The Gas Imaging Spectrometer (GIS) system on board ASCA is described. The experiment consists of 2 units of imaging gas scintillation proportional counters with a sealed-off gas cell equipped with an imaging phototube. The performance is characterized by the high X-ray sensitivity (from 0.7 keV to over 10 keV), good energy resolution (7.8% FWHM at 6 keV following E~0-5 as a function of X-ray energy E), moderate position resolution (0.5 mm FWHM at 6 keV with E~0-5 dependence), fast time resolution down to 61 /xs, and an effective area of 50 mm diameter. The on-board signal processing system and the data transmitted to the ground are also described. The background rejection efficiency of the GIS is reaching the level achieved by the non-imaging multi-cell proportional counters.
Various analogues of a new antidiabetic agent, pioglitazone (AD-4833, U-72107), were synthesized in order to study in more detail the structure-activity relationships of this class of drug. 5-(4-Pyridylalkylthiobenzyl)-2,4-thiazolidinediones (I), thia-analogues of pioglitazone, were prepared via Meerwein arylation of the alkylthioanilines (IV). 5-(4-Pyridylalkoxybenzylidene)-2,4-thiazolidinediones (IIa) and related heterocyclic analogues (IIb) were synthesized by Knoevenagel condensation of the aldehydes (VIII) with the corresponding azolidinones. Compounds I and II were evaluated for hypoglycemic and hypolipidemic activity in genetically obese and diabetic yellow KK (KKAy) mice. Several 5-[4-[2-(2-pyridyl)ethoxy]-benzylidene]-2,4- thiazolidinediones (IIa) were equipotent to pioglitazone. However, the thia-analogues (I) and the benzylideneheterocycles (IIb) had decreased activity. Catalytic hydrogenation of the 5-benzylidene analogue (14) was found to be a convenient new synthetic method for pioglitazone. The configuration of 14 is also discussed.
The pyridylethanols (I) are transformed into the p‐nitrophenyl ethers (III) which undergo coupling with the acrylate (IV) via reduction and diazotization to form the pyridylethoxyphenylpropionates (V).
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.