5-nitrothiazole derivs antiparasitic anti-protozoal

摘要

Compounds (I): - X = O or SO, - R', R2, R3 and R4 = H, or an aliphatic, aralkyl, or aryl residue, all opt. substd. e.g. by halogen, NO2, O alkyl, CN, CO2H, CO2 alkyl, or SO3H. - or R' + R2 and/or R3 + R4 may form a 6-membered carbocyclic ring. - Anti-protozoals, active, e.g. vs. Entamoeba histolytica and Trichomonas vaginalis. - 3-methyltetrahydro-1,4-thiazine-1,1-dioxide (50.7g.) and 2-bromo-5-nitrothiazole (41.9g.) were refluxed 7h. in dioxan (500ml.), dild. with H2O (500ml.), cooled, filtered, washed (EtOH) and dried, giving I (39.0g., 71%), m.p. 223-4 deg. (from EtOH).