scholarly journals Synthesis and Biological Activity of Sterol 14α-Demethylase and Sterol C24-Methyltransferase Inhibitors

Molecules ◽  
2018 ◽  
Vol 23 (7) ◽  
pp. 1753 ◽  
Author(s):  
David Leaver
Keyword(s):  
Biological Activity ◽  
Drug Target ◽  
Human African Trypanosomiasis ◽  
Neglected Tropical Diseases ◽  
Pathogenic Fungi ◽  
Molecular Target ◽  
Tropical Diseases ◽  
Sterol Metabolism ◽  
Methyl Group ◽  
Animal Host

Sterol 14α-demethylase (SDM) is essential for sterol biosynthesis and is the primary molecular target for clinical and agricultural antifungals. SDM has been demonstrated to be a valid drug target for antiprotozoal therapies, and much research has been focused on using SDM inhibitors to treat neglected tropical diseases such as human African trypanosomiasis (HAT), Chagas disease, and leishmaniasis. Sterol C24-methyltransferase (24-SMT) introduces the C24-methyl group of ergosterol and is an enzyme found in pathogenic fungi and protozoa but is absent from animals. This difference in sterol metabolism has the potential to be exploited in the development of selective drugs that specifically target 24-SMT of invasive fungi or protozoa without adversely affecting the human or animal host. The synthesis and biological activity of SDM and 24-SMT inhibitors are reviewed herein.

Neglected tropical diseases

2019 ◽  
pp. 463-506
Author(s):  
Jan Hajek
Keyword(s):  
Clinical Experience ◽  
Human African Trypanosomiasis ◽  
Neglected Tropical Diseases ◽  
Diagnostic Testing ◽  
Available P ◽  
Tropical Diseases ◽  
African Trypanosomiasis ◽  
Humanitarian Settings ◽  
Contextual Features ◽  
The Poor

This chapter on neglected tropical diseases (NTDs) provides an overview of the background and main contextual features of NTDs, and includes clear guidance on their clinical recognition and management. Recognizing the prevalence of NTDs in humanitarian settings, with their disproportional effect on the poor, this chapter covers the fundamentals of management of NTDs, and is especially helpful for the provider who may have little prior clinical experience with such conditions. It also includes detailed guidance on recognition and diagnosis of the main NTDs, such as dengue, human African trypanosomiasis, leishmaniasis, leprosy, and schistosomiasis, in settings with very limited diagnostic testing available.

scholarly journals Strengthening data collection for neglected tropical diseases: What data are needed for models to better inform tailored intervention programmes?

2021 ◽  
Vol 15 (5) ◽  
pp. e0009351
Author(s):  
Jaspreet Toor ◽  
Jonathan I. D. Hamley ◽  
Claudio Fronterre ◽  
María Soledad Castaño ◽  
Lloyd A. C. Chapman ◽  
...  
Keyword(s):  
Data Collection ◽  
Human African Trypanosomiasis ◽  
Neglected Tropical Diseases ◽  
World Health ◽  
Tropical Diseases ◽  
Tailored Intervention ◽  
Specific Data ◽  
Tailored Interventions ◽  
The World ◽  
Health Organization

Locally tailored interventions for neglected tropical diseases (NTDs) are becoming increasingly important for ensuring that the World Health Organization (WHO) goals for control and elimination are reached. Mathematical models, such as those developed by the NTD Modelling Consortium, are able to offer recommendations on interventions but remain constrained by the data currently available. Data collection for NTDs needs to be strengthened as better data are required to indirectly inform transmission in an area. Addressing specific data needs will improve our modelling recommendations, enabling more accurate tailoring of interventions and assessment of their progress. In this collection, we discuss the data needs for several NTDs, specifically gambiense human African trypanosomiasis, lymphatic filariasis, onchocerciasis, schistosomiasis, soil-transmitted helminths (STH), trachoma, and visceral leishmaniasis. Similarities in the data needs for these NTDs highlight the potential for integration across these diseases and where possible, a wider spectrum of diseases.

Recent Approaches to Chemical Discovery and Development Against Malaria and the Neglected Tropical Diseases Human African Trypanosomiasis and Schistosomiasis

2014 ◽  
Vol 114 (22) ◽  
pp. 11138-11163 ◽  
Author(s):  
Mathew Njoroge ◽  
Nicholas M. Njuguna ◽  
Peggoty Mutai ◽  
Dennis S. B. Ongarora ◽  
Paul W. Smith ◽  
...  
Keyword(s):  
Human African Trypanosomiasis ◽  
Neglected Tropical Diseases ◽  
Tropical Diseases ◽  
African Trypanosomiasis

scholarly journals The Atlas of human African trypanosomiasis: a contribution to global mapping of neglected tropical diseases

2010 ◽  
Vol 9 (1) ◽  
pp. 57 ◽  
Author(s):  
Pere P Simarro ◽  
Giuliano Cecchi ◽  
Massimo Paone ◽  
José R Franco ◽  
Abdoulaye Diarra ◽  
...  
Keyword(s):  
Human African Trypanosomiasis ◽  
Neglected Tropical Diseases ◽  
Tropical Diseases ◽  
African Trypanosomiasis ◽  
Global Mapping

Fe3+chelating quinoline–hydrazone hybrids with proven cytotoxicity, leishmanicidal, and trypanocidal activities

