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. 2019 Jun 21;10(9):1599–1605. doi: 10.1039/c9md00298g

Table 2. In vitro antimalarial activity and yield of alkylated thiosalicylic acid derivatives and of 1,2,3-triazolyl thiosalicylic acid derivatives.

Entry Cmpd R Yield (%) P. falciparum a IC50 μM Z value R 2
1 1 Propargyl 81 >200 graphic file with name c9md00298g-u1.jpg
2 1a Cyclohexyl 87 >200
3 1b Benzyl 73 >200
4 1c 3-Phenyl-propyl 75 >200
5 1d Cinnamyl 68 >200
6 1e Octyl 83 >200
7 1f Decyl 81 >200
8 1g CH2CH2CO2CH2CH3 78 >200
9 1h Prenyl 72 >200
10 1i Geranyl 88 >200
11 1j Farnesyl (Salirasib) 79 20.34 ± 5.52 0.93 ± 0.06 0.95 ± 0.02
12 1k Phytyl 85 13.40 ± 1.53 0.93 ± 0.06 0.98 ± 0.02
13 2a Cyclohexyl 84 >200 graphic file with name c9md00298g-u2.jpg
14 2b Benzyl 80 >200
15 2c 3-Phenyl-propyl 88 >200
16 2d Cinnamyl 86 65.33 ± 10.71 0.89 ± 0.09 0.87 ± 0.01
17 2e Octyl 78 >200
18 2f Decyl 88 >200
19 2g CH2CH2CO2CH2CH3 91 >200
20 2h Prenyl 89 >200
21 2i Geranyl 84 >200
22 2j Farnesyl 90 25.97 ± 1.32 0.94 ± 0.06 0.96 ± 0.02
23 2k Phytyl 83 9.75 ± 1.97 0.92 ± 0.06 0.98 ± 0.01
24 2l CH2CO2CH2CH3 92 >200
25 2m Cetyl 81 14.44 ± 5.43 0.93 ± 0.06 0.97 ± 0.01
26 2n Tridecanyl 55 19.83 ± 5.14 0.88 ± 0.08 0.97 ± 0.02
27 2o 2-Phenyl-ethyl 94 >200
28 2p 2-Naphthylmethyl 33 20.54 ± 5.45 0.92 ± 0.06 0.96 ± 0.04
CQ 8.15 ± 1.83 nM 0.75 ± 0.18 0.96 ± 0.02
ART 1.64 ± 0.08 nM 0.86 ± 0.11 0.96 ± 0.03

aEvaluated by the NanoLuc luciferase method.