URI
URI Label
Revisions
Add to List
Edit Entry
Export:
XML
- November 2017 (1)
- July 2017 (1)
- February 2017 (1)
- January 2017 (2)
- May 2016 (1)
- April 2016 (1)
- December 2015 (1)
- November 2015 (2)
- August 2015 (1)
- June 2015 (1)
- May 2015 (3)
- April 2015 (1)
- January 2015 (1)
- December 2014 (1)
- November 2014 (2)
- August 2014 (4)
- July 2014 (2)
- June 2014 (3)
- May 2014 (1)
- April 2014 (3)
- March 2014 (2)
- February 2014 (2)
- January 2014 (1)
- December 2013 (2)
- November 2013 (3)
- September 2013 (1)
- August 2013 (1)
- July 2013 (2)
- June 2013 (2)
- April 2013 (1)
- March 2013 (1)
- February 2013 (2)
- January 2013 (1)
- December 2012 (2)
- November 2012 (1)
- September 2012 (2)
- June 2012 (2)
- April 2012 (4)
- March 2012 (2)
- March 2012 (2)
- January 2012 (3)
- 3D7 IC50 Avery Lab (3)
- AstraZeneca (2)
- MetID (3)
- Potencies GSK (1)
- Potencies Guy (1)
- Syngene (8)
- UCSD (1)
- Biology (37)
- DMPK (2)
- Dundee (4)
- GSH-EE - Chapman Lab (2)
- GSK PRR Assay (1)
- Imperial DGFA (1)
- Kirk Lab (5)
- Metabolism (1)
Show/Hide Keys
A set of 16 Series 4 Triazolopyrazine Frontrunner compounds were sent to have their efficacy re-evaluated against Plasmodium falciparum in-vitro at Dundee.
N.B. Potency values are an average of 2 runs. In one case (MMV672687), the 2 runs gave more-divergent-than-ideal values, however the average is still reported.
Discussion of the Frontrunner compounds and previous in-vitro data can be found here.
The following results were obtained:
Brief comments:
In comparison with the previous Frontrunner data linked above, all but one of the new potency values were slightly higher than before, but all values still indicate the active compounds were active etc.
MMV672687 had better activity than before even considering the N.B. above.
Strings:
MMV663915 OSM-S-293
ClC(C=C1)=CC=C1C2=NN=C3C=NC=C(OCCC4=CC=CC=C4)N32 InChI=1S/C19H15ClN4O/c20-16-8-6-15(7-9-16)19-23-22-17-12-21-13-18(24(17)19)25-11-10-14-4-2-1-3-5-14/h1-9,12-13H,10-11H2
MMV670936 OSM-S-366
FC1=C(F)C=CC(CCOC2=CN=CC3=NN=C(C4=CN=C(C(F)(F)F)C=C4)N32)=C1 InChI=1S/C19H12F5N5O/c20-13-3-1-11(7-14(13)21)5-6-30-17-10-25-9-16-27-28-18(29(16)17)12-2-4-15(26-8-12)19(22,23)24/h1-4,7-10H,5-6H2
MMV639565 OSM-S-272
ClC(C=C1)=CC=C1C2=NN=C3C=NC=C(OCCC4=CC(F)=C(F)C=C4)N32 InChI=1S/C19H13ClF2N4O/c20-14-4-2-13(3-5-14)19-25-24-17-10-23-11-18(26(17)19)27-8-7-12-1-6-15(21)16(22)9-12/h1-6,9-11H,7-8H2
MMV897709 OSM-S-218
FC1=C(F)C=CC(C(OC)COC2=CN=CC3=NN=C(C4=CC=C(C#N)C=C4)N32)=C1 InChI=1S/C21H15F2N5O2/c1-29-18(15-6-7-16(22)17(23)8-15)12-30-20-11-25-10-19-26-27-21(28(19)20)14-4-2-13(9-24)3-5-14/h2-8,10-11,18H,12H2,1H3
