Background: Leishmaniasis is a complex devastating disease that is widespread across the globe with 400 million people in 90 countries at a risk of acquiring leishmaniasis. It is caused by intracellular parasites belonging to genus Leishmania.
Objective: The therapeutic use of commonly available drugs like Pentostam, Glucantime, Amphotericin B, Paramomycin, and Miltefosine have has been declined due to their low efficacy, drug resistance and high toxicity. Therefore, a continuous effort is needed in order to find out less toxic and more successful drugs in future for the handling of leishmaniasis. Results: Quinazoline derivatives are reported to have promising antileishmanial activities. A number of quinazoline derivatives were synthesized in the past three decades, by means of various synthetic pathways due to their ease of synthesis and favorable physicochemical properties. Conclusion: This review focuses on various synthetic procedures, chemical characteristics and antileishmanial activities of various quinazoline derivatives with respect to antileishmanial drug discovery.Keywords: Antileishmanial analogues, drug resistance, leishmaniasis, quinazolinone derivatives.