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. Author manuscript; available in PMC: 2024 Jun 10.
Published in final edited form as: J Med Chem. 2024 May 9;67(10):8323–8345. doi: 10.1021/acs.jmedchem.4c00517

Table 4.

In Vitro Antileishmanial Activity of TAs (110–116) with Modifications on Ring-A and Terminal Amine.

survival (%) at 0.1 μMa
vs		 EC50 (nM)a
vs
compound structure L.mexicana
amastigote		 J774A.1
macrophage		 L.mexicana
amastigote		 J774A.1
macrophage		 TI
110 graphic file with name nihms-1993233-t0101.jpg 3.7 ± 1.0 71.2 ± 20.5 40.9 ± 19.6 1140 ± 498 28
111 graphic file with name nihms-1993233-t0102.jpg 2.3 ± 0.1 74.5 ± 15.7 44.3 ± 24.7 1237 ± 130 28
112 graphic file with name nihms-1993233-t0103.jpg 1.3 ± 0.4 53.6 ± 14.8 31.4 ± 12.6 573 ± 63.4 18
113 graphic file with name nihms-1993233-t0104.jpg 23.8 ± 4.3 63.3 ± 26.0 117 ± 47.4 1328 ± 73.5 11
114 graphic file with name nihms-1993233-t0105.jpg 43.8 ± 7.5 56.8 ± 15.9 182 ± 80.7 ND ND
115 graphic file with name nihms-1993233-t0106.jpg 12.5 ± 3.00 93.2 ± 50.4 46.5 ± 12.0 667 ± 473 14
116 graphic file with name nihms-1993233-t0107.jpg 10.7 ± 5.4 63.5 ± 16.2 54.0 ± 15.5 675 ± 459 12
miltefosine - 0.020 ± 0.010 39.2 ± 5.1 3460 ± 781 >100000 ± 0.0 > 29
a

Data represent the mean ± standard deviation of results of at least two independent experiments; an error of 0.0 indicates identical values were obtained for each replicate; TI = Therapeutic Index (J774A.1 EC50/L. mexicana EC50); ND, not determined.