Synthesis and SAR Studies of New Oxadiazole-2-oxide Derivatives with Remarkable In Vitro Activity against Schistosoma japonicum

M, C M A Gause; F, Wen Hua; S, Li Jun; Y, Chuan Xin; Feng, Bo

doi:10.4172/1948-5948.1000339

Cited by 2 publications

(1 citation statement)

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“…This is mainly due to the implementation of higher complexity screening assays, and to other factors such as the parallel use of genetic and small molecules screens, as well as more complicated hit validation and target identification efforts (48). Furthermore, the establishment of structure-activity relationship (SAR) is more challenging due to other concurrent factors, such as membrane permeability and off-target binding, though there are several examples of successful SAR studies using schistosome phenotypic assays in the literature (49)(50)(51). Hence, PDD approach is limited in this sense due to unknown mechanism of action, potentially targeting different types of proteins, such as receptors, enzymes, transcription factors and even different signaling pathways (45).…”

Section: Phenotypic Screeningmentioning

confidence: 99%

Schistosomiasis Drug Discovery in the Era of Automation and Artificial Intelligence

et al. 2021

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Schistosomiasis is a parasitic disease caused by trematode worms of the genus Schistosoma and affects over 200 million people worldwide. The control and treatment of this neglected tropical disease is based on a single drug, praziquantel, which raises concerns about the development of drug resistance. This, and the lack of efficacy of praziquantel against juvenile worms, highlights the urgency for new antischistosomal therapies. In this review we focus on innovative approaches to the identification of antischistosomal drug candidates, including the use of automated assays, fragment-based screening, computer-aided and artificial intelligence-based computational methods. We highlight the current developments that may contribute to optimizing research outputs and lead to more effective drugs for this highly prevalent disease, in a more cost-effective drug discovery endeavor.

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