2018 ◽  
Vol 20 (31) ◽  
pp. 20382-20390 ◽  
Author(s):  
Juan Carlos Coa ◽  
Wilson Cardona-Galeano ◽  
Albeiro Restrepo
Keyword(s):  
Developing Countries ◽  
Biological Activity ◽  
Direct Relationship ◽  
Neglected Tropical Diseases ◽  
Tropical Diseases ◽  
Chelating Ability

Neglected tropical diseases cause great concern in developing countries where there are millions of reported infected humans. Our calculations support a direct relationship between biological activity and the Fe3+chelating ability of the shown set of quinoline–hydrazone hybrids.

scholarly journals Putting Anthropology into Global Health

2019 ◽  
Vol 26 (1) ◽  
pp. 31-41 ◽  
Author(s):  
Jorge Varanda ◽  
Josenando Théophile
Keyword(s):  
Public Health ◽  
Global Health ◽  
Human African Trypanosomiasis ◽  
Neglected Tropical Diseases ◽  
Tropical Diseases ◽  
Health Campaigns ◽  
African Trypanosomiasis ◽  
Public Health Campaigns ◽  
Insight Into

This analysis of over a century of public health campaigns against human African trypanosomiasis (sleeping sickness) in Angola aims to unravel the role of (utopian) dreams in global health. Attention to the emergence and use of concepts such as neglected tropical diseases (NTDs) and ideas about elimination or eradication highlights how these concepts and utopian dreams are instrumental for the advancement of particular agendas in an ever-shifting field of global health. The article shows how specific representations of the elimination and eradication of diseases, framed over a century ago, continue to push Western views and politics of care onto others. This analysis generates insight into how global health and its politics of power functioned in Angola during colonialism and post-independence.

The use of Sulfonamide Derivatives in the Treatment of Trypanosomatid Parasites including Trypanosoma cruzi, Trypanosoma brucei, and Leishmania ssp

2020 ◽  
Vol 16 (1) ◽  
pp. 24-38 ◽  
Author(s):  
Cauê B. Scarim ◽  
Rafael C. Chelucci ◽  
Jean L. dos Santos ◽  
Chung M. Chin
Keyword(s):  
Trypanosoma Cruzi ◽  
Trypanosoma Brucei ◽  
Human African Trypanosomiasis ◽  
Neglected Tropical Diseases ◽  
Economic Incentive ◽  
Tropical Diseases ◽  
Lipinski’S Rule ◽  
Novel Drugs ◽  
Trypanosomatid Parasites ◽  
Research And Policy

More than 10 million people around the world are afflicted by Neglected Tropical Diseases, such as Chagas Disease, Human African Trypanosomiasis, and Leishmania. These diseases mostly occur in undeveloped countries that suffer from a lack of economic incentive, research, and policy for new compound development. Sulfonamide moieties are effective scaffolds present in several compounds that are determinants to treat various diseases, principally neglected tropical diseases. This review article examines the contribution of these scaffolds in medicinal chemistry in the last five years, focusing on three trypanosomatid parasites: Trypanosoma cruzi, Trypanosoma brucei, and Leishmania ssp. We also present perspectives for their use in drug designs in an effort to contribute to new drug development. In addition, we consider the physicochemical parameters, whose molecules all presented according to Lipinski's rule. The correlation between the selective index and LogP was evaluated, showing that sulfonamide derivatives can act differently against each trypanosomatid parasite. Moreover, the approaches of novel drugs and technologies are very important for the eventual drug discovery against trypanosomatid diseases.

Dual Inhibition of Parasitic Targets: a Valuable Strategy to Treat Malaria and Neglected Tropical Diseases

2021 ◽  
Vol 28 ◽  
Author(s):  
Santo Previti ◽  
Carla Di Chio ◽  
Roberta Ettari ◽  
Maria Zappalà
Keyword(s):  
Human African Trypanosomiasis ◽  
Neglected Tropical Diseases ◽  
Parasitic Diseases ◽  
Tropical Diseases ◽  
Parasite Survival ◽  
Innovative Idea ◽  
Dual Inhibition ◽  
Antiparasitic Drugs ◽  
Effective Drugs ◽  
Made In

: Despite the countless efforts made in the last decades, malaria and neglected tropical diseases remain a high-impact health problem in developing countries. Malaria is one of the most severe parasitic diseases, with over 200 million cases and 400 000 deaths in 2019. Parasitic diseases caused by trypanosomatidae, namely Human African Trypanosomiasis, Chagas disease, and leishmaniasis, register the highest rates of mortality amongst all the neglected tropical diseases. In this scenario, chemotherapy remains the first strategy which aims to control and eliminate these diseases. However, the use of outdated, unsafe, and poorly effective drugs, together with the onset of resistance, prompted the researchers to the identification of new and valid targets. The innovative idea, aimed at the development of multi-target ligands addressing two different targets playing key roles in the parasite survival, could represent a valuable strategy. Thanks to this approach, the well-known limitations characterizing the antiparasitic drugs, such as toxicity, rapid resistance onset and narrow spectrum of action, could be overcome. In this review, we now describe the most recent multi-target ligands endowed with antiparasitic effect reported in the literature, focusing our attention on their binding with the targets, inhibitory activities, and potential therapeutic applications.

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