Synthesis and antiviral evaluation of n-glycosides derived from 6-amino-3-aryl-2-methyl-4-(3h)-quinazolinones.

Reaction of monosaccharides (D-glucose. D-galactose, D-xylose or L-arabinose) with 6-amino-3-aryl-2-methyl-4-(3H) quinazolinones (1a-c) in boiling methanol yielded the corresponding N-glycopyranosides 3a-c, 4a-c, 5a,b and 6a,b. The N-glycopyranosides 3a-c, 4a-c, 5a,b and 6a,b were acetylated with acetic anhydride and pyridine to give the corresponding acetate derivatives 7a-c, 8a-c, 9a,b and 10a,b. The structures of all these glycosides were assessed by elemental analysis, IR, NMR and mass spectra. Some of these products were tested for anti-cancer and anti-AIDS activity.

Differential diagnosis of hepatic neoplasms: spin echo versus gadolinium-diethylenetriaminepentaacetate-enhanced gradient echo imaging.

Early results are reported of hepatic neoplasms studied with dynamic gadolinium-diethylenetriaminepentaacetate (Gd-DTPA)-enhanced magnetic resonance imaging (MRI). The purpose of this study was to evaluate the potential of the Gd enhancement pattern for characterizing these neoplasms and to compare the performance of spin-echo (SE) to SE plus dynamic Gd-enhanced gradient-echo (GRE) pulse sequences. Forty-two patients with hepatic neoplasms were examined at 1.5 T field strength. In each patient, short and long repetition time/echo time (TR/TE) SE images were obtained, followed by pre- and post-Gd-DTPA (0.1 mmol/kg body wt), single-slice, breath-hold (13 s/scan) GRE images, which were serially acquired less than or equal to 12 min postinjection. The patterns of contrast enhancement of the various hepatic lesions were documented and analyzed. The time to peak Gd signal enhancement-to-noise ratio (SE/N), contrast-to-noise ratio (C/N), contrast (defined as the signal intensity ratio [SIR]), as well as the peak values of these quantities, were determined. The C/N and SIR values on the short and long TR/TE SE and pre-Gd GRE images for all hepatic neoplasms were also obtained. The discriminating abilities (hemangiomas vs. malignant neoplasms) of these quantities were analyzed statistically. In addition, the impact of lesion characterization on the SE versus the SE plus the Gd-enhanced GRE scans was assessed by means of a blinded reader study. Malignant hepatic neoplasms could be differentiated from hemangiomas by visual inspection of their enhancement patterns (p = 0.0009), by the time to peak C/N on Gd-enhanced images (p = 0.0002), and by the magnitude of such peak (p = 0.02). Combined SE + Gd-enhanced GRE scans afforded minor, though statistically significant (p less than 0.01), improvement of the accuracy in differentiating benign from malignant hepatic neoplasms. Late scans (12 min post-Gd) may be particularly useful in identifying hemangiomas that, unlike other neoplasms, have a significant high signal of their enhancing portions on such images.