2004 Folia Pharm. Univ. Carol. 31—32 Pag. 53—58




Study of Antimycobacterial 5-Methyl-N-pyridylsalicylamides

Karel Waisser1 (waisser@faf.cuni.cz), Kateřina Dražková1, Josef Matyk1, Jiří Kuneš1, Jarmila Kaustová2

1 Department of Inorganic and Organic Chemistry, Charles University in Prague, Faculty of Pharmacy in Hradec Králové, Czech Republic
2 Department of Diagnosis Mycobacteria, Regional Institute of Public Health, Ostrava, Czech Republic



Summary

A series of derivatives of substituted 5-methyl-N-pyridinyl salicylamides was synthesized. The compounds were evaluated for in vitro antimycobacterial activity against M. tuberculosis, Mycobacterium avium and two strains of Mycobacterium kansasii. The compounds are antimycobacterial inactive. Twenty seven of new compounds were synthesized in our last three papers. From our this and other two our previous paper we concluded: a) In drug design of development of antimycobacterial agents in series of N-heteroarylsalicylamides is necessary eliminate every structure with steric hindrance of amide groups. b) The substitution of salicyl-moiety by methyl in position 5 is necessary eliminate, as well.