Post-surgical hallux varus. A case report.

Sometimes a hallux varus occurs as a consequence of the treatment for a hallux valgus, determined by an alteration of the balance between the muscolo-ligamentous structure which crosses the first metatarso-phalangeal joint. This complication is poorly tolerated by patients. Various operations have been proposed to correct the varus, which includes the bone and the soft tissue. A clinical case has been presented which uses a split extensor hallucis longus transfer, distally sectioned and made to pass under the deep transverse intermetatarsal ligament, used as a pulley, and through a tunnel made in the bone at the proximal-lateral base of the proximal phalanx, and then tensioned and sutured to its medial side.

Synthesis and antiproliferative activity of 3-aryl-2-(1H-benzotriazol-1-yl)acrylonitriles. Part III.

A new series of 30 3-aryl-2-(1H-benzotriazol-1-yl)acrylonitriles were synthesized and tested for biological activity as part of our research in the antimicrobial and antitumor fields. In particular, title compounds were evaluated in vitro against representative strains of Gram-positive and Gram-negative bacteria (S. aureus, Salmonella spp), mycobacteria (M. fortuitum, M. smegmatis ATCC 19420 and M. tuberculosis ATCC 27294), yeast and mould (C. albicans ATCC 10231 and A. fumigatus). Furthermore, their antiretroviral activity against HIV-1 was determined in MT-4 cells together with cytotoxicity. In these assays title compounds and 47 additional derivatives described previously (P. Sanna, A. Carta, M.E. Rahbar Nikookar, Eur. J. Med. Chem. 35 (2000) 535-543; P. Sanna, A. Carta, L. Gherardini, M.E. Rahbar Nikookar, Farmaco 57 (2002) 79-87) were tested for their capability to prevent MT-4 cell growth. All compounds resulted devoid of antibacterial, antifungal and anti-HIV-1 activity. In anti-mycobacterial assays several compounds resulted active (MIC(50)=6.0-70 microM) against M. tuberculosis. However, since they showed cytotoxicity against MT-4 cells at lower concentrations (CC(50)=0.05-25 microM), their anti-mycobacterial activity was not selective. For this reason, the most cytotoxic compounds were also evaluated for antiproliferative activity against a panel of human cell lines derived from both hematological and solid tumors. Compound 34 resulted the most potent compound against the above human tumor-derived cell lines.

Novel substituted quinoxaline 1,4-dioxides with in vitro antimycobacterial and anticandida activity.

Thirty-six 6(7)-substituted-3-methyl- or 3-halogenomethyl-2-phenylthio-phenylsulphonyl-chloro-quinoxaline 1,4-dioxides belonging to series 3-6 were synthesised and submitted to a preliminary in vitro evaluation for antimycobacterial, anticandida and antibacterial activities. Antitubercular screening showed a generally good activity of 3-methyl-2-phenylthioquinoxaline 1,4-dioxides (3d,e,h-j) against Mycobacterium tuberculosis, and exhibited MIC between 0.39 and 0.78 microg mL(-1) (rifampicin MIC=0.25 microg mL(-1)), whereas in compounds 4d,e, 5a,b,d,e,l and 6b-e,j,l MIC ranged between 1.56 and 6.25 microg mL(-1). Results of the antibacterial and anticandida screening showed that 6e and 6l exhibited MIC=0.4 and 1.9 microg mL(-1), respectively, against Candida krusei (miconazole MIC=0.9 microg mL(-1)), and 4i, 5b,d, 6e, MIC=3.9 microg mL(-1) against Candida glabrata (miconazole MIC=0.4 microg mL(-1)), while compounds 3d,l, 5e,l, and 6b,d,e,l showed MIC=15.6 microg mL(-1) against Vibrio alginolyticus.

Synthesis and antimycobacterial activity of 3-aryl-, 3-cyclohexyl- and 3-heteroaryl- substituted-2-(1H(2H)-benzotriazol-1(2)-yl)prop-2-enenitriles, prop-2-enamides and propenoic acids. II.

A series of 32 3-aryl-, 3-cyclohexyl-, and 3-heteroaryl-substituted-2-(1H(2H)-benzotriazol-1(2)-yl)-prop-2-enenitriles, prop-2-enamides and propenoic acids, was synthesized as a part of our research in the antitubercular field, according to an international program with the Tuberculosis Antimicrobial Acquisition and Coordinating Facility (TAACF). This work reports the preparation and analytical and spectroscopic characterization (MS, UV, IR, 1H NMR) of all compounds synthesized. Among these only a few compounds (E-4b,c, E-5a, E-7e and E-8d) were found to be endowed with modest growth inhibition of Mycobacterium tuberculosis. However, the obtained results allowed to acquire interesting structure-activity relationships.

Synthesis and evaluation for biological activity of 3-alkyl and 3-halogenoalkyl-quinoxalin-2-ones variously substituted. Part 4.

A new series of 3-isopropyl-, 3-trifluoromethyl- and 3-bromomethylquinoxaline-2-ones variously substituted on the benzo-moiety were synthesized and submitted to a preliminary in vitro evaluation for antibacterial, antifungal and anti-HIV activities. Furthermore, all compounds were also tested for cytotoxicity. Results of the screening showed that compound 10 exhibits moderate antimicrobial activity against Staphylococcus aureus (MIC = 33 microM), and that 25 and 26 showed interesting cytotoxicity versus mock-infected MT-4 cells. All the other compounds were inactive.