Synthesis and SAR of novel, 4-(phenylsulfamoyl)phenylacetamide mGlu(4) positive allosteric modulators (PAMs) identified by functional high-throughput screening (HTS)

Herein we disclose the synthesis and SAR of a series of 4-(phenylsulfamoyl)phenylacetamide compounds as mGlu(4) positive allosteric modulators (PAMs) that were identified via a functional HTS. An iterative parallel approach to these compounds culminated in the discovery of VU0364439 (11) which represents the most potent (19.8 nM) mGlu(4) PAM reported to date. (C) 2010 Elsevier Ltd. All rights reserved.

Analysis of pharmacists attitudes toward a distance learning initiative on health screening

A questionnaire was developed to investigate pharmacists' attitudes to distance learning (DL) as a vehicle for continuing education (CE). It was included in each of a two part DL course on Health Screening. Part One was mailed to all community pharmacists in England (16,400) and returns were received from 1487. The questionnaire in Part Two was returned by 436 pharmacists. Attitude statements were scored using a five-point Likert scale. The mean response to all attitude statements was positive. Participants were significantly more satisfied than non-participants with DL in general and the DL course studied (P less than or equal to 0.05). Over 80 percent of respondents completing the course found DL to be enjoyable and more suitable than other CE methods. More females and less males than expected (based on registration statistics) requested (P less than or equal to 0.001) and completed the course (P less than or equal to 0.001). Pharmacists of all ages participated, although those recently qualified showed greater interest.

Role of the plasma scale length in the harmonic generation from solid targets

We have investigated the generation of high harmonics from the interaction of 150 fsec, 790 nm, and 395 nm laser pulses with solid targets. Experiments are presented that demonstrate a strong dependence of the conversion efficiency on the temporal pulse shape and the resulting density scale length (L/lambda) of the preformed plasma. The highest conversion efficiencies are achieved for short density scale lengths (L/lambda less than or equal to 0.4), which result from high contrast ratio pulse interactions. [S1063-651X(98)50211-5].