Mohamad S. I. Makki

Synthesis of Novel Cyclic Benzenesulfonylurea and Thiourea Derivatives

Treatment of the pyrazoline derivatives (1-6) with isocyanates or isothiocyanates afforded ureas (7-18) and thioureas (19-32) in a good yield. Subsequent treatment of the benzenesulfonylthioureas (19-32) with f - and g -halogenocarbonyl compounds gave the corresponding thiazolidines (33-41) and 1,3-thiazinones (42-46) respectively. When urea derivatives (7-18) were reacted with dimethyl malonate in sodium ethoxide, they gave the corresponding pyrazolebarbiturate derivatives (53-56) . The structure of the isolated product were determined by the spectral methods.

Synthesis, photophysical and antimicrobial activity of new water soluble ammonium quaternary benzanthrone in solution and in polylactide film

The synthesis of a new cationic water soluble fluorescent 1-[(7-oxo-7H-benzo[de]anthracen-3-ylcarbamoyl)-methyl]-triethylammonium chloride (B) has been described. Due to the presence of the quaternary amino group, the compound is soluble in water. Its photophysical characteristics in aqueous solution and organic solvents with different polarity have been determined using absorption and fluorescence spectroscopy. The photostability of compound B has been investigated in aqueous media. The newly synthesized compound has been tested in vitro for its antimicrobial activity against eight bacterial and two yeasts cultures. The results obtained suggest that the newly synthesized compound is effective in treating the relevant pathogens and is suitable in designing new effective antimicrobial preparations. The incorporation of the compound into thin polylactic acid film and its release into water solution has been also investigated. It was demonstrated that the compound released from the polymer polylactic acid matrix exhibited a prolonged good antibacterial activity.

SYNTHESIS AND REACTIONS OF SOME ETHYL 3(5)AROYL-4-ARYL-2-PYRAZOLINE-5(3)CARBOXYLATES

A series of ethyl 3-aroyl-4-aryl-2-pyrazoline-5-carboxylates 1 was prepared. Their reactions with bromine water, potassium permanganate and potassium hydroxide afforded the corresponding pyrazoles. With aryl and aroyl hydrazines the pyrazolines 1 gave the Schiff bases 9 while with hydrazine hydrate they yielded the corresponding acid hydrazides 11. Condensation of 11 with aromatic aldehydes gave the arylidene derivatives 12, which on cyclization with the proper reagent afforded 13 or 14. Reaction of 1 with hydrochloric acid gave the corresponding dipyrazolo-pyrazine derivatives 10

4-(3-Methyl-4,5-dihydro-1H-benzo[g]indazol-1-yl)benzene-sulfonamide.

In the title compound, C18H17N3O2S, the aromatic ring bearing the sulfamide unit is aligned at 61.65 (1)° with respect to the pyrrole ring; its amino group forms N—H⋯N and N—H⋯O hydrogen bonds to neighboring molecules, generating sheets in the ac plane.