tuberculosis inhibitor 9

Tuberculosis inhibitor 9 (compound 3d), a 3-methoxy-2-phenylimidazo[1,2-b]pyridazine derivative, exhibits potent activity against Mycobacterium tuberculosis and Mycobacterium marinum, with an MIC 90 of 0.64 μM for both organisms [1].

Biotin protein ligase-IN-1 (Compound Bio-9) is an inhibitor of biotin protein ligase (BPL) with a Kd of 7 nM. This compound exhibits antimicrobial activity, with minimum inhibitory concentration (MIC) values of 0.2 μM against Staphylococcus aureus (including MRSA and MSSA) and 20 μM against Mycobacterium tuberculosis.

Mtb-IN-9 (Compound M1) is a selective Mtb inhibitor that suppresses the activity of MtbFadD32 and MtbFadD28. In a chronic infection model using BALB/c mice, Mtb-IN-9 reduced the survival rate of Mtb in infected macrophages and decreased Mtb burden and tuberculous granulomas. It holds promise for tuberculosis research.

InhA-IN-9 (compound 7h) is an inhibitor of the Mycobacterium tuberculosis enzyme InhA (an enoyl ACP reductase). It has the ability to bind with InhA and demonstrates anti-tuberculosis activity with a MIC value of 2 μg/mL.

MtTMPK-IN-9 is a moderately potent inhibitor of Mycobacterium thymidylate kinase (MtbTMPK) (IC50: 48 μM).MtTMPK-IN-9 has submicromolar activity against Mycobacterium but no significant cytotoxicity.MtTMPK-IN-9 can be used to study tuberculosis.

SEQ-9 is an orally active inhibitor of the Mycobacterium tuberculosis (Mtb) 23S bacterial ribosome, with an inhibitory concentration (IC50) around 170 nM against unmethylated Mtb ribosomes and potent effects on A2296 methylated ribosomes. It is used in research on bacterial infections and drug resistance [1].