The antituberculous properties of some derivatives of 2H-1,3-benzoxazine.

Abstract

The bacteriostatic concns. of 3,4-dihydro-3-cyclohexyl-6-bromo-2H-1,3-benzoxazine (m.p.: free base = 92-3°, -HCl = 240-3°) (I), 3,4-dihydro-3-benzyl-6-methyl-2H-l,3-benzoxazine (m.p.: free base = 79-80°, -HCl = 110-12°) (II), 3,4-dihydro-3-benzyl-6-bromo-2H-1,3-benzoxazine (m.p.: free base = 85-7°, -HCl = 182-4°) (III), 3,4-dihydro-3-ethyl-6-bromo-2H-1,3-benzoxazine (m.p.: -HCl = 171-2°) (IV), and 2,3-dihydro-2-methyl-1H-naphth[1,2-e]-m-oxazine (m.p.: free base = 67-8°, -HCl = 190-3°) (V) against saprophytic Mycobacterium were as follows: Myc. 297, I 3.9: II 31; III 3.9; IV 62; V 7.8; Myc. smegmatis I 7.8, II 31, III 7.8, IV 31, V 15.5; Myc. H37Rv: I 7.8, II 31, III 3.9; IV 11.5, V 15.5 (concn. units not given). [on SciFinder(R)]