Imidazopyridine derivatives as potent and selective Polo-like kinase (PLK) inhibitors.

A novel class of imidazopyridine derivatives was designed as PLK1 inhibitors. Extensive SAR studies supported by molecular modeling afforded a highly potent and selective compound 36. Compound 36 demonstrated good antitumor efficacy in xenograft nude rat model.

Practical synthesis of a neuropeptide Y antagonist via stereoselective addition to a ketene.

[Reaction: see text]. The synthesis of neuropeptide Y antagonist 1, currently under clinical investigation for the treatment of obesity, is described. The convergent synthesis from trans-spirolactone carboxylic acid intermediate 2a and aminopyrazole 3 is predicated on a stereoselective route to the former.

Correlation between intracranial pressure (ICP) and changes in CT images of cerebral hemorrhage.

The relationship between intracranial pressure and CT images was investigated in 80 cases of cerebral hemorrhage that occurred between 1984 and 1990. In traumatic intracerebral hematoma, positive correlation was found between intracranial pressure and both shift of midline structures and volume of hematoma except in the occipital lobe or at the base of the frontal lobe. In nontraumatic intracerebral hematoma, increased intracranial pressure was found to correlate with changes in the configuration of the lateral ventricles, intraventricular hemorrhage, and compression of the basal cisterns and cortical sulci.

CSF shunt physics: factors influencing inshunt CSF flow.

Cerebrospinal fluid (CSF) in a shunt does not have a constant flow rate. The flow fluctuates from 0.01 ml/min to 1.

Cine magnetic resonance imaging of aqueductal stenosis.

Cerebral aqueductal stenosis is one of the most common causes of congenital and acquired hydrocephalus, but the etiology, pathophysiology and cerebrospinal fluid (CSF) dynamics of aqueductal stenosis have yet to be clarified. Utilizing cardiac gated cine magnetic resonance (MR) imaging, we evaluated aqueductal configuration and pulsatile motion of brain and CSF flow stimulated by cardiac pulsation in five patients with non-tumoral aqueductal stenosis. Cine MR of four cases revealed obliteration of the aqueduct by thickening mesencephalic tectum, turbulent CSF flow in the III ventricle, and absence of flow-related signal void, which in all normal cases indicates CSF movement within the aqueduct.