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

From: Therapeutic potential of heterocyclic pyrimidine scaffolds

Compounds In vitro assessment Selectivity index CC50/IC50 In vivo activity (dose—50 mg/kg × 5 days, ipb) % Inhibition ± SD
IC50 (µM) CC50 (µM)
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
SSGa 59.8 ± 7.5 > 400 ± 0 > 7 88.5 ± 4.4
Miltefosinec 12.5 ± 0.9 54.7 ± 6.9 4 98.1 ± 1.0
  1. IC50 and CC50 values are the mean ± SD of two independent experiments
  2. The selectivity index is defined as the ratio of CC50 on vero cells to IC50 on L. donovani intramacrophagic amastigotes
  3. aSSG = sodium stibogluconate (40 mg/kg × 5 days, ip)
  4. bip = intraperitonial; c Miltefosine (30 mg/kg × 5 days, po) used as a reference drugs