Preparation of phenyl and benzylguanidine compounds as antimicrobial compounds, compositions and methods
Potter BVL., Nigam Y., Dudley E., Su X., Dohle W., Normanton JR.
A compd. of formula I [wherein A and B are independently (un)substituted aryl or heteroaryl; X is -(R1)W(R2)-, Y is a bond, C1-3 alkylene, C=O, etc.; W is O, S, SO, SO2, NH, N(C1-6)alkyl, etc.; Z is -N(R6)C(=R9)N(R7)R8; R1 and R2 are independently a bond or C1-3alkylene; R6, R7, and R8 are independently H, C1-6alkyl, CN, etc.; R9 is O, S, SO, SO2, etc.] or a pharmaceutically active salt or N-oxide thereof, are claimed and exemplified. Example compd. II·TFA was prepd. from N,N'-di-Boc deprotection of the corresponding intermediate in 99% yield. Candidate compds. of I were evaluated for antibacterial activity expressed as min. inhibitory concns. against Escherichia coli and methicillin resistant Staphylococcus aureus. The compds. are useful in the treatment or prophylaxis of bacterial infections in an animal. [on SciFinder(R)]