In-vitro Preliminary Evaluation of Antioxidant and Anticoagulant Activity of Novel N-Phenyl Hydrazine 1-Carbothioamide Derivatives of (2-Methyl-3-(Substituted Thio)Propanoyl) Proline

Abstract

A series of (2-methyl-3-(substituted thio)propanoyl)proline (2 to 7) were evaluated in-vitro for antioxidant activity and anticoagulant activity. The antioxidant were determined using the most common models, 2,2-Diphenyl-1-picrylhydrazyl (DPPH), H2O2, and reducing power method. The better radical scavenging antioxidant activity was observed with compound (4) with % inhibition (93.04 ± 0.7 μg\mL and IC50 69.56 μg\mL), using the DPPH method, while with H2O2 model, the observed % inhibition for compound (4) was (92.18 ± 1.52). For reducing power assay, the absorbance of the formed complex at 700 nm was (1.245 ± 0.213). The anticoagulant activity of the compound (3) shows significant prolongation in clotting time compare with (3-mercapto-2-methylpropanoyl) proline (captopril) with Prothrombin time (PT) and Activated partial thromboplastin time (aPTT) values (17.1 ± 0.1 s and 75.13 ± 0.15 s), respectively. The results of this study refer to an improvement of the biological activity of novel captopril derivatives with the introduction of electron donated group as (NH) and the presence of free thiol group.