tuberculosis inhibitor 1

Tuberculosis inhibitor 1 is a potent and non-cytotoxic inhibitor of trypanosoma brucei growth (EC50: 5 nM).

Tuberculosis inhibitor 12（compound 12）作为恶二唑衍生物，表现出对结核分枝杆菌的显著抑制作用。在7H9-Tw-OADC介质中，Tuberculosis inhibitor 12（20 μM）展现了82%的抑制率，而在相同条件下抑制率为78%。

Tuberculosis inhibitor 11 (Compound 14) 是一种增强抗结核药物针对分枝杆菌活性的化学化合物。

Tuberculosis inhibitor 10 对 MSMEG_6649 的酶活性呈现中等抑制效果，并增强了 PAS 对分枝杆菌的抑制作用。

LeuRS-IN-1 是一种具有口服活性和高效性的结核分枝杆菌 leucyl-tRNA 合成酶抑制剂，具有抗白血病活性和抗疟活性，抑制 M.tb LeuRS，抑制 HepG2 蛋白合成，可用于研究白血病。

D-Cycloserine (RO-1-9213) 是一种抗生素，靶向细菌细胞壁肽聚糖生物合成酶。它是一种NMDA 部分激动剂，可以改善认知功能，可研究耐多药结核病。

LeuRS-IN-1 hydrochloride 是一种具有口服活性和高效性的结核分枝杆菌 leucyl-tRNA 合成酶抑制剂，具有抗白血病活性和抗疟活性，抑制 M.tb LeuRS，抑制 HepG2 蛋白合成，可用于研究白血病。

MenA-IN-2是一种有效的 1,4-二羟基-2-萘甲酸酯异戊二烯转移酶 (MenA) 抑制剂，对 MenA 的 IC50 值为 22 µM，对结核分枝杆菌 (Mtb) 的 GIC50 值为 10 µM。MenA-IN-2 Mtb 的持续传播具有抑制作用。

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).

Norverapamil hydrochloride (D591 hydrochloride) 是 Verapamil 的 N-去甲基代谢物，是 L 型钙通道阻滞剂和 P-糖蛋白 (P-gp) 功能抑制剂。

VEGFR-2 InhA-IN-1是一种含吡唑结构的双功能抑制剂，既具有抗结核活性也有抗血管生成的效用。该化合物对结核分枝杆菌H37Rv株展示出有效的抑菌作用（MIC=6.25 μg mL），同时对VEGFR-2的抑制也相当显著（IC50=15.27 nM）。

InhA-IN-8 (compound 6c) 为一种抗结核分枝杆菌InhA（烯酰ACP还原酶）的口服有效抑制剂。此化合物对Mtb UalRv显示出较高的抑制效果（MIC = 0.5-1 μg mL）。InhA-IN-8 同时也适用于进行急性结核模型小鼠的实验研究。

Soulattrolide是一种由Calophyllum (Calophyllaceae)雨林树叶合成的天然香豆素，作为HIV-1逆转录酶（RT-HIV-1）的强效抑制剂，并显示出对Mycobacterium tuberculosis的活性。

Biotin protein ligase-IN-1 (Compound Bio-9) 是一种生物素蛋白连接酶 (BPL) 抑制剂，Kd值为7 nM。它显示出对金黄色葡萄球菌（包括MRSA和MSSA）及结核分枝杆菌的抗菌活性，MIC值分别为0.2 μM和20 μM。

Pks13-IN-1 (Compound 44) 是一种口服有效的 Mycobacterium tuberculosis 聚酮合酶 13 (Pks13) 抑制剂。它对结核分枝杆菌 H37Rv 菌株的抑制浓度 (MIC) 为 0.07 μM。在小鼠模型中，Pks13-IN-1 展示了抗菌活性。

DXR-IN-4 (Compound 12a) 是 1-脱氧-D-木酮糖 5-磷酸还原异构酶 (DXR) 的有效抑制剂。它在恶性疟原虫 Plasmodium falciparum、大肠杆菌 Escherichia coli 和结核分枝杆菌 Mycobacterium tuberculosis 中，分别抑制 DXR 的 IC50 值为 18、4.9 和 89 nM。DXR-IN-4 展现了抗疟活性，对恶性疟原虫菌株 3D7 和 Dd2 的抑制作用的 IC50 分别为 11 μM 和 12 μM。

