m. tuberculosis

Pyrazinamide (Pyrazinecarboxamide) 是一种口服抗结核类抗生素。它是一种前药，通过结核分枝杆菌pncA 基因编码的 PZase 烟酰胺酶转化为活性吡嗪酸形式。

C-215 是MmpL3抑制剂。它在 HTS 中被鉴定为对结核分枝杆菌具有独立的甘油活性，对哺乳动物细胞的非特异性毒性较低，对结核分枝杆菌的IC90=16 μM，并且能够有效抑制在巨噬细胞中生长的结核分枝杆菌。

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。

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.

Mycobacterium Tuberculosis-IN-6 (compound b1) 是一种结核分枝杆菌烯酰还原酶InhA的抑制剂，其IC50值为7.74 μM，可用于抗菌研究。

Mycobacterium Tuberculosis-IN-2 (化合物 29) 作为有效的细菌抑制剂，主要用于抑制Mycobacterium Tuberculosis。该化合物在结核病研究中具有显著应用价值，其最小抑菌浓度（MIC）范围为0.07-0.16 μM。

Gliotoxin 是一种次生代谢产物，由A. fumigatus 分泌，可以抑制巨噬细胞的吞噬作用和其他免疫细胞的免疫功能。它通过阻止 IκB 降解来抑制诱导型NF-κB 活性，从而诱导宿主细胞凋亡。它可以激活PKA 并增加细胞内 cAMP 浓度，调节肌动蛋白细胞骨架重排以促进A. fumigatus 内化到肺上皮细胞。

Mycobacterium Tuberculosis-IN-5 (Compound 11),作为5-Fluoroindole的盐酸盐形式,具有显著的抗菌功能,能够抑制Mycobacterium tuberculosis,其MIC值达到29.1 μM.此化合物在大鼠肝微粒体中显示良好的代谢稳定性,并且在小鼠体内展示出抗结核活性.

α-Viniferin 也称为2-芳基苯并呋喃类黄酮，是前列腺素H2合成酶抑制剂。具有抗阿尔茨海默病、抗结核、抗肿瘤、抗炎、抗糖尿病等多种药理活性

GSK572A 是一种新型且强效的EchA6强效抑制剂，可用来治疗肺结核。

GSK2556286 (GSK286) 是一种具有口服活性的结核分枝杆菌 (M. tuberculosis) 抑制剂。GSK2556286 对人巨噬细胞 (macrophages) 生长具有抑制作用，IC50值为 0.07 μM。GSK2556286对多重耐药 (MDR) 或广泛耐药 (XDR) 和药物敏感 (DS) 结核分枝杆菌均有效。

Lansoprazole sulfide (AG-1777，兰索拉唑硫醚)是Lansoprazole的活性代谢物，具有相似的活性。Lansoprazole是一种质子泵抑制剂和抗结核剂，对 Mycobacterium tuberculosis 的 IC50= 0.59 µM。

Sodium 4-aminosalicylate dihydrate (4-Amino-salicylic acid sodium salt) 是一种抗耐药性结核化合物。

BM212 是一种分枝杆菌膜蛋白 MmpL3抑制剂。它抑制结核分枝杆菌和部分非结核分枝杆菌，抗结核杆菌 H37Rv 菌株的 MIC 值为 5 µM。

GSK2200150A 是一种通过高通量筛选活动确定的抗结核剂，对 H37Rv 的 MIC 是 0.38 μM。

BB2-50F 是一种强效的M. tuberculosis多靶点生物能杀菌抑制剂，能够有效杀死复制型和非复制型M. tuberculosis。它通过抑制琥珀酸氧化，降低三羧酸 (TCA) 循环的活性，导致M. tuberculosis分泌琥珀酸。

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.

Anisofolin A has promising antimalarial activity (IC50 4.39 ± 0.25 uM). It has promising antimycobacterium activity [IC50 4.50 ± 0.75 uM (3.31 ug mL)] against M. tuberculosis H37Ra and at 100 ug mL, shows 55.6 % inhibition of M. bovis.

DHFR-IN-2 (化合物 4e) 是一种有效且非竞争性的MtDHFR 抑制剂，其IC50值为 7 μM。来自结核分枝杆菌 (MtDHFR) 的二氢叶酸还原酶具有很高的未开发潜力，可以成为抗结核病 (TB) 新药的靶标，因为它对病原体存活很重要。DHFR-IN-2可用于结核病(TB)研究。

Homo-BacPROTAC7 是一个 ClpC1NTDBacPROTAC 降解剂，可以靶向 ClpC2。Homo-BacPROTAC7 能有效杀死 M. tuberculosis。

Diaporthein B 是氧化程度极高的 pimarane 二萜之一。Diaporthein B 表现出抗结核分枝杆菌的活性，MIC 为 3.1 μg mL。Diaporthein B 显示对 HCT 116 和 LoVo 结肠癌细胞的 IC50为 1.5-3 μM L。

WX-081 是抗结核剂 (anti-tuberculosis)，对 M. tuberculosisH37Rv 表现出明显的抗分枝杆菌效果，并能够作用于药物敏感结核病 (DS-TB) 杆菌 (MIC: 0.083 μg ml) 和耐多药结核病 (MDR-TB) 菌株 (MIC: 0.11 μg ml)，对 hERG 通道表现出抑制作用 (IC50: 1.89 μM)。

Antituberculosis agent-7 是一种氧杂环丁基喹啉衍生物，对P. mirabilis 具有良好的抗菌活性，MIC 为 31.25 μM。Antituberculosis agent-7 对A. niger 显示出良好的抗真菌活性，MIC 为 62.5 μM。Antituberculosis agent-7 显示出优异的抗分枝杆菌活性，对结核分枝杆菌 H37Rv 的 MIC 为 3.41 μM。

sCNH240(2-Fluoro-N-[3-(3-thienyl)-5-isoxazolyl]benzenesulfonamide)是一种潜在的选择性 Rv1625c Cya 激活剂，具有良好的细胞渗透性和口服活性，在胆固醇补充的7H12培养基中对结核分枝杆菌（Mtb）H37Rv 株的IC90=1.24 µM，对 CYP2C19，CYP2C9 和hERG 通道具有抑制作用。