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A series of novel 3-O-(3-aryl-propenyl)clarithromycin derivatives were designed, synthesized and evaluated for their in vitro antibacterial activities. Regioselective allylation at 3-OH was efficiently achieved in the presence of 9-oxime ether, compared with 9-keto. Most of the side chains were identified as the 3-O-(3-aryl-Z-prop-1-enyl) group, not the expected 3-O-(3-aryl-E-prop-2-enyl) group. Some derivatives of this series showed improved activities against erythromycin-resistant Staphylococcus aureus and Staphylococcus pneumoniae compared with the reference compound, clarithromycin, but weaker activities against susceptible strains.

Mumps virus infection is a potentially serious viral infection of childhood and early adulthood. In China, live attenuated S(79) mumps vaccine has been licensed for pediatric use since 1990. The objective of this study was to determine the effectiveness of live attenuated S(79) mumps vaccine against clinical mumps in outbreaks.Cases were selected from mumps outbreaks in schools in Guangzhou between 2004 and 2005. Each case was matched by gender, age and classroom. Vaccination information was obtained from Children's EPI Administrative Computerized System. Vaccine effectiveness (VE) was calculated for 1 or 2 doses of S(79) vaccine with 95% confidence intervals (CI).One hundred and ninety-four cases and 194 controls were enrolled into the study. VE of the S(79) mumps vaccine for 1 dose versus 0 confer protection 80.4% (95% CI, 60.0%-90.4%) and VEs against mumps in outbreaks for 1 dose of mumps vaccine are similar among those children aged 4-9 years and aged over 10 years old.The live attenuated S(79) mumps vaccine can be effective in preventing clinical mumps outbreaks.

To investigate the effects of risperidone on the polysomnography (PSG) in the patients with first-episode schizophrenia.Twenty-five patients with first-episode schizophrenia, 13 males and 12 females, aged 29 +/- 8, underwent polysomnographic recording for 4 consecutive nights, the first night being used for acclimatization, and on the 3 rd and 4 th nights risperidone in the dose of 1.2 mg was administered before going to bed. Forty-four healthy persons, 23 males and 21 females, aged 28 +/- 8, underwent polysomnographic recording for 2 consecutive nights, the first night being used for acclimatization.The baseline PSG recording showed that in comparison with the normal control group the total sleep time of the schizophrenia patients was shorter (378 min +/- 30 min vs 462 min +/- 21 min), sleep latency was longer (30 min +/- 14 min vs 18 min +/- 8 min), rapid eye movement (REM) sleep latency was shorter (59 min +/- 20 min vs 88 min +/- 10 min), REM sleep time was shorter (61 min +/- 17 min vs 84 min +/- 12 min), awakening time was longer (34 min +/- 17 min vs 15 min +/- 5 min), stage 1 (S1) time was longer (22% +/- 10% vs 9.0% +/- 1.7%), S3 time and S4 time were shorter, and the sleep efficacy was lower (86% +/- 10%) (P0.05 approximately P0.01); however, there was no significant difference in the S2 time between these 2 groups (54% +/- 16% vs 56% +/- 4%, P0.05). In the schizophrenia group, in comparison with the baseline levels in the third and fourth nights the total sleep times were significantly increased (406 min +/- 34 min and 428 min +/- 31 min respectively), the awakening times were significantly decreased (23 min +/- 15 min and 19 min +/- 8 min respectively), and S1 times were significantly decreased (14 min +/- 9 min and 10 min +/- 9 min respectively), with such changes time-dependently; and in the 4 th night the REM sleep time was significantly increased (87 min +/- 20 min) and the sleep efficacy was significantly improved (93% +/- 12%) (P0.05 approximately P0.01), however, there were no significant differences in the sleep latency and slow wave sleep (both P0.05).Risperidone significantly improves the quality of sleep.

To investigate the characteristics of sensory gating P50 of patients with first-episode schizophrenia.The auditory evoked potentials P50 were recorded in 66 patients (Group Sch) with first-episode schizophrenia and 92 normal controls (Group NC) by using conditioning/testing paradigm presented with auditory double click stimuli.The value of S1-P50 of Group Sch was 3 microV +/- 2 microV, significantly lower than that of Group NC (6 microV +/- 3 microV, P0.01). The value of S2-P50 of Group Sch was 4 microV +/- 2 microV, significantly higher than that of Group NC (2 microV +/- 1 microV, P0.01). The S2/S1 ratio of Group Sc was 81% +/- 40%, significantly higher than that of Group NC (42% +/- 21%, P0.01). The value of S2 - S1 of Group Sch was 2 microV +/- 1 mciroV, significantly lower than that of Group Sch (3 mciroV +/- 2 microV). The value of 100 (1-S2/S1) of Group Sch was 19% +/- 17%, significantly lower than that of Group NC (58% +/- 21% , P0.01).Sensory gating deficit exists in the patients with first-episode schizophrenia, manifested in deficiency of inhibition that can be quantitatively observed by measuring auditory evoked potential P50.

The ratio of E/Z of 2'-,4"-O-bis(trimethylsilyl)erythromycin A 9-O-(1-isopropoxycyclohexyl) oxime were much higher prepared in CH 3 CN than those in CH 2 Cl 2 . And the ratio would increase with elevation of temperature. Compared with 2'-OH, 4"-OH was liable to be silylated in the presence of 1,1,1,3,3,3-hexamethyldisilizane and an NH 4 +. The crystal structure of E-title compound was determined by single-crystal X-Ray structure analysis to elucidate the origin of regioselectivity occurring at 6-hydroxyl group in the O-methylation of erythromycin A.