EventsThe 9th International Electronic Conference on Synthetic Organic Chemistry
Published
This submission belongs to the session c. Bioorganic Chemistry and Natural Products of the event The 9th International Electronic Conference on Synthetic Organic Chemistry
Published date
01 Nov, 2005
Citation
Lukas Palek, Martin Dolezal, Jaroslav Dvorak, Vladimir Buchta, Pavel Cermak, Marian Mednansky, Substituted 3-aminopyrazine-2,5-dicarbonitriles as New Antiinfectives, in Proceedings of The 9th International Electronic Conference on Synthetic Organic Chemistry, 1 November–30 November 2005, MDPI: Basel, Switzerland, doi: 10.3390/ecsoc-9-01512
Share
Email
Facebook
Twitter
LinkedIn

Substituted 3-aminopyrazine-2,5-dicarbonitriles as New Antiinfectives

Lukas Palek 1
Martin Dolezal 1
Jaroslav Dvorak
Vladimir Buchta 2
Pavel Cermak 3
Marian Mednansky 3
1. Department of Pharmaceutical Chemistry and Drug Control, Faculty of Pharmacy, Charles University, Heyrovskeho 1203, 500 05 Hradec Kralove, Czech Republic
2. Department of Biological and Medical Sciences, Faculty of Pharmacy, Charles University, Heyrovskeho 1203, 500 05 Hradec Kralove, Czech Republic
3. Department of Clinical Microbiology, University Hospital, Sokolska 581, 500 05 Hradec Kralove, Czech Republic
Abstract
A series of new pyrazinamide analogues have been prepared. Report that 5-chloropyrazinamide [1] has different mode of action than pyrazinamide itself [2] promises good chance to reach new structure with high antimycobacterial activity and new action mechanism that is realy needed because of resisance increase [3] to drugs in current use. Dericatives of pyrazine-2,5-dicarbonitrile promise good starting point to further studies (best activity reached yet is 3-(3-chlorophenylamino)pyrazine-2,5-dicarbonitrile, with MIC = 8µmol.l-1 against classical TBC strains and with lower activity against atypical strains. Compared to pyrazinamide with MIC = 4µmol.l-1 against classical strains and no activity against atypical ones).
Keywords
pyrazinamide
tuberculosis
antimycobacterial
antifungal
2-(4H-4-Oxo-benzopyran-3-yl)benzothiazolium Salts. Synthesis, Reactions and Plant Growth Activity
Synthesis and Biological Evaluation of Pyrazinecarboxamides