tuberculosis inhibitor 1

Tuberculosis inhibitor 1 is a potent, non-cytotoxic inhibitor of Trypanosoma brucei growth [EC50: 5 nM].

Tuberculosis Inhibitor 12, an oxadiazole derivative, effectively inhibits Mycobacterium tuberculosis, demonstrating inhibition rates of 82% and 78% at a concentration of 20 μM on 7H9-Tw-OADC media, respectively [1].

Compound 14, also known as Tuberculosis Inhibitor 11, enhances the antimycobacterial efficacy of antitubercular agent [1].

Tuberculosis Inhibitor 10 moderately inhibits the enzyme MSMEG_6649 and potentiates the antimycobacterial activity of PAS [1].

LeuRS-IN-1 is an orally active and potent Mycobacterium tuberculosis leucyl-tRNA synthetase inhibitor with anti-leukemic and anti-malarial activity, inhibits M.tb LeuRS, inhibits HepG2 protein synthesis, and can be used in leukemia research.

D-Cycloserine (RO-1-9213) is a broad spectrum antibiotic used as a second line agent for treatment of drug resistant tuberculosis, always in combination with other antituberculosis agents.

LeuRS-IN-1 hydrochloride is an orally active and highly potent inhibitor of Mycobacterium tuberculosis leucyl-tRNA synthetase with anti-leukemic activity and anti-malarial activity, inhibits M.tb LeuRS, inhibits HepG2 protein synthesis, and can be used in the study of leukemia.

MenA-IN-2 is a potent 1, 4-dihydroxy-2-naphthoate isopentadiene transferase (MenA) inhibitor with an IC50 value of 22 µM for MenA and 10 µM for Mycobacterium tuberculosis (Mtb). The continuous transmission of MenA-IN-2 Mtb has inhibitory effect.

FadD32 inhibitor -1 has anti-tuberculosis activity and is an effective FadD32 inhibitor.

MtbHU-IN-1 is a Mycobacterium tuberculosis nucleoid-associated protein HU (MtbHU)inhibitor(binding to WT MtbHU with a Kd of 98 nM).

3-(1-Carboxyvinyloxy)benzoic acid is a dual enzymatic inhibitor of MbtI from Mycobacterium tuberculosis and arginine synthase from Serratia marcescens, exhibiting Ki values of 500 μM and 3.2 μM respectively, 3-(1-Carboxyvinyloxy)benzoic acid display measurable antibacterial activity that supports its application as a mechanistic probe and lead compound for anti-infective and antimicrobial drug discovery research.

Norverapamil hydrochloride (D591 hydrochloride) ((±)-Norverapamil hydrochloride) is an N-demethylated metabolite of Verapamil and it is an L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor.

VEGFR-2/InhA-IN-1, a dual inhibitor based on pyrazole, targets InhA and VEGFR, exhibiting both anti-tuberculosis and anti-angiogenic properties. It demonstrates effective antibacterial activity against the Mycobacterium tuberculosis H37Rv strain (MIC = 6.25 μg/mL) and significantly suppresses VEGFR-2 activity (IC 50 = 15.27 nM).

InhA-IN-8 (compound 6c) serves as an orally effective inhibitor of the Mycobacterium tuberculosis enzyme InhA (enoyl-ACP reductase). This compound demonstrates robust inhibitory activity against Mtb H37Rv, with a minimum inhibitory concentration (MIC) ranging from 0.5 to 1 μg/mL. Additionally, InhA-IN-8 is utilized in studies involving acute tuberculosis models in mice.

Soulattrolide, a naturally occurring coumarin synthesized by Calophyllum (Calophyllaceae) rainforest tree leaves, acts as a potent inhibitor of reverse transcriptase from HIV-1 (RT-HIV-1) and exhibits activity against Mycobacterium tuberculosis.

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.

Pks13-IN-1 (Compound 44) is an orally active inhibitor of Mycobacterium tuberculosis polyketide synthase 13 (Pks13). It inhibits the M. tuberculosis H37Rv strain with a minimum inhibitory concentration (MIC) of 0.07 μM. In mouse models, Pks13-IN-1 demonstrates antibacterial activity.

DXR-IN-4 (Compound 12a) is an inhibitor of 1-deoxy-D-xylulose 5-phosphate reductoisomerase (DXR). It effectively inhibits DXR in Plasmodium falciparum, Escherichia coli, and Mycobacterium tuberculosis, with IC50 values for PfDXR, EcDXR, and MtDXR at 18, 4.9, and 89 nM, respectively. Additionally, DXR-IN-4 demonstrates antimalarial activity against Plasmodium falciparum strains 3D7 and Dd2, with IC50 values of 11 μM and 12 μM.

Mtb against-1 (compound 17af) is an inhibitor of Mycobacterium tuberculosis, demonstrating an IC90 of 1.2 μM against wild-type strains and 0.9 μM against low-permeability LepB strains.

BioA-IN-1 (Compound 15) is an inhibitor of the key enzyme BioA in the biotin biosynthesis pathway of Mycobacterium tuberculosis, with an IC50 value of 0.195 μM. It exhibits antibacterial activity without cytotoxicity.

SufS-IN-1, a (2R,3R)-3-ethoxycarbonylaziridine-2-carboxylic acid (EAC), acts as a selective type II cysteine desulfurase (SufS) inhibitor. It significantly inhibits SufS activity by forming a stable PLP-ligand complex through covalent bonding with the cofactor PLP. SufS-IN-1 is applicable in the study of pathogenic microorganisms such as [Plasmodium falciparum], [Staphylococcus aureus], and [Mycobacterium tuberculosis].

NADH-IN-3 (Compound C4-1) is an NADH inhibitor with a minimum inhibitory concentration (MIC) of 4 μg/mL (13.042 μM) against the type II NADH dehydrogenase of Mycobacterium tuberculosis (Mtb). It effectively blocks ATP synthesis and demonstrates potent inhibitory effects on both single-drug (Rifampicin and Isoniazid) and multidrug-resistant (Mtb) strains, exhibiting antibacterial activity while maintaining low cytotoxicity towards HepG2 cells (SI: 16.52).

10-DEBC hydrochloride is a selective Akt inhibitor with an IC50 value of 1.28 μM that has also been identified as a novel anti-tuberculosis research compound, supporting investigations into Akt signaling modulation, host–pathogen interactions, and therapeutic strategies targeting kinase-regulated survival pathways in infectious disease models.

TBA-7371 (DprE1-IN-1) is a potent inhibitor of DprE1 and PDE6.