No abstract

Das Thiadiazol (I) reagiert mit den Phenacylbromiden (II) zu den Thiadiazol‐phenacylsulfiden (III); diese gehen mit Polyphosphorsäure in die heterocyclischen Ammoniumsalze (IV) über.

In search for novel anti-cancer and antimicrobial agents with promising pharmacotoxicological profile, the synthesis of some substituted 4-halofuran-2(5H)-ones (8a-l, 9, 11) and derived halogenated quinoxalin-2(1H)-ones (12a-d) is described. Some of the halogenated furanones were readily oxidized to the corresponding 2-bromo-2-propenoic acids (13a-c) with hydrogen peroxide in alkaline medium. Twenty-two compounds were preliminary tested for their in vitro activity against three bacteria and one fungus and revealed encouraging activity. On the other hand, three compounds were screened as anti-cancer agents using cell line panel protocol and 22 compounds were subjected to cycline-dependent kinases (CDKs) inhibition screening program but were inactive.Keywords 5-Aryl-4-halo-3-hydroxyfuran-2(5H)-ones Á 3-(2-Aryl-1-halovinyl)quinoxalin-2(1H)-ones Á 3-Aryl-2-bromo-2-propenoic acids Á Anti-cancer and anti-microbial properties

Die Aminothiadiazole (I) ergeben mit den Phenacylbromiden (II) die Phenacylthiadiazol‐hydrobromide (III), die beim Erhitzen in Gegenwart von Natriumacetat zu den Imidazothiadiazolen (IV) cyclisieren.

Die 2‐Hydrazino‐thiadiazole (I) werden in Ethanol oder Pyridin zu den Monoacylierungsprodukten (III), in Dioxan zu den zweifach acylierten Derivaten (IV) umgesetzt.