In Vitro Antileishmanial Activities of 2-Aryl-4(3H)-quinazolinones

作者：Perveen Shama; Saad Syed Muhammad; Perveen Shahnaz; Hameed Abdul; Alam Muhammad Tanveer; Khan Khalid Mohammed^*; Choudhary M Iqbal

来源：Journal of the Chemical Society of Pakistan, 2016, 38(2): 352-357.

• 2-Aryl-4(3H)-quinazolinones
• Leishmania major promastigotes
• Antileishmanial activity
• Structure activity relationship

A series of synthetic 2-aryl-4(3H)-quinazolinones (1-25) was evaluated for in vitro antileishmanial activities against promastigotes of Leishmania major. Compound 1, with nitro group installed at C-4', was found to be the most active analog having the IC50 value of 35.8 +/- 0.1 mu M against the standard, pentamidine (IC50 = 5.09 +/- 0.09 mu M). Fourteen other derivatives i.e. 2, 5-8, 10-12, 14, 16, 19, 22, 24, ad 25, showed a moderate to weak antilieshmanial activity with IC50 values between 62.8 - 90.45 mu M. The results indicate the potential of these compounds as leads for further studies towards the development of antileishmanial drugs.

• 出版日期2016-4