A small collection of 2-hydroxy-N-(5-methyl/nonsubstituted 4-oxo-2-substituted phenyl-1,3-thiazolidin-3-yl)-2-phenylacetamides (3-16) was synthesized from the cyclocondensation of 2-hydroxy-2-phenyl-N'-[(substitutedphenyl)methylene]acetohydrazides (2) and mercaptoethanoic acid or 2-mercaptopropanoic acid, characterized with spectral and elemental analysis. In order to explore their antimycobacterial potential, newly synthesized fourteen compounds were screened for their inhibitory activity against Mycobacterium tuberculosis strain H37Rv at 6.25 μg/mL with in-vitro primary tests. Compound 7 was found to provide the highest inhibition (98%) M. tuberculosis strain H37Rv, while most of the new derivatives showed different inhibition ratios. For the search of the putative targets which are considered as related to the antimycobacterial activity of these molecules, docking studies were performed. With molecular dynamic simulations, further possible interactions between ligands and the active site of the selected enzymes were investigated. Eventually, molecular modelling studies indicated that at least part of the mechanism of action of these compounds may be mediated by inhibition of MtInhA.

Tumor cells benefit from some certain signals, which are referred to as “immune checkpoints”, to escape immune-mediated destruction. With that in mind, it is believed that the blockade of these points, such as programmed cell death Ligand-1 (PD-L1) and programmed cell death 1 (PD-1), can restore an adaptative immune response against tumoral cells. In this study, we have designed and synthesized some novel peptidomimetics with a 2-aminobenzathiazole scaffold, which targets the PD-1/PDL-1 pathway. In the viability assay, it was found that these compounds decreased the proliferation of peripheral blood mononuclear cells in the concentration of 10 uM. Overall, our results indicate that these novel compounds are potential checkpoint inhibitors for cancer immunotherapy.rnrn

Tumor cells benefit from some certain signals, which are referred to as “immune checkpoints”, to escape immune-mediated destruction. With that in mind, it is believed that the blockade of these points, such as programmed cell death Ligand-1 (PD-L1) and programmed cell death 1 (PD-1), can restore an adaptative immune response against tumoral cells. In this study, we have designed and synthesized some novel peptidomimetics with a 2-aminobenzathiazole scaffold, which targets the PD-1/PDL-1 pathway. In the viability assay, it was found that these compounds decreased the proliferation of peripheral blood mononuclear cells in the concentration of 10 uM. Overall, our results indicate that these novel compounds are potential checkpoint inhibitors for cancer immunotherapy.