Benzothiazole analogs (1-20) have been synthesized, characterized by EI-MS and (1)H NMR, and evaluated for urease inhibition activity. All compounds showed excellent urease inhibitory potential varying from 1.4±0.10 to 34.43±2.10μM when compared with standard thiourea (IC50 19.46±1.20μM). Among the series seventeen (17) analogs 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 16, 17, and 18 showed outstanding urease inhibitory potential. Analogs 15 and 19 also showed good urease inhibition activity. When we compare the activity of N-phenylthiourea 20 with all substituted phenyl derivatives (1-18) we found that compound 15 showed less activity than compound 20 having 3-methoxy substituent. The binding interactions of these active analogs were confirmed through molecular docking.
The objective of this study was to evaluate the effects of solid-to-solvent ratio (1:5. 1:10, 1:15 and 1:20) on the extraction of phenolic compounds (TPC and TFC) and antioxidant capacity (ABTS and DPPH radical scavenging capacity) of P. niruri. Solid-to-solvent ratio showed a significant effect for both phenolic compounds (TPC and TFC) and antioxidant capacity (ABTS and DPPH radical scavenging capacity) with 1:20 was the condition for extracting the highest of phenolic compounds (TPC and TFC) with a value of 5788.7 mg GAE/100 g DW and 1906.5 mg CE/100 g DW, respectively and exhibited high antioxidant capacities (ABTS and DPPH radical scavenging capacities) with a value of 0.820 mM and 1.598 mM, respectively among the four levels studied. TPC was positively and significantly correlated with ABTS and DPPH (r=0.999 and r=0.999) under the effects of solid-to-solvent ratio as compared to TFC, positively and strongly correlated (r=0.865 and r=0.868) with ABTS and DPPH.