The leishmaniases are a group of diseases caused by protozoan parasites—Leishmania sp. Leishmaniasis is classified among the 20 neglected diseases by WHO. Although the disease has been known for more than 120 years, the number of drugs used for the treatment is still limited to 5–6. The first-line drugs against leishmaniasis are pentavalent antimonials, which were introduced to the treatment 70 years ago—despite all their side effects. Molecular targets are becoming increasingly important for efficacy and selectivity in postgenomic drug research studies. In this chapter, we have discussed potential therapeutic targets of antileishmanial drug discovery such as pteridine reductase (PTR1), trypanothione reductase (TR), N-myristoyltransferase (NMT), trypanothione synthetase (TryS), IU-nucleoside hydrolase, and topoisomerases, enzymes and their inhibitors reported in the literature.
Part of the book: Leishmaniasis
Five-membered heteroaromatic ring fused pyridine derivatives are of increasing interest in drug design and medicinal chemistry. The structural similarity of many drugs (especially antiviral and anticancer ones) with DNA bases such as adenine and guanine is a key factor to explain their effectiveness. Apart from these, it is also found in the structures of substances with antituberculosis, antibacterial, antifungal, anti-inflammatory, and antimalarial activities. Another advantage of this group of compounds is their positive contribution to solubility, polarity, lipophilicity, and hydrogen bonding capacity properties of the compounds they are incorporated into. In this chapter, various bioactivities of fused pyridine derivatives will be categorized and summarized.
Part of the book: Exploring Chemistry with Pyridine Derivatives
Leishmaniasis is a parasitic disease caused by protozoa belonging to the genus Leishmania. Over one billion people are living in areas endemic to leishmaniasis and are at risk of infection. Each year, more than one million new cases are reported. Although few drugs are available for the treatment of leishmaniasis, none of them are ideal due to their high resistance and toxicity risk. Many compounds with quinazoline scaffold were synthesized and reported to have promising antiparasitic and antileishmanial activities. This review aims to evaluate the reported antileishmanial activities of quinazoline and its derivatives with a special focus on their structure-activity relationships.
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