259816-71-2Relevant academic research and scientific papers
Pyridinylpyrrolyl analogs of isoniazid: Synthesis and antimycobacterial activities
Costi, Roberta,Artico, Marino,Di Santo, Roberto,De Martino, Gabriella,Massa, Silvio,Deidda, Delia,Lampis, Giorgio,Pompei, Raffaello
, p. 408 - 423 (2007/10/03)
Pyridinylpyrrolyl analogs of isoniazid (INH) were prepared by reaction of ethyl 3-(4-pyridinyl)-2-propenoate with toluenesulfonylmethylisocyanide (TosMIC). The pyrrole esters which formed were reacted with hydrazine hydrate to afford INH analogs 7-10. These compounds and various related derivatives were tested against a number of mycobacteria in comparison with INH and streptomycin (SM). Although 4-(4-pyridinyl)pyrrole-3-carboxyhydrazide 34 was not active, some related derivatives showed interesting antitubercular activities. Among them, derivative 19 was the most potent both against M. tuberculosis (MIC = 1.47 μM) and M. avium (MIC = 4.40 μM), a non- tuberculous agent responsible of fatal infection in AIDS patients. Compounds 15 and 33 also were endowed with appreciable activities against M. tuberculosis and M. avium.
