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8716368 
Journal Article 
Design, synthesis, and in vitro biological evaluation of novel thiazolopyrimidine derivatives as antileishmanial compounds 
Istanbullu, H; Bayraktar, G; Akbaba, H; Cavus, I; Coban, G; Debelec Butuner, B; Kilimcioglu, AA; Ozbilgin, A; Alptuzun, V; Erciyas, E 
2020 
Yes 
Archiv der Pharmazie
ISSN: 0365-6233
EISSN: 1521-4184 
353 
8 
e1900325 
English 
32484266 
A series of thiazolopyrimidine derivatives was designed and synthesized as a Leishmania major pteridine reductase 1 (LmPTR1) enzyme inhibitor. Their LmPTR1 inhibitor activities were evaluated using the enzyme produced by Escherichia coli in a recombinant way. The antileishmanial activity of the selected compounds was tested in vitro against Leishmania sp. Additionally, the compounds were evaluated for cytotoxic activity against the murine macrophage cell line RAW 264.7. According to the results, four compounds displayed not only a potent in vitro antileishmanial activity against promastigote forms but also low cytotoxicity. Among them, compound L16 exhibited an antileishmanial activity for both the promastigote and amastigote forms of L. tropica, with IC50 values of 7.5 and 2.69 µM, respectively. In addition, molecular docking studies and molecular dynamics simulations were also carried out in this study. In light of these findings, the compounds provide a new potential scaffold for antileishmanial drug discovery. 
antileishmanial; Leishmania major; Leishmania tropica; neglected disease; PTR1 enzyme inhibition; thiazolo[5,4-d]pyrimidine