Synthesis and Biological Activity of Piperidinothiosemicarbazones Derived from Aminoazinecarbonitriles.

ABSTRACT: To investigate how structural modifications affect tuberculostatic potency, we synthesized seven new piperidinothiosemicrabazone derivatives 8-14, in which three of them had a pyrazine ring replacing the pyridine ring. Derivatives 8-9 and 13-14 exhibited significant activity against the standard strain (minimum inhibitory concentration (MIC) 2-4 μg/mL) and even greater activity against the resistant M. tuberculosis strain (MIC 0.5-4 μg/mL). Additionally, the effects of compounds 8-9 were entirely selective (MIC toward other microorganisms ≥ 1000 μg/mL) and non-toxic (IC50 to HaCaT cells 5.8 to >50 μg/mL). The antimycobacterial activity of pyrazine derivatives 11-12 was negligible (MIC 256 to >500 μg/mL), indicatin

SUBMITTER: Ziembicka D 

PROVIDER: S-EPMC10535983 | biostudies-literature | 2023 Sep

REPOSITORIES: biostudies-literature