title: 4, 5-Dihydrooxazole-pyrazoline hybrids: Synthesis and their evaluation as potential antimalarial agents.
abstract: A new series of oxazoline-pyrazoline hybrids (4a-p) were synthesized by condensation reaction of substituted oxazoline based chalcones (3a-m) and substituted hydrazines in methanol. Some of the compounds exhibited promising in vitro antimalarial activity for chloroquine sensitive CQ(S) (3D7) strain and chloroquine resistant CQ(R) (RKL9) strain. The most potent analogue 4i (IC50 0.322 μg/ml) exhibited significant in vivo antimalarial potential against Plasmodium berghei mouse model. The stable complex of 4i with hematin (1:1 stoichiometry) suggests that heme may be one possible target for these hybrid compounds. The study has revealed potential of title compounds as lead for the development of antimalarial agents.
authors: Drug Design and Medicinal Chemistry Lab, Department of Pharmaceutical Chemistry, Faculty of Pharmacy and Bioinformatics Infrastructure Facility(BIF), Jamia Hamdard, New Delhi, 110062, India.
authors: Ashutosh Kumar
authors: AK
authors: Pandey
authors: National Institute of Malaria Research (ICMR), Sector 8, Dwarka, New Delhi, 110077, India.
authors: Supriya
authors: S
authors: Sharma
authors: BBS Institute of Pharmaceutical & Allied Sciences, Greater Noida, 201310, U.P, India.
authors: Minakshi
authors: M
authors: Pandey
authors: Drug Design and Medicinal Chemistry Lab, Department of Pharmaceutical Chemistry, Faculty of Pharmacy and Bioinformatics Infrastructure Facility(BIF), Jamia Hamdard, New Delhi, 110062, India.
authors: M Mumtaz
authors: MM
authors: Alam
authors: Drug Design and Medicinal Chemistry Lab, Department of Pharmaceutical Chemistry, Faculty of Pharmacy and Bioinformatics Infrastructure Facility(BIF), Jamia Hamdard, New Delhi, 110062, India.
authors: M
authors: M
authors: Shaquiquzzaman
authors: Drug Design and Medicinal Chemistry Lab, Department of Pharmaceutical Chemistry, Faculty of Pharmacy and Bioinformatics Infrastructure Facility(BIF), Jamia Hamdard, New Delhi, 110062, India. Electronic address: mymoonaakhter@gmail.com.
authors: Mymoona
authors: M
authors: Akhter
mesh_terms: D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D047188:Chalcones / Q000737:chemistry; D060326:Chemistry Techniques, Synthetic; D002522:Chlorocebus aethiops; D015195:Drug Design; D005260:Female; D020128:Inhibitory Concentration 50; D051379:Mice; D010962:Plasmodium berghei / Q000187:drug effects; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D051381:Rats; D014709:Vero Cells
chemical_list: D000962:Antimalarials; D047188:Chalcones; D011720:Pyrazoles
keywords: Antimalarial; IC(50); Oxazoline; Plasmodium falciparum; Pyrazoline