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。

Kuwanon G (Moracenin B) 是一种从桑树中得到的黄酮类蛙皮素受体拮抗剂，具有杀菌作用。

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.