Characterisation of meticillin-resistant Staphylococcus aureus ST97 and ST5 isolated from pigs in Japan.

The objective of this study was to determine the frequency and clonal types of meticillin-resistant Staphylococcus aureus (MRSA) among slaughter pigs in a top pig-producing area in Japan. In total, 100 nasal swabs were collected from slaughterhouse pigs originating from 21 different farms. MRSA isolates were analysed by staphylococcal cassette chromosome mec (SCCmec) typing, spa typing and multilocus sequence typing (MLST) and were examined for susceptibility to nine antimicrobial agents (ampicillin, oxacillin, gentamicin, kanamycin, erythromycin, clindamycin, vancomycin, ciprofloxacin and tetracycline).

Design and synthesis of rho kinase inhibitors (III).

The structure-activity relationship of Rho kinase inhibitors bearing an isoquinoline scaffold was studied. N-(1-Benzyl-3-pyrrolidyl)-N-(5-isoquinolyl)amine analogues were optimized with respect to their inhibitory potencies for the enzyme and for chemotaxis. The potent analogues were further evaluated by an ex vivo test in which the selected compounds were orally administered to rats, and the Rho kinase inhibitory potency observed in the rat serum was evaluated 3h after the administration.

Design and synthesis of Rho kinase inhibitors (II).

In a previous study, we identified several structurally unrelated scaffolds of the Rho kinase inhibitor using pharmacophore information obtained from the results of a high-throughput screening and structural information from a homology model of Rho kinase. 1H-Indazole is one of the candidate scaffolds on which a new series of potent Rho kinase inhibitors could be developed. In this study, the detailed structure-activity relationship of 1H-indazole analogues was studied.