Kumar Gautam, Tanwar Omprakash, Kumar Jitender, Akhter Mymoona, Sharma Supriya, Pillai C R, Alam Md Mumtaz, Zama M S
Drug Design and Medicinal Chemistry Lab, Department of Pharmaceutical Chemistry, School of Pharmaceutical Education and Research, Jamia Hamdard, New Delhi, India.
Drug Design and Medicinal Chemistry Lab, Department of Pharmaceutical Chemistry, School of Pharmaceutical Education and Research, Jamia Hamdard, New Delhi, India.
Eur J Med Chem. 2018 Apr 10;149:139-147. doi: 10.1016/j.ejmech.2018.01.082. Epub 2018 Feb 15.
A series of pyrazole-pyrazoline substituted with benzenesulfonamide were synthesized and evaluated for their antimalarial activity in vitro and in vivo. The compounds were active against both chloroquine (CQ) sensitive (3D7) and CQ resistant (RKL-9) strains of Plasmodium falciparum. Seven compounds (7e, 7i, 7j, 7l, 7m, 7o and 7p) exhibiting EC less than 2 μM. A mechanistic study of compound 7o revealed that these compound act through the inhibition of β-hematin. The study indicated that these compounds can serve as lead compounds for further development of potent antimalarial drugs.
合成了一系列苯磺酰胺取代的吡唑-吡唑啉，并对其体外和体内抗疟活性进行了评估。这些化合物对恶性疟原虫的氯喹（CQ）敏感株（3D7）和CQ耐药株（RKL-9）均有活性。七种化合物（7e、7i、7j、7l、7m、7o和7p）的半数有效浓度（EC）小于2μM。对化合物7o的机理研究表明，该化合物通过抑制β-血红素发挥作用。研究表明，这些化合物可作为进一步开发强效抗疟药物的先导化合物。
