Table 1.
The in vitro Inhibitory Activity of the Monocyclic Compounds against L. donovani.
| Sample Code | L. donavani Promastigotes | L. donavani Amastigotes | L. donavani Amastigotes + THP1 | THP1 cells (Cytotoxicity) | ||||
|---|---|---|---|---|---|---|---|---|
| IC50 (μM) | IC90 (μM) | IC50 (μM) | IC90 (μM) | IC50 (μM) | IC90 (μM) | IC50 (μM) | IC90 (μM) | |
| Pentamidine | 2.93 | 6.52 | 20.42 | >25 | 29.38 | 9.14 | >20 | >25 |
| Amphotericine B | 0.134 | 0.262 | 0.790 | 0.959 | 0.48 | 1.94 | >10 | >10 |
| Bn1Me1Bcyclen (L1) | >20 | >20 | >20 | >20 | >20 | >20 | >20 | >20 |
| [Cu(L1)(OAc)]PF6 | >20 | >20 | >20 | >20 | >20 | >20 | >20 | >20 |
| [Zn(L1)(OAc)]PF6 | >20 | >20 | >20 | >20 | >20 | >20 | >20 | >20 |
| Bn1Me1Bcyclam (L2) | >20 | >20 | >20 | >20 | >20 | >20 | >20 | >20 |
| [Ni(L2)(OAc)]PF6. 0.35NH4PF6 | >20 | >20 | >20 | >20 | >20 | >20 | >20 | >20 |
| [Cu(L2)(OAc)]PF6 | >20 | >20 | >20 | >20 | >20 | >20 | >20 | >20 |
| [Zn(L2)OAc)]PF6 | >20 | >20 | >20 | >20 | >20 | >20 | >20 | >20 |
| Bn2Bcyclen (L3) | 12.68 | 11.44 | 15.14 | 22.29 | >25 | >25 | >25 | >25 |
| Mn(L3)Cl2 | 18.93 | >20 | 11.50 | 17.09 | >20 | >20 | >20 | >20 |
| [Fe(L3)(OAc)]PF6 | >20 | >20 | >20 | >20 | >20 | >20 | >20 | >20 |
| [Ni(L3)(OAc)]PF6 | 10.95 | >20 | >20 | >20 | >20 | >20 | >20 | >20 |
| [Cu(L3)(OAc)]PF6 | >20 | >20 | >20 | >20 | >20 | >20 | >20 | >20 |
| [Zn(L3)(OAc)]PF6 | 4.73 | >20 | 13.64 | >20 | >20 | >20 | >20 | >20 |
| Bn2PBCyclen (L4) | 15.61 | >20 | >25 | >25 | 18.24 | >25 | >25 | >25 |
| [Mn(L4)(C2H3O2)]PF6. 1.9NH4PF6 | >10 | >10 | >10 | >10 | >10 | >10 | >10 | >10 |
| [Fe(L4)(C2H3O2)]PF6. 1.2NH4PF6 | >20 | >20 | >10 | >10 | >10 | >10 | >10 | >10 |
| [Co(L4)(C2H3O2)]PF6. DMF | 20.66 | >20 | >10 | >10 | >10 | >10 | >10 | >10 |
| [Zn(L4)(C2H3O2)]PF6 0.2DMF | 22.92 | >20 | >10 | >10 | >10 | >10 | >10 | >10 |
| CNBQ (L5) | >20 | >20 | >20 | >20 | >20 | >20 | >20 | >20 |
| Mn(L5)Cl2 | 7.40 | 11.46 | >15 | >15 | 8.59 | 10.99 | 13.20 | >15 |
| Fe(L5)Cl2 | 4.13 | 7.07 | >10 | >10 | 3.52 | 5.24 | 3.95 | 8.79 |
| Bis-BQ-Cyclen (L6) | >20 | >20 | >20 | >20 | >20 | >20 | >20 | >20 |
| Bn2Cyclen (L7) | 10.47 | >20 | >25 | >25 | - | 2.8 | >25 | >25 |
| Mn(L7)Cl2 | 2.82 | 9.12 | >20 | >20 | 1.02 | 2.40 | >20 | >20 |
| Fe(L7)Cl2 | 5.50 | 13.09 | >15 | >15 | 1.89 | 6.56 | >15 | >15 |
| Ni(L7)Cl2. 3H2O | 18.63 | >20 | >20 | >20 | >20 | >20 | >20 | >20 |
| Bn2Bcyclam (L8) | 20.81 | >20 | >20 | >20 | 10.06 | 10.43 | >20 | >20 |
| Mn(L8)Cl2 | 21.99 | >20 | >15 | >15 | >15 | >15 | 14.27 | >15 |
| Fe(L8)Cl2 | 7.80 | 20.09 | >15 | >15 | >15 | >15 | >15 | >15 |
| [Co(L8)(OAc)]PF6. H2O | 35.29 | >20 | >15 | >15 | >15 | >15 | >15 | >15 |
| [Ni(L8)(OAc)]PF6 | 6.51 | >20 | >15 | >15 | >15 | >15 | >15 | >15 |
| [Zn(L8)(OAc)]PF6 | 4.73 | >20 | >15 | >15 | >15 | >15 | >15 | >15 |
| Bn2PBCyclam (L9) | 12.98 | 18.97 | 18.54 | 23.11 | 11.10 | 11.43 | 20.63 | 22.80 |
| [Mn(L9)][MnCl4]. CH3CN | 3.48 | 9.11 | 1.50 | 2.68 | 1.89 | 2.17 | 3.49 | 5.90 |
| [Fe(L9)][FeCl4]. H2O | 11.69 | >20 | 10.14 | >14 | 11.93 | >14 | >14 | >14 |
| [Co(L9)(OAc)1.1](PF6)0.9. DMF | 7.98 | >13 | 10.45 | 13.09 | >13 | >13 | >13 | >13 |
| [Ni(L9)(OAc)1.1](PF6)0.9. DMF | 9.33 | >13 | 10.12 | 12.96 | >13 | >13 | >13 | >13 |
| [Zn(L9)(OAc)]PF6.0.3NH4PF6 | 8.17 | 10.50 | 9.91 | 13.48 | 7.81 | 8.53 | >14 | >14 |
| Bn2Cyclam (L10) | 9.40 | 17.84 | >25 | >25 | 12.93 | 13.19 | >25 | >25 |
| Mn(L10)Cl2. H2O | 6.62 | 12.36 | >19 | >19 | 12.36 | 12.68 | >19 | >19 |
| Fe(L10)Cl2. 0.5 H2O | 5.64 | 13.91 | >19 | >15 | 9.61 | 9.68 | >19 | >19 |
| [Co(L10)(OAc)](PF6). H2O | >15 | >15 | >15 | >15 | >15 | >15 | >15 | >15 |
| Cu(L10)(OAc)](PF6). H2O | >20 | >20 | >15 | >15 | >15 | >15 | >15 | >15 |
| [Zn(L10)(OAc)]PF6. 0.1H2O | 5.65 | 11.28 | >15 | >15 | 6.80 | 7.04 | >15 | >15 |