Synthesis and anti-mycobacterial evaluation of some pyrazine-2-carboxylic acid hydrazide derivatives.
A series of pyrazine-2-carboxylic acid hydrazide derivatives were synthesized and screened for their activity against Mycobacterium tuberculosis. The results show that pyrazine-2-carboxylic acid hydrazide-hydrazone derivatives 3a-l were less active than pyrazinamide. In contrast, the N(4)-ethyl-N(1)-pyrazinoyl-thiosemicarbazide 4 showed the highest activity against M. tuberculosis H(37)Rv (IC(90) = 16.87 microg/mL). Details of the structure-activity and structure-cytotoxicity relationships are discussed.
Abdel-Aziz
Mohamed
M
Department of Medicinal Chemistry, Faculty of Pharmacy, Minia University, 61519-Minia, Egypt. abulnil@hotmail.com
Abdel-Rahman
Hamdy M
HM
D000818:Animals; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D002522:Chlorocebus aethiops; D006834:Hydrazines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D009169:Mycobacterium tuberculosis / Q000187:drug effects; D011719:Pyrazines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D014709:Vero Cells
D000900:Anti-Bacterial Agents; D006834:Hydrazines; D011719:Pyrazines; C552061:pyrazine-2-carboxylic acid hydrazide; C029424:hydrazine