MMV688895 OSM-S-278
OC(C1=CC=CC=C1)COC2=CN=CC3=NN=C(C4=CN=C(C(F)(F)F)C=C4)N32 InChI=1S/C19H14F3N5O2/c20-19(21,22)15-7-6-13(8-24-15)18-26-25-16-9-23-10-17(27(16)18)29-11-14(28)12-4-2-1-3-5-12/h1-10,14,28H,11H2
MMV672687 OSM-S-390
OC(C1=CC(F)=C(F)C=C1)COC2=CN=CC3=NN=C(C4=CC=C(OC(F)F)C=C4)N32 InChI=1S/C20H14F4N4O3/c21-14-6-3-12(7-15(14)22)16(29)10-30-18-9-25-8-17-26-27-19(28(17)18)11-1-4-13(5-2-11)31-20(23)24/h1-9,16,20,29H,10H2
MMV688896 OSM-S-279
OC(C1=CC=CC=C1)COC2=CN=CC3=NN=C(C4=CC=C(OC(F)F)C=C4)N32 InChI=1S/C20H16F2N4O3/c21-20(22)29-15-8-6-14(7-9-15)19-25-24-17-10-23-11-18(26(17)19)28-12-16(27)13-4-2-1-3-5-13/h1-11,16,20,27H,12H2
MMV693155 OSM-S-353
OCC(C1=CC=CC=C1)COC2=CN=CC3=NN=C(C4=CC=C(OC(F)F)C=C4)N32 InChI=1S/C21H18F2N4O3/c22-21(23)30-17-8-6-15(7-9-17)20-26-25-18-10-24-11-19(27(18)20)29-13-16(12-28)14-4-2-1-3-5-14/h1-11,16,21,28H,12-13H2
MMV897763 OSM-S-389
FC1=C(F)C=CC(C(N(C)C)COC2=CN=CC3=NN=C(C4=CC=C(OC(F)F)C=C4)N32)=C1 InChI=1S/C22H19F4N5O2/c1-30(2)18(14-5-8-16(23)17(24)9-14)12-32-20-11-27-10-19-28-29-21(31(19)20)13-3-6-15(7-4-13)33-22(25)26/h3-11,18,22H,12H2,1-2H3
MMV669000 OSM-S-177
O=C(N1CC(C=CC=C2)=C2C1)C3=CN=CC4=NN=C(C5=CC=C(OC(F)F)C=C5)N43 InChI=1S/C21H15F2N5O2/c22-21(23)30-16-7-5-13(6-8-16)19-26-25-18-10-24-9-17(28(18)19)20(29)27-11-14-3-1-2-4-15(14)12-27/h1-10,21H,11-12H2
MMV670246 OSM-S-367
O=C(NC1=CC=C(Cl)C=C1)C2=CN=CC3=NN=C(C4=CC=C(OC(F)F)C=C4)N32 InChI=1S/C19H12ClF2N5O2/c20-12-3-5-13(6-4-12)24-18(28)15-9-23-10-16-25-26-17(27(15)16)11-1-7-14(8-2-11)29-19(21)22/h1-10,19H,(H,24,28)
MMV670767 OSM-S-379
O=C(NC1=CC=C(F)C(Cl)=C1)C2=CN=CC3=NN=C(C4=CC=C(OC(F)F)C=C4)N32 InChI=1S/C19H11ClF3N5O2/c20-13-7-11(3-6-14(13)21)25-18(29)15-8-24-9-16-26-27-17(28(15)16)10-1-4-12(5-2-10)30-19(22)23/h1-9,19H,(H,25,29)
MMV670944 OSM-S-175
O=C(NC1=CC=NC(C(F)(F)F)=C1)C2=CN=CC3=NN=C(C4=CC=C(OC(F)F)C=C4)N32 InChI=1S/C19H11F5N6O2/c20-18(21)32-12-3-1-10(2-4-12)16-29-28-15-9-25-8-13(30(15)16)17(31)27-11-5-6-26-14(7-11)19(22,23)24/h1-9,18H,(H,26,27,31)
MMV675718 OSM-S-201
O=C(NC1=CC=CC(Cl)=C1C)C2=CN=CC3=NN=C(C4=CC=C(OC(F)F)C=C4)N32 InChI=1S/C20H14ClF2N5O2/c1-11-14(21)3-2-4-15(11)25-19(29)16-9-24-10-17-26-27-18(28(16)17)12-5-7-13(8-6-12)30-20(22)23/h2-10,20H,1H3,(H,25,29)
MMV675946 OSM-S-946
O=C(NC1=CC=CC(Cl)=C1F)C2=CN=CC3=NN=C(C4=CC=C(OC(F)F)C=C4)N32 InChI=1S/C19H11ClF3N5O2/c20-12-2-1-3-13(16(12)21)25-18(29)14-8-24-9-15-26-27-17(28(14)15)10-4-6-11(7-5-10)30-19(22)23/h1-9,19H,(H,25,29)
MMV675947 OSM-S-254
O=C(NC1=C(C)C=CC(Cl)=C1)C2=CN=CC3=NN=C(C4=CC=C(OC(F)F)C=C4)N32 InChI=1S/C20H14ClF2N5O2/c1-11-2-5-13(21)8-15(11)25-19(29)16-9-24-10-17-26-27-18(28(16)17)12-3-6-14(7-4-12)30-20(22)23/h2-10,20H,1H3,(H,25,29)