Therapeutic potential of heterocyclic pyrimidine scaffolds

BMC Chemistry

Table 48 In vitro and in vivo antileishmanial activity and cytotoxicity results of synthetic pyrimidine derivatives

Compounds	In vitro assessment		Selectivity index CC₅₀/IC₅₀	In vivo activity (dose—50 mg/kg × 5 days, ip^b) % Inhibition ± SD
Compounds	IC₅₀ (µM)	CC₅₀ (µM)	Selectivity index CC₅₀/IC₅₀
g1	2.0 ± 0.1	375.9 ± 5.1	188	88.4 ± 10.6
g2	0.5 ± 0.1	57.8 ± 5.9	116	78.1 ± 17.7
g3	2.7 ± 0.5	345.4 ± 19.6	128	78.2 ± 4.4
SSG^a	59.8 ± 7.5	> 400 ± 0	> 7	88.5 ± 4.4
Miltefosine^c	12.5 ± 0.9	54.7 ± 6.9	4	98.1 ± 1.0

IC₅₀ and CC₅₀ values are the mean ± SD of two independent experiments
The selectivity index is defined as the ratio of CC₅₀ on vero cells to IC₅₀ on L. donovani intramacrophagic amastigotes
^aSSG = sodium stibogluconate (40 mg/kg × 5 days, ip)
^bip = intraperitonial; ^c Miltefosine (30 mg/kg × 5 days, po) used as a reference drugs

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