Mtb against-1 (compound 17af) 是一种结核分枝杆菌抑制剂，其对野生型菌株的IC90为1.2 μM，对LepB低变形菌株的IC90为0.9 μM。

BioA-IN-1 (Compound 15) 是一种抑制结核分枝杆菌生物素合成途径关键酶BioA的抑制剂，其IC50为0.195 μM。BioA-IN-1 显示出抗菌活性，并且没有细胞毒性。

10-DEBC hydrochloride 是选择性的Akt 抑制剂，IC50为 1.28 μM。10-DEBC hydrochloride 也是一种新型抗肺结核的化合物。

TBA-7371 (DprE1-IN-1) 是一种非共价 DprE1有效抑制剂，具有强大的抗结核活性。

OPC-167832 is a potent and orally active dprE1 Inhibitor with an IC50 of 0.258 μM. OPC-167832 has antituberculosis activity and can be used for the research of tuberculosis caused by Mycobacterium tuberculosis[1]. OPC-167832 exhibits very low MICs against laboratory strains of M. tuberculosis H37Rv (MIC: 0.0005 μg ml) and Kurono (MIC: 0.0005 μg ml) and strains with monoresistance to rifampin (RIF), isoniazid (INH), ethambutol (EMB), streptomycin (STR), and pyrazinamide (PZA) (MIC: 0.00024-0.001 μg ml). However, OPC-167832 has minimal or no activity against standard strains of nonmycobacterial aerobic and anaerobic bacteria[1].The IC90 values of OPC-167832 against intracellular M. tuberculosis strains H37Rv and Kurono are 0.0048 and 0.0027 μg ml, respectively. OPC-167832 shows bactericidal activity against intracellular M. tuberculosis at a low concentration, and the bactericidal activity is saturated at concentrations of 0.004 μg ml or higher[1]. OPC-167832 (oral administration; 0.625-10 mg kg) exhibits a good pharmacokinetic characteristic. The plasma reaches peak at 0.5 h to 1.0 h (tmax) and is eliminated with a half-life (t1 2) of 1.3 h to 2.1 h OPC-167832 distribution in the lungs is approximately 2 times higher than that in plasma, and the Cmax and AUCt of OPC-167832 in plasma and the lungs shows dose dependency[1].OPC-167832 (oral administration; 0.625-10 mg kg; 4 weeks) significantly reduces lung CFU compared to the vehicle group. The dose-dependent decrease of lung CFU is observed from 0.625 mg kg to 2.5 mg kg. In a M. tuberculosis Kurono-infected ICR female mice model. OPC-167832 combines with DMD, BDQ, or LVX via oral gavage exhibits significantly higher efficacies than each single agent alone[1].[1].OPC-167832 (oral gavage; 2.5 mg kg; combination with DCMB; 12 weeks) demonstrates the most potent efficacy when compares with DC, DCB. The lung CFU count after 6 weeks of treatment is below the detection limit, and at the end of just 8 weeks of treatment, the bacteria in the lungs of all the evaluated mice had already been eradicate[1]. [1]. Norimitsu Hariguchi, et al. OPC-167832, a Novel Carbostyril Derivative with Potent Antituberculosis Activity as a DprE1 Inhibitor.Antimicrob Agents Chemother. 2020 May 21;64(6):e02020-19.

S.pombe lumazine synthase-IN-1 is an inhibitor of lumazine synthases with Ki values of 243 μM and 9.6 μM for Schizosaccharomyces pombe and Mycobacterium tuberculosis lumazine synthases, respectively[1]. [1]. Arindam Talukdar, et al. Discovery and Development of a Small Molecule Library With Lumazine Synthase Inhibitory Activity. J Org Chem. 2009 Aug 7;74(15):5123-34.

ML338 is a selective small molecule inhibitor probe specifically targeting non-replicating Mycobacterium tuberculosis bacilli. It exhibits potent activity against non-replicating M. tuberculosis, with IC90 and IC99 values of 1 μM and 4 μM, respectively, as determined by CFU. This compound, ML338, is an invaluable tool for identifying essential functions and vulnerabilities of M. tuberculosis bacilli under nutrient deprivation conditions. Additionally, ML338 is highly useful for studying M. tuberculosis chemotherapy.