4-Arylamino-6-nitroquinazolines: Synthesis and their activities against neglected disease leishmaniasis.

ABSTRACT - 4-Arylamino-6-nitroquinazolines (2-25) were synthesized and evaluated for their
leishmanicidal activities against Leishmania major promastigotes in vitro with
IC50 values = 1.87-61.48 muM. Among the twenty four synthetic derivatives,
4-[4'-(methylsulfanyl)phenyl]amino-6-nitroquinazoline (21), and
4-(2'-methoxyphenyl)amino-6-nitroquinazoline (8) showed excellent antileishmanial
activities with IC50 values 1.87 +/- 0.31 and 4.37 +/- 0.02 muM, respectively,
more active than the standard drug, pentamidine (IC50 = 5.09 +/- 0.09 muM).
Compound 16 (IC50 = 6.53 +/- 0.21 muM) displayed an activity comparable to the
standard. Compounds 15 (IC50 = 9.04 +/- 0.03 muM), 18 (IC50 = 12.28 +/- 0.18
muM), 14 (IC50 = 19.87 +/- 0.22 muM), and 5 (IC50 = 24.03 +/- 2.71 muM) also
showed good activities.

CI - Copyright (c) 2015. Published by Elsevier Masson SAS.

AUTHORS - Saad SM

H. E. J. Research Institute of Chemistry, International Center for Chemical and
Biological Sciences, University of Karachi, Karachi 75270, Pakistan.

Ghouri, Nida

H. E. J. Research Institute of Chemistry, International Center for Chemical and
Biological Sciences, University of Karachi, Karachi 75270, Pakista- Perveen, Shahnaz
Perveen S
PCSIR Laboratories Complex, Karachi, Shahrah-e-Dr. Salimuzzaman Siddiqui, Karachi
75280, Pakistan.

Khan, Khalid Mohammed

AD - H. E. J. Research Institute of Chemistry, International Center for Chemical and
Biological Sciences, University of Karachi, Karachi 75270, Pakistan. Electronic
address: khalid.khan@iccs.edu.

Choudhary, M Iqbal
I
AD - H. E. J. Research Institute of Chemistry, International Center for Chemical and
Biological Sciences, University of Karachi, Karachi 75270, Pakistan; Department
of Biochemistry, Faculty of Sciences, King Abdulaziz University, Jeddah 21412,
Saudi Arabia.

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