ChemInform Abstract: Synthesis, Potent anti‐Staphylococcal Activity and QSARs of Some Novel 2‐Anilinobenzazoles.

Abstract

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.

1H‐Benzimidazole‐2‐acetonitriles as synthon in fused benzimidazole synthesis

“…1 H ‐Benzimidazole‐2‐acetonitriles 1 were synthesized by fusion of o ‐phenylenediamines and cyanoacetate at high temperature (Scheme ) [7–15].…”

Ethyl 3-nitro-4-(n-propylamino)benzoate

“…For bond-length data, see: Allen et al (1987). For the synthesis, see: Ates-Alagoz & Buyukbingol (2001); Oezden et al (2005).…”