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. 2020 Aug 25;14:80–90. doi: 10.1016/j.ijpddr.2020.08.006

Table 1.

Reported diacyl ureas, acyl ureas and acyl carbamates with their overall yields, ClogP values, and IC50 indices against T. gondii and C. parvum parasites.

 Image 2
Compound
 Starting Material I Nucleophile III Final Product Yielda ClogPg IC50 (μM)
Code No T. gondii C. parvum
JS-1-07 1 a Image 3 a Image 4 Image 5 89b,c 2.64 NAh NA
JS-1-11 2 b Image 6 b Image 7 Image 8 70c,d 0.90 NA NA
JS-1-09 3 c Image 9 c Image 10 Image 11 88b,c 2.71 1.21 NA
JS-1-37 4 d Image 12 d Image 13 Image 14 77b,c -0.86 NA NA
JS-2-11 5 e Image 15 e Image 16 Image 17 59 5.31 NTi NT
JS-2-14 6 e Image 18 f Image 19 Image 20 49e 4.11 NT NT
JS-2-34 7 e Image 21 g Image 22 Image 23 63 5.15 NT NT
JS-2-36 8 e Image 24 h Image 25 Image 26 85 4.60 NT NT
JS-2-20 9 e Image 27 i Image 28 Image 29 34c,e 5.18 10.92 NA
JS-2-10 10 f Image 30 e Image 31 Image 32 66 6.00 NT NT
JS-2-16 11 g Image 33 e Image 34 Image 35 70f 6.46 NT NT
JS-2-17 12 h Image 36 e Image 37 Image 38 66 6.20 NT NT
AGH-1-09 13 i Image 39 e Image 40 Image 41 58 5.89 NT NT
GMG-1-11 14 i Image 42 g Image 43 Image 44 60c 5.73 NT NT
JS-2-21 15 i Image 45 i Image 46 Image 47 84 5.76 NT NT
JS-2-49 16 e Image 48 j Image 49 Image 50 81 4.16 12.09 NA
JS-2-35 17 e Image 51 k Image 52 Image 53 98 5.20 10.49 NA
AGH-1-08 18 e Image 54 l Image 55 Image 56 60 5.23 NT NT
GMG-1-10 19 e Image 57 m Image 58 Image 59 45e 5.23 NT NT
GMG-1-08 20 i Image 60 l Image 61 Image 62 31e 4.92 NA NA
GMG-1-09 21 i Image 63 m Image 64 Image 65 29e 4.92 NA 32.24
a

Yield reported after purification by flash chromatography on silica (unless indicated otherwise).

b

Isolated pure crude material.

c

Compound reported previously (Garcia Hernandez et al., 2017).

d

After purification by crystallization from methanol.

e

Difficult purification by column chromatography hence the low yield.

f

After purification by recrystallization from hexane : ethyl acetate.

g

Calculated with ChemDraw Professional 15.1.

h

NA = not active.

i

NT = not tested against parasites due to apparent cytotoxicity against mammalian cells.