Reaction of methylene-bis [5-hydroxyfurocoumarins] with amines and hydrazines

Fusion of 6, 6'-methylene-bis-[5-hydroxybergapten] [IIIa] or [5- hydroxyisopimpinellin] [IIIb] with aromatic amines and hydrazine hydrate led to the formation of 6, 6'-methylene-bis-[5-amino] [IVa-f] or [5-hydrazino] [IVg], h] derivatives. On the other hand, when IIIa or IIIb were refluxed with aliphatic amines, cleavage of the methylene bridge followed by opening of the coumarin ring occurred to give the corresponding alpa-substituted acetamides [Va-d]. Fusion of IIIa or IIIb with phenylhydrazine also led to the methylene bridge followed by opening of the coumarin ring to form VIa, b. The reaction of 5- hydroxybergapten or 5-hydroxyisopimpinellin with propylamine or benzylamine in ethanol led to the respective 5-amino-derivatives [VIIa-c]. The antimicrobial activity of compounds IVa, b, e, f, Va, b, d and VIa, b has been tested. Only compound Vb showed a broad spectrum activity

Some amino derivatives of 4-substituted -a-phenylpropiophenones and their antimicrobial activity

Aminomethylation of p-CH3OC6H4 COCH2C6H5 [I] using formaldehyde solution and different amines gave the corresponding new 4-methoxy- alpha-phenyl-beta-aminopropio-phenone derivatives III a-c. The Mannich reaction was run for p-HOC6H4 COCH2C6H3 [II] using different amines to yield the new [IV a-d]. Glyoxalic acid may replace formaldehyde in the Mannich reaction of II with morpholine to produce the new morpholinium salt V of the corresponding amino acid. Hydrolysis of the salt gave the unsaturated acid VI which was esterified to the ester VII. Compound IIIc was found to be active against gram positive bacteria [Bacillus subtilus], IVd and VI found to be active against fungi [A. niger], whileas VI and VII found to be active against gram negative bacteria [E. coli]

Synthesis and pharmacological studies of new pyridopyrazole derivatives

New derivatives of pyrido [2, 3-c] pyrazoles were prepared. Compounds 4a, 6, 8a, b and 14 were tested along with the previously reported pyranopyrazole derivatives 16-20 on the albino Swiss mice to study their effect on the blood constituents and on the glucose and cholesterol levels. Among the investigated compounds, 4a and 8a were found to be highly potent beside the pronounced activity of the others