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Chapter – 5 Synthesis and Characterization…..
5.2 BIOLOGICAL ACTIVITIES ASSOCIATED WITH 4-
ARYLAMINOCOUMARINS AND ITS DERIVATIVES
Spalding et. al. 4 studied 4-morpholino coumarins as analogue of the
camaqauin (quinoline-antimalarial) for antimalarial activity in the plasmodium
gallinaceum infection in chicks, but the compounds were found to be inactive,
while 7-(4-aminosulphonamide) coumarins were found to possess stronger
tubercular activity. 38
Bechmann 39 studied the antibacterial activity of the compounds for the
type shown in Fig. 5.6. 3-nitro-4-(2-pyridylamino) coumarins were tested for
their antimicrobial activity against S. aureus, E. coli and C. alebicans. 40
N
O O
NH
NO 2
Fig. 5.6
O O
Leurquin
41
reported orally active 4-piperazinylcoumarin as
psychotropic compounds.
42, 43
Zagorevskii et. al.
have prepared several 3-nitro-4aminocoumarins
possessing neutropic activity, generally inhibiting
spontaneous locomotor activity and decreasing hypersensitivity induced by
phenamine and prolonging sleep due to a barbiturate drug thiopental.
Zagorevskii 44 further reported weak psychotropic activity in arylamino
coumarin derivatives of the type shown in Fig. 5.7.
Department of Chemistry, Saurashtra University, Rajkot – 360 005 284
HN
N(CH 2 ) 3 Ph