Antiprotozoal Drugs

Thurston, Scott; Hite, Gary L.; Petry, Alyssa N.; Ray, Sidhartha D.

doi:10.1016/bs.seda.2015.08.008

Cited by 8 publications

(3 citation statements)

References 19 publications

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“…Nitazoxanide is FDA-approved and licensed to treat cryptosporidial diarrhea and other intestinal parasitic infections [53]. This thiazolide agent interferes with the electron transfer reaction in anaerobic metabolism and has been found to both inhibit Ebolavirus growth and increase the host antiviral response [54,55]. Griffin et al [56] found that the benzimidazole histamine H1 antagonist, clemizole, acts as an antiepileptic and speculate that it could be used to treat Dravet syndrome based on their study in zebrafish.…”

Section: Discussionmentioning

confidence: 99%

Discovery of Anti-Amoebic Inhibitors from Screening the MMV Pandemic Response Box on Balamuthia mandrillaris, Naegleria fowleri, and Acanthamoeba castellanii

et al. 2020

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Pathogenic free-living amoebae, Balamuthia mandrillaris, Naegleria fowleri, and several Acanthamoeba species are the etiological agents of severe brain diseases, with case mortality rates > 90%. A number of constraints including misdiagnosis and partially effective treatments lead to these high fatality rates. The unmet medical need is for rapidly acting, highly potent new drugs to reduce these alarming mortality rates. Herein, we report the discovery of new drugs as potential anti-amoebic agents. We used the CellTiter-Glo 2.0 high-throughput screening methods to screen the Medicines for Malaria Ventures (MMV) Pandemic Response Box in a search for new active chemical scaffolds. Initially, we screened the library as a single-point assay at 10 and 1 µM. From these data, we reconfirmed hits by conducting quantitative dose–response assays and identified 12 hits against B. mandrillaris, 29 against N. fowleri, and 14 against A. castellanii ranging from nanomolar to low micromolar potency. We further describe 11 novel molecules with activity against B. mandrillaris, 22 against N. fowleri, and 9 against A. castellanii. These structures serve as a starting point for medicinal chemistry studies and demonstrate the utility of phenotypic screening for drug discovery to treat diseases caused by free-living amoebae.

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Section: Discussionmentioning

confidence: 99%

Discovery of Anti-Amoebic Inhibitors from Screening the MMV Pandemic Response Box on Balamuthia mandrillaris, Naegleria fowleri, and Acanthamoeba castellanii

et al. 2020

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“…Other drugs can produce enzymatic inhibition, for example trimethoprim-sulfamethoxazole, which is used to inhibit folic acid synthesis in Pneumocystis carinii. However, the chemotherapy for protozoal infections causes adverse effects during therapeutic doses that limit their safety use where combined therapies are considered too ( Thurston et al, 2015 ). At least nine species from Calosphace have been investigated as potential options for antiprotozoal therapy the 5,6-dihydroxy-7,3′,4′-trimethoxyflavone was isolated from acetone extract and ethyl acetate fraction of S. amarissima Ortega and proved to be effective against E. histolytica , IC 50 = 0.05 μg/ml and G. lamblia , IC 50 = 0.13 μg/ml ( Calzada and Bautista, 2020 ).…”

Section: Resultsmentioning

confidence: 99%

A Review on the Ethnopharmacology and Phytochemistry of the Neotropical Sages (Salvia Subgenus Calosphace; Lamiaceae) Emphasizing Mexican Species

et al. 2022

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Salvia is the most diverse genus within the mint family (Lamiaceae), many of its species are well-known due to their medicinal and culinary uses. Most of the ethnopharmacological and phytochemical studies on Salvia are centred on species from the European and Asian clades. However, studies about the most diverse clade, the Neotropical sages (Salvia subgenus Calosphace; 587 spp.), are relatively scarce. This review aims to compile the information on the traditional medicinal uses, pharmacological and phytochemistry properties of the Neotropical sages. To do so, we carried out a comprehensive review of the articles available in different online databases published from the past to 2022 (i.e., PubMed, Scopus, and Web of Science, among others) and summarized the information in tables. To uncover phylogenetic patterns in the distribution of four different groups of metabolites (mono-, sesqui-, di-, and triterpenes), we generated presence-absence matrices and plotted the tip states over a dated phylogeny of Salvia. We found several studies involving Mexican species of Salvia, but only a few about taxa from other diversity centres. The main traditional uses of the Mexican species of Calosphace are medicinal and ceremonial. In traditional medicine 56 species are used to treat diseases from 17 categories according to the WHO, plus cultural-bound syndromes. Pharmacological studies reveal a wide range of biological properties (e.g., antinociceptive, anti-inflammatory, anxiolytic, cytotoxic, and antidiabetic, etc.) found in extracts and isolated compounds of 38 Neotropical sages. From extracts of these species, at least 109 compounds have been isolated, identified and evaluated pharmacologically; 73 of these compounds are clerodanes, 21 abietanes, six flavonoids, five sesquiterpenoids, and four triterpenoids. The most characteristic metabolites found in the Neotropical sages are the diterpenes, particularly clerodanes (e.g., Amarisolide A, Tilifodiolide), that are found almost exclusively in this group. The Neotropical sages are a promising resource in the production of herbal medication, but studies that corroborate the properties that have been attributed to them in traditional medicine are scarce. Research of these metabolites guided by the phylogenies is recommended, since closely related species tend to share the presence of similar compounds and thus similar medicinal properties.

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“…It does affect more than 500 million people all around the world. 50 The lack of effective antiprotozoal and drug resistance encouraged researchers to search for new drugs against protozoan parasites. 51 Following a Gewald synthesis, De Lima Serafim et al described in 2018 the synthesis of 2-ATs (6, 7a-g) whose synthesis is disclosed in scheme 2.…”

Section: Antiprotozoal Activitymentioning

confidence: 99%

Recent contribution of medicinally active 2-aminothiophenes: A privileged scaffold for drug discovery

Duvauchelle

Meffre

Benfodda

2022

European Journal of Medicinal Chemistry

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Antiprotozoal Drugs

Cited by 8 publications

References 19 publications

Discovery of Anti-Amoebic Inhibitors from Screening the MMV Pandemic Response Box on Balamuthia mandrillaris, Naegleria fowleri, and Acanthamoeba castellanii

Discovery of Anti-Amoebic Inhibitors from Screening the MMV Pandemic Response Box on Balamuthia mandrillaris, Naegleria fowleri, and Acanthamoeba castellanii

A Review on the Ethnopharmacology and Phytochemistry of the Neotropical Sages (Salvia Subgenus Calosphace; Lamiaceae) Emphasizing Mexican Species

Recent contribution of medicinally active 2-aminothiophenes: A privileged scaffold for drug discovery

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