2005
Thiadiazole derivatives
R 0300
Synthesis and Antitrypanosomal Profile of New Functionalized 1,3,4-ThiaDerivatives, Designed as Non-mutagenic Megazol
15- 123 diazole-2-arylhydrazone
Analogues. — The design concept of the arylhydrazone derivatives is based on the
introduction of the arylhydrazone moiety in the heterocyclic framework of megazol, in
order to act, in the structural pattern of the lead compound, as a radical scavenger group.
The evaluation of the activity against bloodstream trypomastigote forms of T. cruzi
identifies brazilizone A (Vc) as a new potent trypamomicide prototype. —
(CARVALHO, S. A.; DA SILVA, E. F.; SANTA-RITA, R. M.; DE CASTRO, S. L.;
FRAGA*, C. A. M.; Bioorg. Med. Chem. Lett. 14 (2004) 24, 5967-5970; Lab.
Avaliacao Sint. Subst. Bioativas, Fac. Farm., Univ. Fed. Rio de Janeiro, 21944 Rio de
Janeiro, Brazil; Eng.) — H. Hoennerscheid