bearing bulky N-alkyl substituted amidino groups at position C-5 and 3,4-dichloro substituted phenyl at the C-2 position of the benzimidazole skeleton, show good activity profiles versus Gram-positive bacteria S.aureus. Replacement of the cationic amidine unit by the neutral amide group in (XIII) results in loss of activity. -(GOEKER*, H.; OEZDEN, S.; YILDIZ, S.; BOYKIN, D. W.; Eur. J. Med. Chem. 40 (2005) 10, 1062-1069; Dep. Pharm. Chem., Fac. Pharm., Ankara Univ., TR-06100 Tandogan, Ankara, Turk.; Eng.) -H. Haber 07-135

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nobenzazoles. -Thirty-four new anilinobenzimidazoles, two anilinobenzothiazoles, and one anilinobenzoxazole are synthesized in multiple steps and moderate yields by using three different methods. Mainly the CuCl-promoted intramolecular cyclization of the intermediary thioureas for the synthesis of anilinobenzimidazoles is applied. While anilinobenzimidazoles, and especially compounds (IIIb) and (IIId) show potent activities against Gram-positive bacteria S. aureus and MRSA, none of the anilinobenzothiazoles and benzoxazole derivatives exhibit inhibitory activity. The QSAR analysis of the anilinobenzimidazoles is examined, based on the relationship between the anti-staphylococcal activity and hydrophobicity parameters. -(OEZDEN, S.; ATABEY, D.; YILDIZ, S.; GOEKER*, H.; Eur.

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Synthesis of Some Flavone Derivatives: Potent Inhibitors of Human Platelet Aggregation. -The regioisomeric ethoxycarbonyl-flavones (Ia) and (IIa) are formed according to Jain's method and transformed into amides (18 examples in all). (Ia) and (IIa) represent the most potent inhibitors of platelet aggregation within the flavonoids. -(ERTAN, R.; GOEKER, H.; ERTAN, M.; BERETZ, A.; CAZENAVE, J. P.; HAAG, M.; ANTON, R.; Eur.