ABSTRACT
Condensation of carbohydrazide derivatives Ia, b with dimethyl acetylenedicarboxylate and acetylenedicarboxylic acid yielded benzofuran derivatives II a-d. Reaction of Ib with aromatic aldehydes formed products III a-d. Treatment of compounds III a-d with mercaptoacetic acid yielded the cyclocondensation products (IVa-d). Phthalic anhydride reacted with compounds (Ia, b)to form products (Va, b). It has been found that both khellin and visnagin (VIa, b)react with aromatic aldehydes to give arylidene derivatives (VIIa-e). Condensation of diphenyl nitrilamine with 2-arylidene furochromones VII derivatives afforded cyclo-adducts (VIII a-i). The antibacterial activities of the selected compounds were tested against Staphylococcus aureus, B. subtilis, E. coli, Pseudomonas, Salmonella and Erwinia with good results.
Subject(s)
Anti-Bacterial Agents/chemical synthesis , Anti-Bacterial Agents/pharmacology , Bacteria/drug effects , Oxazoles/chemical synthesis , Oxazoles/pharmacology , Phthalimides/chemical synthesis , Phthalimides/pharmacology , Thiazoles/chemical synthesis , Thiazoles/pharmacology , Chemical Phenomena , Chemistry, Physical , Indicators and Reagents , Khellin/chemistry , Magnetic Resonance Spectroscopy , Microbial Sensitivity Tests , Spectrophotometry, InfraredABSTRACT
Schiff bases 3a-j were prepared by reacting the beta-enaminonitriles (1a,b) with the appropriate hetarylcarboxaldehyde, in boiling ethanol. Structural elucidations for the new compounds (3a-j) were based upon compatible analytical and spectroscopic results. Compounds 1a, 1b, 3a, 3c, 3d and 3i were tested for their anti-inflammatory and ulcerogenic activities.
Subject(s)
Anti-Inflammatory Agents, Non-Steroidal/chemical synthesis , Furans/chemical synthesis , Nitriles/chemical synthesis , Schiff Bases/chemical synthesis , Stomach Ulcer/chemically induced , Animals , Anti-Inflammatory Agents, Non-Steroidal/pharmacology , Anti-Inflammatory Agents, Non-Steroidal/toxicity , Carrageenan , Edema/chemically induced , Edema/drug therapy , Furans/pharmacology , Furans/toxicity , Male , Nitriles/pharmacology , Nitriles/toxicity , Rats , Schiff Bases/pharmacology , Schiff Bases/toxicity , Spectrophotometry, Infrared , Stomach Ulcer/pathologyABSTRACT
The Friedel-Craft's acylation of 2,3-diphenyl-5-methylbenzofuran 1a with succinic anhydride gives beta-(2,3-diphenyl-5-methylbenzofuranoyl)propionic acid 1b. Acid 1b reacts with hydrazines yielding the corresponding tetrahydropyridazinones 2. 4,5-Dihydro-1,2-oxazin-6H-6-one 6 is formed by reaction of 1b with hydroxylamine hydrochloride. The reaction of the pyridazinone 2a with dialkyl sulfates, ethyl chloroacetate, Grignard reagents, amines in presence of formaldehyde (Mannich reaction), o-amino-phenol and thiourea has been investigated. The antimicrobial activities of compounds 1a-c, 2a-c, e, f, 4a, b and 5a, b as well as 7b are studied.
Subject(s)
Anti-Infective Agents/chemical synthesis , Benzofurans/chemical synthesis , Anti-Bacterial Agents , Bacteria/drug effects , Benzofurans/pharmacology , Chemical Phenomena , Chemistry , Fungi/drug effects , Microbial Sensitivity TestsABSTRACT
A TOTAL of 204 cases with acute viral hepatitis were studied: 93 bilharzial and 111 non-bilharzial. This study is concerned with the 106 cases showing positive HBS Ag test. Follow up of the cases after discharge from the Fever Hospital was carried out by repeated clinical and laboratory examinations 3 montly in the first year and 6 monthly subsequently. The bilharzial and non-bilharzial patients were found to be equally susceptible to HBS Ag positive hepatitis (p=0.25). However, antigenaemia tended to last longer as a whole in the bilharzial patients (p=0. 005) and was not affected by successful specific antibilharzial treatment. It seems that bilharzial infection predisposes to "retention" of HBs antigen, after subsidance of the acute attack, thus increasing the volume of reservoir for HB virus in our rural community.