Research on durene derivatives. Note I - hypertensive activity of 2-(2,3,5,6-tetramethylbenzyl)imidazoline and related compounds.

A series of substituted 2-(2,3,5,6-tetramethylbenzyl)imidazolines and related compounds have been synthesized to study the steric and hydrophobic effects on the vasoactivity of the introduction of four methyl groups on the phenyl moiety. The 2-(2,3,5,6-tetramethylbenzyl)imidazoline (I) showed a high hypertensive activity, whereas the 2-benzylimidazoline possesses an adrenolytic activity. The 2-(2,3,5,6-tetramethylphenoxy)methylimidazoline (XVII) retained the hypertensive activity, whereas the corresponding thioether (XIX) was inactive. Some structure-activity relationships with regard to the presence of substituents in the 4-position of the phenyl moiety and on the benzylic CH2 are reported.

New 2-methyldialkylammoniumalkylthio-4,p-substituted phenyl-3H-1,5-benzodiazepine iodides with antibacterial activity note I.

A series of 2-methyldialkylammoniumalkylthio-4,p-substituted phenyl-3H-1,5-benzodiazepine iodides has been synthesized. Some compounds showed high selective activity against Staph. aureus and Strep. pyogenes. The nature of the sustituents at the phenyl moiety bound to the 4-position of the 1,5-benzodiazepine ring is of decisive influence, wherease the length of the aliphatic chain and the modification of the cationic head are of minor importance for the activity. The most active compound, 2-methyldiethylammoniumethylthio-4,p-phenylthiophenyl-3H-1,5-benzodiazepine iodide (XXXVIII), was selected for further research.