title: Synthesis, characterization, and tuberculostatic activity of novel 2-(4-nitrobenzoyl)hydrazinecarbodithioic acid derivatives.
abstract: A series of novelS-esters of 2-(4-nitrobenzoyl)hydrazinecarbodithioic acid andS,S'-diesters of (4-nitrobenzoyl)carbonohydrazonodithioic acid were synthesized by reaction of 4-nitrobenzohydrazide andN-methyl-4-nitrobenzohydrazide with carbon disulfide and alkyl halides in the presence of triethylamine. Novel 5-(4-nitrophenyl)-1,3,4-oxadiazoles were also obtained. The structures were confirmed by IR, NMR, and mass spectroscopy, and by elemental analysis. All the compounds obtained were screened in vitro for their tuberculostatic activity. Promising preliminary results were obtained for some of the compounds. The crystal structure of the most active compound was determined.
authors.affiliation: Department of Organic Chemistry, Medical University of Gdansk, 107 Gen. Hallera Str., 80-416 Gdansk, Poland.
authors.forename: Katarzyna
authors.initials: K
authors.lastname: Gobis
authors.affiliation: Department of Organic Chemistry, Medical University of Gdansk, 107 Gen. Hallera Str., 80-416 Gdansk, Poland.
authors.forename: Henryk
authors.initials: H
authors.lastname: Foks
authors.affiliation: Department of Microbiology, Institute of Tuberculosis and Pulmonary Diseases, Warsaw, Poland.
authors.forename: Ewa
authors.initials: E
authors.lastname: Augustynowicz-Kopec
authors.affiliation: Department of Microbiology, Institute of Tuberculosis and Pulmonary Diseases, Warsaw, Poland.
authors.forename: Agnieszka
authors.initials: A
authors.lastname: Napiorkowska
authors.affiliation: Institute of General and Ecological Chemistry, Technical University of Lodz, Lodz, Poland.
authors.forename: Malgorzata
authors.initials: M
authors.lastname: Szczesio
authors.affiliation: Institute of General and Ecological Chemistry, Technical University of Lodz, Lodz, Poland.
authors.forename: Andrzej
authors.initials: A
authors.lastname: Olczak
authors.affiliation: Institute of General and Ecological Chemistry, Technical University of Lodz, Lodz, Poland.
authors.forename: Marek L
authors.initials: ML
authors.lastname: Glowka
keywords: 5-(4-Nitrophenyl)-1,3,4-oxadiazole-; Crystal structure; Drug research; Structure–activity relationship; Tuberculostatic activity