Synthesis, structure, and biological activity of novel heterocyclic sulfonyl-carboximidamides

Katarzyna Gobis , Henryk Foks , Jarosław Sławiński , Artur Sikorski , Damian Trzybiński , Ewa Augustynowicz-Kopeć , Agnieszka Napiórkowska , Krzysztof Bojanowski


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 with GI 50 values of 0.92–13 μM.
Author Katarzyna Gobis
Katarzyna Gobis,,
, Henryk Foks
Henryk Foks,,
, Jarosław Sławiński
Jarosław Sławiński,,
, Artur Sikorski (FCh / DPCh / PK)
Artur Sikorski,,
- Pracownia Krystalochemii
, Damian Trzybiński (FCh / DPCh / LRS)
Damian Trzybiński,,
- Laboratory of Rentgenography and Spectroscopy
, Ewa Augustynowicz-Kopeć
Ewa Augustynowicz-Kopeć,,
, Agnieszka Napiórkowska
Agnieszka Napiórkowska,,
, Krzysztof Bojanowski
Krzysztof Bojanowski,,
Journal seriesMonatshefte für Chemie, ISSN 0026-9247, e-ISSN 1434-4475, (A 25 pkt)
Issue year2013
Publication size in sheets0.55
ASJC Classification1600 General Chemistry
Languageen angielski
LicenseOther; published final; Uznanie Autorstwa (CC-BY); with publication
Score (nominal)25
ScoreMinisterial score = 25.0, 24-07-2019, ArticleFromJournal
Ministerial score (2013-2016) = 25.0, 24-07-2019, ArticleFromJournal
Publication indicators Scopus SNIP (Source Normalised Impact per Paper): 2013 = 0.707; WoS Impact Factor: 2013 = 1.347 (2) - 2013=1.445 (5)
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* presented citation count is obtained through Internet information analysis and it is close to the number calculated by the Publish or Perish system.