A series of 1-benzylbenzimidazole and 3-benzylimidazo[4,5-b]pyridine substituted in the 2-position by an alkanoic or mercaptoalkanoic acid chain was synthesized for evaluation as potential thromboxane A2/prostaglandin H2 (TXA2/PGH2) receptor antagonists. The affinity of each compound for washed human platelet TXA2/PGH2 receptors was determined by radioligand binding studies using [125I]PTA-OH. Structure-activity relationships led to the conclusions that 2-alkanoic acid derivatives were slightly more potent than 2-mercaptoalkanoic acids and that compounds possessing a 3,3-dimethylbutanoic acid in the 2-position were definitely the most potent with Ki values of 4-39 nM (11a, 11g-x, 37a, 37f-o, 23a-c). The replacement of this 3,3-dimethylbutanoic acid side chain by a shorter one led to a marked decrease of affinity (11b and 11c; Ki = 5600 and 1700 nM, respectively). Compounds of benzimidazole and imidazo[4,5-b]pyridine series displayed similar potencies (11q and 23c have Ki values of 6 and 7 nM, respectively). The interesting pharmacological profile of compound 23a (UP 116-77: 4-[3-[(4-chlorophenyl)methyl]-6-chloroimidazo[4,5-b]pyridin-2-yl]- 3,3-dimethylbutanoic acid) and its excellent tolerance led us to select this derivative for further development.

Laser-induced damage in two types of silicon photosensor array has been studied. The samples were MOS CCD time delay integration (TDI) sensors with a 2048×96 element array of pixels and CID photodiode arrays of 512×1 pixels. The laser source was a Q-switched 1064 nm Nd:YAG laser (10 Hz rep rate, 10 ns pulses with a 250 μm spot radius). Tests for morphological and electrical damage to the CCD arrays have been reported previously. In new experiments, the micro-damage morphology is examined and correlated with both the observed electrical degradation and newly observed stress effects. We report the observation of surface deformation and lattice defects due to laser-induced stresses in the SiO2 and poly-silicon thin films on the silicon substrate. Measurements of damage for the CID arrays show them to be more resistant to laser damage than MOS structures such as CCD arrays. In addition, electrical degradation of these arrays was observed which affected the video output signal from the devices.

Abstract-Geostationary Ocean Colour Imager (GOCI) is the first