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Synthesis of Heterocyclic Chalcones as Novel Antileishmanial Agents
Author(s) -
Ashburn Bradley
Publication year - 2021
Publication title -
the faseb journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.709
H-Index - 277
eISSN - 1530-6860
pISSN - 0892-6638
DOI - 10.1096/fasebj.2021.35.s1.00118
Subject(s) - malaria , leishmaniasis , sandfly , neglected tropical diseases , tropical disease , disease , disfigurement , cutaneous leishmaniasis , environmental health , medicine , geography , immunology , leishmania , parasite hosting , surgery , pathology , world wide web , computer science
Severe skin disfigurement, scarring of the mouth and nose, and internal organ failure afflict an estimated 1.3 million people annually due to the flesh‐eating parasite which causes the disease known as leishmaniasis. It the second largest parasitic killer behind malaria. There are no vaccines and current drug treatments are highly toxic. Even after treatment, the parasite is not eradicated, it remains dormant in the body to potentially strike again. The World Health Organization classifies leishmaniasis as a Neglected Tropical Disease (NTD) which means it occurs in tropical or sub‐tropical regions of the Earth. The most affected areas are Northern Africa, the Middle East, Southern Europe, parts of Asia, and Central America; plaguing those that live in poverty the hardest. These people typically do not have the access, finances, or ability to obtain treatments which need intravenous delivery over multiple sessions, thus creating an unfortunate health disparity. The skin lesions and disfiguration caused by the cutaneous and mucosal forms may result in becoming outcasts from their communities and cause a significant reduction in quality of life. The visceral form, also known as kala‐azar, is potentially fatal. The areas affected are growing due to vector habitat increase from the warming global climate. The parasite is transmitted via the bite of the phlebotomine sandfly. With more than 1 billion people in approximately 90 countries at risk of infection due to living in areas where leishmaniasis is endemic, the discovery of new effective medications is imperative to improve the lives of millions worldwide. Recent reports of a privileged class of natural products known as chalcones show promise as new antileishmanial agents for all three forms of the disease; cutaneous, mucosal, and visceral. This study will showcase our efforts to discover new targets of opportunity that may lead to better treatments for cutaneous leishmaniasis caused by the protozoan parasite Leishmania major via the synthesis of novel chalcones containing heterocyclic functionalities to impart a dual pharmacophore effect.