Synthesis of 2-benzylthiopyridine-4-carbothioamide derivatives and their antimycobacterial, antifungal and photosynthesis-inhibiting activity

A series of 2-benzylthiopyridine-4-carbonitriles 4 and a series of 2-benzyl thiopyridine-4-carbothioamides 5 were prepared. Their chemical structures w ere proved by IR and H-1 NMR data and by elemental analysis. The MIC assess ment was used for the estimation of their potential antimycobacterial and a ntifungal activity in vitro. The compounds were shown to be more active aga inst mycobacterial strains than the tested fungi. Their antimycobacterial a ctivity appears to be related mainly to the benzylthio moiety, while the an tifungal activity appears to be related to the carbothioamide group, Substi tuents on the benzylthio moiety of derivatives 5 modified antifungal activi ty, whereas they did not play any significant role in antimycobacterial act ivity. The inhibiting effect of 4 and 5 on the photochemical activity of sp inach chloroplasts was determined by IC50 values. The compounds exhibited a moderate photosynthesis-inhibiting activity. (C) Elsevier, Paris.