Heterocyclic Amplifiers of Phleomycin. VIII. Mono- Bis-(5'-substituted 1',3',4'-thiadiazol-2'-yl)pyridines and Mono(5'-substituted 1',3',4'-thiadiazol-2'-ylmethyl)pyridines

Abstract

A series of mono- and bis -(5′-substituted 1′,3′,4′-thiadiazol-2′- yl )pyridines with strongly basic side chains, e.g., 3,5-bis[5′(2′-N,N- dimethylaminoethylthio )-1′,3′,4′-thiadiazol-2′-yl]pyridine (1), and (5?-substituted 1′,3′,4′-thiadiazol-2′-ylmethyl)pyridines have been prepared for evaluation as amplifiers of phleomycin. Five of the six bis (5′-substituted 1′,3′,4′-thiadiazol-2′-yl)pyridines were themselves antibacterial under the test conditions, but compound (1) and the mono(5′-substituted 1′,3′,4′-thiadiazol-2′-yl)-pyridines and -methylpyridines displayed moderate two-to-three-star activity.