title: Synthesis, structure, and biological activity of novel heterocyclic sulfonyl-carboximidamides.
abstract: A series of novel heterocyclic sulfonyl-carboximidamides were synthesized in satisfactory yields via condensation of heterocyclic methyl carbimidates with 2-chlorobenzenesulfonamide and 4-chloropyridine-3-sulfonamide. New structures were confirmed by IR and NMR spectra as well as elemental analyses. X-ray crystallography of two derivatives was performed. The single-crystal structures confirmed the presence of a primary amine group in the amidine moiety. All the compounds were screened for their tuberculostatic, antibacterial, and anticancer activities. Preliminary results indicated that target compounds exhibited weak tuberculostatic and antibacterial activities. Seven compounds inhibited the growth of some cancer cell lines, whereas one of the 2-quinoline derivatives displayed favorable activity against all tested cancer cells withGI50values of 0.92-13 μM.
authors.affiliation: Department of Organic Chemistry, Medical University of Gdańsk, Gdańsk, Poland.
authors.forename: Katarzyna
authors.initials: K
authors.lastname: Gobis
authors.affiliation: Department of Organic Chemistry, Medical University of Gdańsk, Gdańsk, Poland.
authors.forename: Henryk
authors.initials: H
authors.lastname: Foks
authors.affiliation: Department of Organic Chemistry, Medical University of Gdańsk, Gdańsk, Poland.
authors.forename: Jarosław
authors.initials: J
authors.lastname: Sławiński
authors.affiliation: Department of Physical Chemistry, University of Gdańsk, Gdańsk, Poland.
authors.forename: Artur
authors.initials: A
authors.lastname: Sikorski
authors.affiliation: Department of Physical Chemistry, University of Gdańsk, Gdańsk, Poland.
authors.forename: Damian
authors.initials: D
authors.lastname: Trzybiński
authors.affiliation: Department of Microbiology, Institute of Tuberculosis and Pulmonary Diseases, Warsaw, Poland.
authors.forename: Ewa
authors.initials: E
authors.lastname: Augustynowicz-Kopeć
authors.affiliation: Department of Microbiology, Institute of Tuberculosis and Pulmonary Diseases, Warsaw, Poland.
authors.forename: Agnieszka
authors.initials: A
authors.lastname: Napiórkowska
authors.affiliation: Sunny BioDiscovery, Santa Paula, CA USA.
authors.forename: Krzysztof
authors.initials: K
authors.lastname: Bojanowski
keywords: Antimicrobial activity; Antitumor activity; Crystal structure; Heterocycles; Structure–activity relationship; Sulfonamidine