Hidayat Hussain and Ahmed Al-Harrasi
UoN Chair of Oman's Medicinal Plants and Marine Natural Products, University of Nizwa, Oman
Malaria affects millions of people in the World and recent reports showed that 40% of the world populations were infected by said disease. The recent WHO reports mentioned that 90% of malaria deaths takes place in African Region and malaria is considered the remarkable parasitic disease of humans and Plasmodium falciparum cause human malaria [1-3]. Drug resistance is the major problem in malaria treatment and P. falciparum showed resistance to cheap drugs. Therefore new classes of effective compounds are necessary in order to reduce the risk of resistance. In a continuation of our biology-oriented synthesis, a series of new phenazines, quinoline-5,8-dione, and hydroxynaphthoquinone derivatives (Scheme 1) [1-3] were synthesized.
Scheme 1: Phenazines and oquinone derivatives.
The synthesized compounds were screened for in vitro antimalarial effects towards chloroquine-resistant strains of P. falciparum. It is noteworthy that most of tested compounds demonstrated significant in vitro effects with IC50 below 5 µM and some compounds have IC50 below 1 µM. Furthermore some tested compounds also demonstrated promising in vivo activities. Details of in vitro, in vivo and molecular docking studies of tested compounds will be presented.
 Hussain, H.; Krohn, K.; Saeftel, M.; Sarite, S. R.; Hoerauf, A., J. Med. Chem. 2011, 54, 4913-4917.
 Hussain, H.; Saeftel, M.; Sarite, S. R.; Hoerauf, A.; Krohn, K., Eur. J. Med. Chem. 2012, 54, 936-942.
 Eyong, K. O.; Hussain, H.; Folefoc, G. N.; Nkengfack, A. E.; Saeftel, M.; Sarite, S. R.; Hoerauf, A.; Krohn, K. Rasayan J. Chem. 2011, 4, 713-722.