Table 2SAR of selected 5H -[1,3,4]thiadiazolo[3,2-a]pyrimidin-5-ones versus the αIIbβ3 receptor

#SIDCIDR2P.Ad.A.a
% inhibitiond
P.Ad.A.a
IC 50d
P.Ag.A.a
I C50d
Image ml165fu5.jpg
3 (Ruc-1)89449667756604ethyl35%b> 20 μM8.4 μM
158944966844820655methyl20%bNDND
168944966944820657tert-butyl21%bNDND
1789449671448206422-(methoxymethyl)18%bNDND
Image ml165fu6.jpg
18 (NCGC00183896-01)89449681448206653-(2-aminoacetamide)92%b1.1 μM0.163 μM
1989449680448206543-((S)-2-aminopropanamide)35%c8.2 μM0.916 μM
2089449679448206403-((R)-2-aminopropanamide)69%c> 20 μM5.9 μM
2189449678448206673-(2-(methylamino)acetamide)24%cNDND
2289449682448206503-(piperidine-4-carboxamide)64%c> 20 μM8.6 μM
a

P.Ad.A. = platelet adhesion assay. P.Ag.A. = platelet aggregation assay;

b

% inhibition at 30 μM;

c

% inhibition at 100 μM

d

% inhibition and IC50 values were determined utilizing modifications of the platelet adhesion and aggregation assays described in Blue et al, Blood 2008, 111, 1248.

ND = not determined.

From: Inhibitors of Platelet Integrin αllbβ3

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