Efficient Electrochemical N-Alkylation of N-Boc-Protected 4-Aminopyridines: Towards New Biologically Active Compounds

Table 5

Anti-parasitic activity of selected di-alkylated 4APs.

		T. cruzi^a; IC50  𝜇M	T. brucei^b; IC50  𝜇M	L. inf^c; IC50  𝜇M	Pf-K1^d; IC50  𝜇M	MRC-5; IC50  𝜇M
	Reference drug	Benznidazole; (IC50 = 1.95)	Suramine; (IC50 = 0.02)	Miltefosine; (IC50 = 10.4)	Chloroquine; (IC50 = 0.14)	Tamoxifen; (IC50= 15.2)
3cc		20.16	31.54	8.06	1.59	39.01
3ee		9.57	28.23	8.64	1.87	30.09
3ff		2.44	6.62	2.16	1.33	7.65

aT. cruzi Tulahuen C4 amastigote stage. ^bT. brucei rhodesiense STIB 900 trypomastigote stage. ^cL. donovani MHOM-ET-67/L82 amastigote stage. ^dP.  falciparum K1 IEF.