| 摘要 |
Thiazole sulphonamide compounds of general formula (I), or salts or prodrugs thereof: (Formula I) wherein R1 is hydrogen, halogen, CN or optionally substituted C1-6alkyl; R11 is hydrogen or C1-4alkyl optionally substituted with halogen or hydroxyl; Y1 is a bond or C1-3alkylene; A1 is optionally substituted C6-10aryl, 5-10 membered heteroaryl, or optionally substituted 3-10-membered carbocyclyl or heterocyclyl; Y2 is (Het)p(Alk1)q- or (Het2)t-(Alk2)-(Het3)-(Alk3)s; p, q, r and s are 0 or 1; Alk1, Alk2 or Alk3 are optionally substituted C1-6alkylene, C2-6alkenylene or C2-6alkynylene such that if two alkyl substituents are present on the same carbon atom in the alkylene, alkenylene or alkynylene moiety they form together with the C atom to which they are attached a C3-6cycloalkyl ring; Het1, Het2 and Het3 are O, S, SO2, NR8b, C(O), C(O)NR8b, NR8bC(O) or C(N-OR8b)-; R8b is H or optionally substituted C1-4alkyl; A2 is is optionally substituted C6-10aryl, 5-10-membered heteroaryl, or optionally substituted 3-10-membered carbocyclyl or heterocyclyl; may be useful for inhibiting metallo-β-lactamase (MBL) enzymes, including NDM-1, and therefore useful in combination with β-lactam antibiotics in the prevention and treatment of bacterial infection. The corresponding ester prodrug compounds of formula (II) are also detailed. |
