasis: Current drug discovery strategies

S Gemma, S Federico, S Brogi, M Brindisi… - Annual Reports in …, 2019 - Elsevier
Schistosomiasis is one of the most prevalent parasitic diseases, accounting for heavy
socioeconomical and health burden in endemic countries. The control of this neglected …