A novel subclass of quinolones, 2-pyridones, showed potent activity against Mycobacterium tuberculosis, with KRQ-10018 being an early lead. KRQ-10018 showed better activity in vitro against M. tuberculosis versus moxifloxacin. In vivo efficacy of KRQ-10018 at 300 mg/kg of body weight was similar to that of isoniazid at 25 mg/kg, but showed less activity than moxifloxacin at 300 mg/kg.

N-Alkyl 2-pyridones and other enolizable heterocycles are important synthetic constructs, due to their prevalence in natural products and pharmaceutical targets and their capacity to serve as models for a number of biological and chemical processes. The disclosed Au(I)-catalyzed reaction utilizes 2-propargyloxypyridines to access N-alkylated 2-pyridone products derived from both 5-exo and 6-end...

The aryl-(Z)-N-[2-amino-1,2-dicyanovinyl]formamidine 2 cyclize in solvent-free conditions and in the presence of a base to give a 5-amino-1-aryl-4-cyanoimidazoles 3. Silica sulfuric acid as an efficient and reusable heterogeneous catalyst has been used for the preparation of amidines 2 from formimidate 1 through reaction with aromatic amines at room temperature and in good to excellent yields. ...

The aryl-(Z)-N-[2-amino-1,2-dicyanovinyl]formamidine 2 cyclize in solvent-free conditions and in the presence of a base to give a 5-amino-1-aryl-4-cyanoimidazoles 3. Silica sulfuric acid as an efficient and reusable heterogeneous catalyst has been used for the preparation of amidines 2 from formimidate 1 through reaction with aromatic amines at room temperature and in good to excellent yields. ...