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. 2019 Aug 23;14(18):1662–1668. doi: 10.1002/cmdc.201900370

Table 1.

In vitro activity of pyrazolone dimers against intracellular amastigotes of T. cruzi (Tulahuen strain) and on MRC‐5 cell growth by phenyldihydropyrazolone dimers with modifications on the phenyl ring.

graphic file with name CMDC-14-1662-g006.jpg
Compd R1 pIC50 [a]
4‐ 3‐ 2‐ T. cruzi MRC‐5
3 Br H H 5.4 <4.2
7 a H Br H <4.2 <4.2
7 b H H Br <4.2 <4.2
7 c H H H <4.2 <4.2
7 d Cl H H 5.3 5.1
7 e H Cl H <4.2 <4.2
7 f H H Cl <4.2 <4.2
7 g F H H <4.2 <4.2
7 h H F H 5.2 4.4
7 i H H F 4.3 <4.2
7 j OMe H H 5.0 <4.2
7 k H OMe H 5.1 4.4
7 l H H OMe <4.2 <4.2
7 m NMe2 H H <4.2 <4.2
7 n H NMe2 H <4.2 <4.2
7 o CN H H <4.2 <4.2
7 p H CN H <4.2 <4.2
7 q OMe F H 5.2 <4.2
7 r OMe Cl H 5.9 <4.2
7 s OMe Br H 6.4 <4.2
7 t Cl OMe H <4.2 <4.2
7 u Br OMe H <4.2 <4.2
7 v OMe OMe H 4.3 <4.2
7 w F F H 5.1 <4.2

[a] All reported values are within a standard deviation of ±0.2.