| 摘要 |
<p>(A) Compounds of formula (I) are new: where R,R' are same or different H, alkyl (C1-C5), or phenyl opt. substd. by one or more halogen, NH2, NO2 or SO2NH2; or NRR' is a satd. heterocycle (5-7 membered) opt. contg. a second heteroatom (O, N or S). (B) The intermediates (III) are also new (see "Preparation"). Oral hypoglycaemic agents for use in human and veterinary medicine. Stage 1 is pref. performed at 70-100 degrees C in conc. H2SO4; stage 2 at 100 to 150 degrees C in absence of solvent; stage 3 pref. at -5 to +25 degrees C in a suitable solvent. PHARMACOLOGY The most active compounds have a similar hypoglycaemic activity to that of chlorpropamide at 50 mg/kg. orally in mice but they are much less toxic (no deaths at 10g/kg; chlorpropamide LD50 is 1.1 g/kg.) Two compounds have slight diuretic activity.</p> |
