677722-97-3Relevant academic research and scientific papers
Synthesis, antimalarial evaluation and molecular docking studies of some thiolactone derivatives
Sainy, Jitendra,Sharma, Rajesh
, p. 350 - 359 (2017)
In present study novel thiolactone derivatives were designed, synthesized and characterized by various analytical techniques such as IR, 1H NMR, 13C NMR, mass spectral data and elemental analysis. All synthesized compounds were evaluated for in?vitro antimalarial activity against Dd2 and 3d7 strain of P.?falciparum. All synthesized compounds were also subjected for molecular docking study with pf KASI/II enzyme to analyze their binding orientation in the active site of the enzyme. Compounds 5d, 5e, and 5i found to be most potent with IC50 in the range of 0.09–0.19?μM and 0.03–0.04?μM against the Dd2 strain and 3D7 strain respectively as well as they showed good binding affinities with the residues of the active site of pf KASI/II.
Analogues of thiolactomycin as potential anti-malarial and anti-trypanosomal agents
Jones, Simon M.,Urch, Jonathan E.,Brun, Reto,Harwood, John L.,Berry, Colin,Gilbert, Ian H.
, p. 683 - 692 (2007/10/03)
A series of analogues of the naturally occurring antibiotic thiolactomycin (TLM) have been synthesised and evaluated for their ability to inhibit the growth of the malaria parasite, Plasmodium falciparum. Thiolactomycin is an inhibitor of Type II fatty acid synthase which is found in plants and most prokaryotes, but not an inhibitor of Type I fatty acid synthase in mammals. A number of the analogues showed inhibition equal to or greater than TLM. The introduction of hydrophobic alkyl groups at the C3 and C5 positions of the thiolactone ring lead to increased inhibition, the best showing a fourteenfold increase in activity over TLM. In addition, some of the analogues showed activity when assayed against the parasitic protozoa, Trypanosoma cruzi and Trypanosoma brucei.
