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Substituted 3-aminopyrazine-2,5-dicarbonitriles as New Antiinfectives
* 1 , 1 , , 2 , 3 , 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

 
 
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