The solvent-free reaction of o-phenylenediamine (I) with the carboxylic acids (II) leads to higher product yields compared to the Phillips method for instance. Some of the products, e.g. (IIIa), (IIIb), and (Va), exhibit a high tuberculostatic activity. -(FOKS*, H.; PANCECHOWSKA-KSEPKO, D.; KUZMIERKIEWICZ, W.; ZWOLSKA, Z.; AUGUSTYNOWICZ-KOPEC, E.; JANOWIEC, M.; Chem. Heterocycl. Compd. (N. Y.) 42 (2006) 5, 611-614; Dep. Org. Chem., Med. Univ. Gdansk, PL-80-416 Gdansk, Pol.; Eng.) -H. Haber 03-110
These compounds were transformed into methane-and benzenesulfonamide derivatives. The benzimidazole derivatives obtained were tested in vitro for their tuberculostatic activity. Compounds with good activity (MIC 6.2-25 µg/ml) have been found.
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