The present invention relates to novel pyrido-imiddazo rifamycines of Formula (I) as defined below and characterized by a highly selective antibacterial activity and low absorption by oral route. (I) wherein R and R1 may be H, (AA) with the proviso that: when I (BB) then R1 = H and R2 = CH3 CO- or H; when (CC) then R= H and R2= CH3 CO- or H; when (DD) then Rj = H and R2 = CH3 CO- or H; and when (EE) then R = H and R2 = CH3 CO- or H; wherein R3 and R4 are the same or different and selected from the group comprising hydrogen, linear or branched C1 -C10 alkyl, optionally substituted with one or more substituents selected from aminoalkyi, alkoxy, phenoxy, or sulfo, and aryl, optionally mono- or disubstituted with C1 -C4 alkyl or alkoxy groups, halogen, amino, nitro; or R3 and R4 taken together with two consecutive carbon atoms of the pyridine core may form a phenyl ring, optionally substituted with C1 -C4 alkyl, or a 5- or 6-membered heterocyclic ring, optionally substituted with C1_ C4 alkyl, R5 is selected from the group comprising hydrogen, hydroxy, linear or branched C1 -C10 alkyl, optionally substituted with one or more substituents selected from aminoalkyi, alkoxy, phenoxy, or sulfo, and aryl optionally mono- or disubstituted with C1 -C4 alkyl or alkoxy groups, halogen, amino, nitro.
本发明涉及以下定义的新型
吡啶咪唑呋喃霉素化合物的
化学式(I)，其具有高度选择性抗菌活性和口服途径低吸收的特征。其中R和R1可以是H，(
AA)条件是：当I (BB)时，R1 = H且R2 =
CH3 CO-或H；当(CC)时，R= H且R2= CO-或H；当(DD)时，Rj = H且R2 = CO-或H；当(EE)时，R = H且R2 = CO-或H；其中R3和R4相同或不同，选自氢、线性或支链的C1-C10烷基，可选地取代为来自
氨基烷基、烷氧基、苯氧基或磺酰基的一个或多个取代基，以及芳基，可选地单取代或双取代为C1-C4烷基或烷氧基、卤素、
氨基、硝基；或者R3和R4连同
吡啶核的两个相邻碳原子可以形成一个苯环，可选地取代为C1-C4烷基，或者一个5-或6-成员杂环，可选地取代为C1-C4烷基，R5选自氢、羟基、线性或支链的C1-C10烷基，可选地取代为来自
氨基烷基、烷氧基、苯氧基或磺酰基的一个或多个取代基，以及芳基可选地单取代或双取代为C1-C4烷基或烷氧基、卤素、
氨基、硝基。
