2-Arylaminoquinoxalines were prepared by the condensation of 2-chloroquinoxaline with the appropriate Mannich bases in the presence of HCl. To synthesize the Mannich bases, 4-acetamidophenol was reacted with formaldehyde and dialkylamine to yield 3-[(dialkylamino) methyl]-4-hydroxyacetanilide, followed by hydrolysis. Antimalarial activities of the new arylaminoquinoxalines were evaluated against the rodent malaria parasite Plasmodium yoelii at a dose of 75 mg kg(-1). Three compounds synthesized (2-[3-[(diethylamino) methyl]-4-hydroxyanilino]-quinoxaline dihydrochloride (2b), 2-[3-[(pyrrolidinyl) methyl]-4-hydroxyanilino]-quinoxaline dihydrochloride (2f), and 2-[3-[(piperidinyl) methyl]-4-hydroxyanilino]-quinoxaline dihydrochloride (2g)) showed moderate antimalarial activity.
Antimicrobial activity of methanolic extracts of plants was screened by disc diffusion assay against four bacteria and four fungal cultures. Streptomycin (10 µg/disc) and nystatin (10 µg/disc) are used as standards for bacteria and fungi respectively. Minimum inhibitory concentration (MIC) of the extracts was evaluated through micro broth dilution method. The antimicrobial potency of plant extracts was assessed by their zone of inhibition and activity index values. Total activity of extracts was evaluated to quantitatively compare the activity of two plants. Methanolic extract of Cleome gynandra showed maximum antibacterial activity against Staphylococcus aureus (IZ-22 ± 0.22 mm, AI-0.917, MIC-0.039 mg/mL, MBC-0.039 mg/mL). Maximum antifungal potential was shown by C. chelidonii against Candida albicans (IZ-25 ± 0.92 mm, AI-1.000, MIC-0.039 mg/mL, MFC-0.039 mg/mL). Both the extracts exhibited good antimicrobial activity with low range of MIC.
The extract showed a dose-dependent, non-specific relaxation of pre-contracted isolated guinea pig trachea. The non-specific relaxant effect of the extract may be due to its ability to modulate calcium activity.
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