Inventors:
George E. Wright - Worcester MA, US
Wei-Chu Xu - Worcester MA, US
Neal C. Brown - Greenfield NH, US
Assignee:
GLSynthesis, Inc. - Worcester MA
International Classification:
C07D473/18, A61K031/522, A61P031/04, C09D005/14
US Classification:
106 1832, 544276, 544118, 5142342, 5142632, 51426337
Abstract:
The invention features compounds of the formula:
or a pharmaceutically acceptable salt thereof, wherein A is CRand B is N; wherein n is 0-3; wherein Ris (CH)—{(G)—(CH)}—L, in which G is CH, CH═CH, C≡C, CO, O, S, or NR, where Ris H or Calkyl, CHR, where Ris OH or Calkyl, CH(CRR), where each of Rand Ris, independently, H, halo, or Calkyl, OCO, CONR, NRCO, where each of Rand Ris, independently, H or Calkyl, SONH, or NHSO; in which m is 1-4, o is 0-4, p is 0-4, and q is 0-4. The compounds disclosed herein have potent anti-microbial, e. g. , both Gram-positive and Gram-negative anti-bacterial properties. The compounds inhibit DNA polymerase IIIC and DNA polymerase IIIE enzymes and thus act therapeutically by inhibiting the growth of a broad array of bacteria. The compounds can be administered to prevent or to treat Gram-positive or Gram-negative bacterial infections, e. g. , in eukaryotic cell cultures, animals, or humans.