Synthesis and biological evaluation of new 2-azetidinones with sulfonamide structures.

New series of N-(arylidene)hydrazinoacetyl sulfonamides 4a1-6, 4b1-6 and N-(4-aryl-3-chloro-2-oxoazetidin-1-yl)aminoacetyl sulfonamides 5a1-6, 5b1-6 were synthesized. The structures of the new derivatives was confirmed using spectral methods (FT-IR, 1H-NMR, 13C-NMR). The antibacterial activities of these compounds against Gram positive (Staphylococcus aureus ATCC 6583, Staphylococcus epidermidis ATCC 12228, Enterococcus faecalis ATCC 25912) and Gram negative (Klebsiella pneumoniae CIP 53153, Proteus vulgaris CIP 104989, Citrobacter freundii CIP 5732, Enterobacter cloacae CIP 103475, Escherichia coli ATCC 25922, Pseudomonas aeruginosa CIP 82118) bacterial strains were evaluated using the broth micro-dilution method. Compound 4a2 displayed the highest antibacterial activity, especially against Staphylococcus epidermidis, Enterococcus faecalis and Pseudomonas aeruginosa. The antioxidant potential of the synthesized compounds was also investigated according to ferric reducing power, total antioxidant activity and DPPH radical scavenging assays. All tested compounds showed excellent antioxidant activity in comparison with sulfadiazine and sulfisoxazole which were used as parent sulfonamides. Moreover, some of them showed an antioxidant activity comparable with that of ascorbic acid. In general, the compounds designed based on a sulfadiazine skeleton (compounds 4a1-6, 5a1-6) are more active than those obtained from sulfisoxazole (compounds 4b1-6, 5b1-6), and the N-(arylidene)hydrazinoacetyl sulfonamide derivatives 4a1-6, 4b1-6 are more active than their azetidionone analogues 5a1-6, 5b1-6.

Bacteriological agents which play a role in the development of infertility.

This study was carried out to determine the prevalence of the bacterial agents Chlamydia trachomatis (C. trachomatis), Neisseria gonorrhoeae (N. gonorrhoeae), Mycoplasma hominis (M. hominis) and Ureaplasma urealyticum (U. urealyticum) and the conditions which may play a role in the development of female infertility, in the county of Iasi in North-Eastern Romania. Cervical and blood samples were collected from 176 infertile women and 45 pregnant women in the third trimester. Classical methods and real time PCR were applied to each cervical sample to detect the presence of these sexually transmitted microorganisms; the ELISA method was applied to blood samples to detect C. trachomatis antibodies (IgA, IgM and IgG). The proportion of C. trachomatis IgG was significantly higher in the infertile group (23.8%) than in the pregnant group (4.4%), p < 0.05. For C. trachomatis antigen (Ag) and N. gonorrhoeae Ag no differences were observed between the two groups. The prevalence of mycoplasma genital infections was higher in the pregnant group (U. urealyticum - 53.3% and M. hominis - 20%) than in the infertile group (U. urealyticum - 39.7% and M. hominis - 7.3%). Higher rate of co-infection with C. trachomatis and mycoplasma were observed among the infertile women (25.7%) than among the pregnant women (7.7%). This combination could be involved in the appearance of pelvic inflammatory disease (PID) and its sequela, including infertility. C. trachomatis IgG determination still remains the gold standard for the diagnosis of PID and should be used as a screening test for the prediction of tubal damage in infertile women. In view of the large number of cases involving the co-existence of genital infections with C. trachomatis, M. hominis and U. urealyticum, it is clearly necessary to perform screening for all three microorganisms among all women of reproductive age but especially those who are infertile.