Stuart R. Michelson

TL;DR: Naphthyridine 7 inhibits the strand transfer of the integration process catalyzed by integrase with an IC50 of 10 nM and inhibits 95% of the spread of HIV-1 infection in cell culture at 0.39 microM.

TL;DR: Permeability measurements of such nonionic derivatives of atenolol, betaxoll, pindolol , propranolol, and timolol through fuzzy rat skin and rabbit cornea mounted on diffusion cells show that derivatization of the hydrophilic beta-blockers results in several-fold increase in permeation through these biological membranes, however, prodrug modification of the lipophilic Beta-blocker leads to little advantage in permeability characteristics.

TL;DR: Chronic oral administration to ethylene glycol fed rats of the 4-(4'-bromo[1,1'-biphenyl]-4-yl) derivative was shown to effect a significant reduction in urinary oxalate levels over a 58-day period, indicating the requirement for the two acidic functions on the 1H-pyrrole-2,5-dione nucleus.

TL;DR: The previously reported oxytocin antagonist L-371,257 has been modified at its acetylpiperidine terminus to incorporate various pyridine N-oxide groups, which has led to the identification of compounds with improved pharmacokinetics and excellent oral bioavailability.

TL;DR: A novel series of benzamidines was synthesized and shown to exhibit NR2B-subtype selective NMDA antagonist activity and is orally active in a carrageenan-induced rat hyperalgesia model of pain and shows no motor coordination side effects.