Čes. slov. farm. 2012, 61(3):127-129

High active potential antimycobacterial agents against Mycobacterium avium

Karel Waisser^1,*, Jiří Kuneš¹, Jiřina Stolaříková²

Charles University in Prague, Faculty of Pharmacy in Hradec Králové, Department of Inorganic and Organic Chemistry

² Regional Institute of Public Health

Derivatives of 3-phenyl-2H-1,3-benzoxazine-2,4(3H)-dione are active against Mycobacterium avium when substituted in position 7 with a methyl. One or two carbonyl groups have to be replaced with a thioxo group. High active derivatives are the compounds without substitution on the phenyl, or those substituted on the phenyl in position 3 or 4 with chlorine, bromine or a methyl. The substitution in position 3 and 4 with two atoms of chlorine lowers the activity. The compounds are active against INH resistant strains. We synthesized other 44 derivatives with a similar structure of the compounds as in the paper but substituted in position 7 with other substituents (chlorine, bromine methoxy). The activity against M. avium was poor. It can be concluded that a new group of compounds with an excellent activity against M. avium has been found.

Keywords: benzoxazine; thioxo group; Mycobacterium avium; antimycobacterial activity

Received: March 21, 2012; Accepted: April 24, 2012; Published: March 1, 2012  Show citation