Exp166

=Objective= To test the inhibitory activity of Ugi products 148B and 150D against Plasmodium Falciparum. For a summary of the project refer to [|this post]. =Contributors= Jiri Gut from the Rosenthal group performed these experiments. =Procedure= The compounds are dissolved in DMSO as 10 mM stock then diluted 1:1000 into culture medium pH 7.4 (50 mM phosphate, 25 mM HEPES and bicarbonate buffers with 10% human serum). The parasites are then added and incubated for 48 hrs. Parasite development is measured by flow cytometry. =Results= =Discussion=
 * **compound** || **Test 1 IC-50 (nM)** || **SD** || **Test 2 IC-50 (nM)** || **SD** ||
 * 148B || 7994 || 733 || 14335 || 120 ||
 * 150D || 5411 || 241 || 8711 || 549 ||
 * chloroquine || 57.627 || 1.2 || 42 || 3 ||

Both Ugi products did inhibit Plasmodium Falciparum at concentrations 100-300 times that of chloroquine. The food vacuole abnormality, which is indicative of cysteine protease inhibition was not observed in the parasites, suggesting other mode of action. =Conclusion= Both Ugi products proved to be inhibitors of Plasmodium Falciparum with IC-50s in the range of 5.4-14.3 micromolar. =Log= =Tags=

[|Phenanthrene-9-carboxaldehyde][|InChI=1/C15H10O/c16-10-12-9-11-5-1-2-6-13(11)15-8-4-3-7-14(12)15/h1-10H] InChIKey: [|QECIGCMPORCORE]-[|UHFFFAOYAE] [|tert-butylisocyanide][|InChI=1/C5H9N/c1-5(2,3)6-4/h1-3H3] InChIKey: [|FAGLEPBREOXSAC]-[|UHFFFAOYAL] [|Crotonic Acid]: [|InChI=1/C4H6O2/c1-2-3-4(5)6/h2-3H,1H3,(H,5,6)/f/h5H] InChIKey: [|LDHQCZJRKDOVOX]-[|UHFFFAOYAC] [|n-Heptylamine] : [|InChI=1/C7H17N/c1-2-3-4-5-6-7-8/h2-8H2,1H3] InChIKey: [|WJYIASZWHGOTOU]-[|UHFFFAOYAD] targetUgiExp148:[|InChI=1/C31H40N2O2/c1-6-8-9-10-15-21-33(28(34)16-7-2)29(30(35)32-31(3,4)5)] [|27-22-23-17-11-12-18-24(23)25-19-13-14-20-26(25)27/h7,11-14,16-20,22,29H,6,8-10,15,21H2,1-5H3,(H,32,35)/b16-7]

[|Phenanthrene-9-carboxaldehyde][|InChI=1/C15H10O/c16-10-12-9-11-5-1-2-6-13(11)15-8-4-3-7-14(12)15/h1-10H] InChIKey: [|QECIGCMPORCORE]-[|UHFFFAOYAE] [|tert-butylisocyanide][|InChI=1/C5H9N/c1-5(2,3)6-4/h1-3H3] InChIKey: [|FAGLEPBREOXSAC]-[|UHFFFAOYAL] [|Crotonic Acid]: [|InChI=1/C4H6O2/c1-2-3-4(5)6/h2-3H,1H3,(H,5,6)/f/h5H] InChIKey: [|LDHQCZJRKDOVOX]-[|UHFFFAOYAC] [|benzylamine] [|InChI=1/C7H9N/c8-6-7-4-2-1-3-5-7/h1-5H,6,8H2] InChIKey: [|WGQKYBSKWIADBV]-[|UHFFFAOYAL] [|Ugi Product Exp150]