A new series of 2-(4- and 3-substituted phenyl)-3-[3-(N,N-dimethylamino) propyl]-1,3-thiazolidin-4-ones were synthesized, characterized, and evaluated for their ability to inhibit the contractions induced by histamine on guinea pig ileum. The measurement of pA2 values suggested that the reported compounds showed H1-antagonism. The more active compounds 5, 9, and 13 exhibited activity close to that of mepyramine.

Synthesis and Antihistaminic Activity of Some Thiazolidin-4-ones.-Consecutive condensation reaction of the aromatic aldehydes (I) with the diamine (II) and α-mercaptoacetic acid (III) yields the thiazolidin-4-ones (IV). The compounds (IVc), (IVd), and (IVf) show an activity close to that of mepyramine concerning the ability to inhibit histamine-induced contractions on guinea pig ileum. -(DIURNO, M. V.; MAZZONI, O.; PISCOPO, E.; CALIGNANO, A.; GIORDANO, F.; BOLOGNESE, A.; J. Med. Chem. 35 (1992) 15, 2910-2912; Univ. Napoli Federico II, Fac. Farm.,

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.

Synthesis and Antimicrobial Activity of 1,3,4-Triaryl-2-azetidinones.-Heating of the 4,4'-disubstituted benzylideneanilines (I) with equimolar amounts of phenylacetic acid (II) and phosphoryl chloride leads to the formation of the 1,3,4-triaryl-2-azetidin-2-ones (III). These are subjected to antibacterial screening procedures against gram-positive and gram-negative bacteria and fungi, epecially (IIIc) and ( IIIe) show activity against Pseudomonas aeruginosa. -(DIURNO, M. V.; MAZZONI, O.; PISCOPO, E.; BOLOGNESE, A.; Farmaco, Ed.

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.