3033990-94-9
Chemical Structure
AAP-SO2
- CAS No.: 3033990-94-9
- Formula:C26H26FN3O4S
- Molecular Weight:495.57
InChIKey: GDQUFAMUOYIJII-HSZRJFAPSA-N
SMILES: FC1=CC=CC=C1C(N[C@H](CC2=CC=CC=C2)C(NC3=CC=CC=C3N4CCS(CC4)(=O)=O)=O)=O
Biological Activity: AAP-SO2 is a Bactericide and Mycobacterium tuberculosis RNA polymerase (Mtb RNAP) inhibitor, with an IC50 of 0.025 μM against Mtb RNAP. AAP-SO2 allosterically slows the nucleotide addition rate during transcriptional elongation and enhances transcription termination efficiency. AAP-SO2 exhibits increased activity against βS450L-type Mtb, possesses activity against non-replicating Mtb, and shows whole-cell activity against Mtb and related mycobacterial species. AAP-SO2 reduces the overall emergence rate of Rifampicin (HY-B0272) tolerance in Mtb, alters the mutation spectrum, and decreases the proportion of βS450L-type Rifampicin-resistant mutants. AAP-SO2 acts synergistically with Rifampicin to kill non-replicating Mtb in a rabbit caseous necrosis model. AAP-SO2 can be used for the research of tuberculosis[1].
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AAP-SO2 | AAP-SO2 is a Bactericide and Mycobacterium tuberculosis RNA polymerase (Mtb RNAP) inhibitor, with an IC50 of 0.025 μM against Mtb RNAP. AAP-SO2 allosterically slows the nucleotide addition rate during transcriptional elongation and enhances transcription termination efficiency. AAP-SO2 exhibits increased activity against βS450L-type Mtb, possesses activity against non-replicating Mtb, and shows whole-cell activity against Mtb and related mycobacterial species. AAP-SO2 reduces the overall emergence rate of Rifampicin (HY-B0272) tolerance in Mtb, alters the mutation spectrum, and decreases the proportion of βS450L-type Rifampicin-resistant mutants. AAP-SO2 acts synergistically with Rifampicin to kill non-replicating Mtb in a rabbit caseous necrosis model. AAP-SO2 can be used for the research of tuberculosis. | |||||||||||||||||||||
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Keywords
