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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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The N 1 -dithioester substituted pyridin-and pyrazincarboxamidrazones underwent cyclocondensation to 5-methylsulfanyl-1,3,4-thiadiazole or 1,2,4-triazole derivatives, depending on the reaction conditions. With an excess of secondary amines, pyrazincarboxamidrazone dithioester gave 5-amino-1,3,4-thiadiazoles and with an ethanoloamine a 1,2,4-triazole derivative. Prepared compounds were evaluated as potential tuberculostatic agents, but the minimum inhibitory concentrations values indicated no significant activity.

The effects of newly synthetized pyrazinimidazolines on the contraction of isolated rat tail artery and on the chronotropic action of rat atria as well as the effects on blood pressure in anaesthetized rats were determined. The structure-activity relationships were studied, including standard imidazoline drugs. Starting from practically inactive derivatives the step-by-step structural modifications have been made resulting in markedly active chemical congeners, which were designed, synthetized and tested pharmacologically.

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