Background and purpose: Isatin derivatives have excited attention due to their biological attractions, especially, anticancer properties. Isatin analogs such as semaxanib and sunitinib were exposed to tyrosine kinase inhibitory properties. N-substituted isatins were reported to show cytotoxic activity. On the other, the extension of impressive and cost-effective agents against leishmaniasis is necessary in third-world countries. The capability of isatin derivatives to create novel anticancer and anti-leishmanial compounds has been identified in medicinal chemistry research. The current study aimed to synthesize N-alkyl-isatin-3-imino aromatic amine compounds and evaluate their biological effects. Experimental approach: Synthesis started with the formation of 2-chloro-N-phenylacetamide derivatives by the reaction of aniline derivatives with chloroacetyl chloride. N-alkylation of isatin was performed in the presence of K2CO3 in N, N-dimethylformamide. Final products were prepared via the condensation of N-alkyl isatin derivatives with aromatic amines. Cell viability was checked out by using the MTT assay against cancer cells. Final compounds were screened for anti-leishmanial activity. The molecules were docked in the active sites of the epidermal growth factor receptor tyrosine kinase to define the possible interactions. Findings/Results: Compounds 5c and 4d with IC50 value of 50 µM showed cytotoxic activity on the MCF-7 cell line. Compound 5b presented anti-leishmanial activity against promastigote form after 48 h (IC50: 59 µM) and 72 h (IC50: 41 µM) incubations. The highest docking score was-7. 33 kcal/mol for compound 4d. Conclusions and implications: The nature of substitution in the N1 region of isatin seems to be able to influence the cytotoxic activity. Based on the obtained results of docking and cytotoxic tests, compound 4d seems to be a good compound for further investigations.

This study discusses the preparation of new series of tetra-dentate complexes Cu (II), Ni (II), Co (II), Zn (II), and Cr (III) complexes with Schiff base (ligand tetradentate) derived from isatin with 2-aminobenzohydrazide, characterized by IR spectroscopy, mass spectra, UV-Vis, 1H-NMR and elemental microanalysis. The complexes Cu (II), Ni (II), Co (II), Zn (II), and Cr (III) were characterized using IR spectroscopy, UVVis, magnetic susceptibility, conductive, elemental microanalysis and metal analysis by atomic absorption. The proposed structures of complexes from the all measurements showed that Ni (II), Co (II), Zn (II), and Cr (III) have octahedral shape and Cu (II) has square planer shape. Bioactivity of the Schiff base and complexes were assessed examined with antibacterial activity. Studies were conducted to assess the growth-inhibiting potential of the complexes synthesized, and the ligands, against various bacterial strains.

Objective(s): Depression is a prevalent psychiatric disorder. Treatment of depression is still a challenge due to the lack of response of some patients to a variety of available medications and side effects. Isatin is an interesting molecule with diversified biological effects. It also participates in many synthetic reactions, as a precursor molecule. In this study, a new series of N-alkyl and N-benzyl isatin derivatives bearing Schiff bases were synthesized and screened for antidepressant activities in mice. Materials and Methods: The synthesis was initiated by N-alkylation and N-benzylation of isatin by an alkylation reaction to give N-substituted isatins. 2-(Benzyloxy) benzohydrazide derivatives were synthesized by treating methyl2-hydroxybenzoate with benzyl bromide or 4-chlorobenzyl bromide which was followed by a reaction with hydrazine hydrate to provide acid hydrazide derivatives. The final compounds were obtained by condensation of N-substituted isatins with 2-(benzyloxy) benzohydrazide derivatives as Shiff-base products. Compounds were evaluated for antidepressant activities in mice by the locomotor activity, marble burying test, and forced swimming test. Monoamine oxidase–, A (MAO–, A) enzyme has been used for molecular docking studies. Results: Compounds 8b and 8e in both doses, and 8 c in the lower dose, reduced immobility time during the forced swimming test relative to the control group. All preparations reduced the number of marbles buried compared with the control group. The highest docking score was-11. 01 kcal/mol for compound 8e. Conclusion: N-Benzylated-isatin (8b, 8e) and N-acetic acid ethyl ester-isatin derivatives (8c) showed more effective antidepressant activity compared with N-phenyl acetamide isatin derivatives. Docking results relatively confirm the pharmacological results.