Novel BACE-1 inhibitors with a hydroxyethylene central core have been developed. Modified P1´ and extended P1 substituents were incorporated with the aim to explore potential interactions with the S1´ and the S1-S3 pocket, respectively, of BACE-1. Inhibitors were identified displaying IC50 values in the nanomolar range, i.e. 69 nM for the most potent compound. Possible inhibitor interactions wi...

All the 28 Bacteroides fragilis strains investigated were susceptible to sulfamethoxazole (minimal inhibitory concentration < 16 mug/ml) and resistant to trimethoprim (TMP; minimal inhibitory concentration > 4 mug/ml). Synergism between sulfamethoxazole and TMP was present in all strains at a ratio of 1:1. The few clostridia investigated proved more resistant to both compounds. Dihydrofolate re...

The activities of pirlimycin (U57930E), lincomycin, clindamycin, erythromycin, josamycin, oleandomycin, and spiramycin were compared against strains of the Bacteroides fragilis group. Pirlimycin was the most active; the 90% minimal inhibitory concentration was 1 microgram/ml, and the activity range was 0.125 to 4 micrograms/ml. This drug was fourfold more active than any of the other drugs, inc...

Amikacin was given to 14 noninfected men as three consecutive intramuscular injections (7.5 mg/kg) at 12-h intervals. Serum and bronchial secretion specimens were obtained at various times during flexible fiberoptic bronchoscopy after the final dose. Serum and bronchial secretion concentrations obtained between 1.5 and 2.0 h after the final dose ranged from 17 to 40 mug/ml and 2.3 to 8.4 mug/ml...

Page 6445. In Table 1, the IC50, pIC50, and LE values of compound 5 are incorrect. They should be 68± 11 nM, 7.2, and 0.89, respectively. The reported values correspond to a different chemical entity; this error was caused by a mislabeling-error in screening of the fragment library. The main text is unaffected by this error. Compound 5 was only discussed as a tolerated structural analogue of co...

Antimicrobial activity of different parts of Croccus sativus L. (saffron) including stigma, stamen, leaves and colora, extracted by various solvents, were tested against different bacteria (Microccucos luteus, Staphylococcus epidermitis, Staphylococcus aureus and E. coli) and fungi (Candida albicans, Aspergillus niger and Cladospourium sp) by cup plate diffusion method. Minimal Inhibitory Conce...

rue, ruta graveolens, is a medicinal plant in traditional medicine that has several therapeutic properties such as anti-carcinogenic agent, antioxidant, anti-inflammatory, antimicrobial, hypotensive, and spasmolytic. this study was carried out to evaluate the antibacterial effects of the etanolic extract of rue against piscine pathogenic bacteria viz. lactococcus garvieae and aeromonas hydrophi...

background and purpose: candidiasis is a major fungal infection, and candida albicans is the major cause of infections in humans. the clinical and laboratory standards institute (clsi) developed new breakpoints for antifungal agents against c. albicans. in this multi-center study, we aimed to determine the drug susceptibility profile of c. albicans, isolated from iranian population according to...

background: trichomoniasis is the most common nonviral sexually transmitted human disease that is caused by protozoan trichomonas vaginalis. metronidazole is the selective drug in trichomoniasis treatment. however, the reported cases show an increasing trend of drug resistance. this study aimed to evaluate the effect of mango and blueberry extracts on t. vaginalis. materials and methods: t. vag...