antituberculosis

Cefsulodin sodium (Sulcephalosporin) 是β内酰胺抗生素，对缘脓杆菌和肠杆菌有活性。

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。

Macozinone (PBTZ169) 是具有杀菌作用的苯并噻嗪酮，也有抗结核作用。它也是一种 DprE1有效抑制剂，可通过与活性位点 Cys387 残基形成共价键来抑制必需的黄素蛋白 DprE1。

DprE1-IN-2 是 DprE1抑制剂，IC50为 28 nM，有抗结核作用。

Antituberculosis agent-5是一种用于高通量测定的小分子。

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。

Antituberculosis agent-12 (compound 3408) 为狭谱磷酸前药，主要用于抑制耐药性结核感染。

Antituberculosis agent-8 是一种抗结核剂，对M. tuberculosis H37Rv 的 MIC 值为 3.53 μM (1.6 μg mL)。Antituberculosis agent-8 对A. niger 也显示出良好的抗真菌 (antifungal) 活性，MIC 为 62.50 μM。

Antituberculosis agent-2 (Compound 8d) 是一种针对耐多药结核病和药物敏感结核病均有效的抗结核剂。Antituberculosis agent-2 在小鼠和人类中显示出良好的微粒稳定性，具有低细胞毒性和可接受的口服生物利用度。Antituberculosis agent-2 具有抗结核活性。Antituberculosis agent-2 对结核分枝杆菌 H37Rv、13946 和 14862 的 MIC 值分别为0.454、1.757 和 1.644 μg mL。

Antituberculosis agent-3 是一种具有抗霉菌作用的抗结核剂，对结核杆菌 H37Rv 株的生长具有抑制作用，其 MIC 值为 12.5 μg mL。

Antituberculosis agent-9 (Compound 5a) 是一种具有口服活性的抗结核剂，对H37Ra 的MIC 为 0.5 μg mL。

Antituberculosis agent-6 是一种有效的抗结核分枝杆菌 (antimycobacterial) 剂。Antituberculosis agent-6 对M. tuberculosis 显示出显著的抑制活性，MIC 为 3.49 μM。Antituberculosis agent-6 还对A. niger 表现出良好的抗真菌 (antifungal) 活性，MIC 为 62.50 μM。 Antituberculosis agent-6 表现出高胃肠道吸收。

Antituberculosis agent-1 (Compound 8a) 是一种抗结核剂，对 M. tuberculosisH37Rv 的 MIC 值为 3.84 μg mL。

Antituberculosis agent-13 (Compound 11) 是一种具有抗结核活性的化合物，对Mycobacterium tuberculosis野生型和突变菌株的IC50为4-62.5 nM。此外，Antituberculosis agent-13 还显示出抗白血病活性，对MOLM-13的IC50为3.8 μM。

NITD-916 是一种具有口服活性和高度亲脂性的分枝杆菌烯酰还原酶 InhA 抑制剂，IC50 为 570 nM。NITD-916是一种有有效的 4-羟基-2-吡啶酮衍生物， 与 InhA 和 NADH 形成三元复合物，阻止进入脂肪酰基底物结合袋。NITD-916 具有抗结核活性。

Imidazoleacetic acid hydrochloride (I4AA) 是咪唑衍生物，具有潜在的抗结核性能。它还用于制备β-分泌酶的酰基胍抑制剂。

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。

Q151 is an IMPDH inhibitor. It also is a potential antituberculosis agent.

Chrysomycin A 是一种可来自链霉菌的抗生素。在胶质母细胞瘤中，Chrysomycin A 通过 Akt GSK-3β β-catenin 信号通路抑制癌细胞的增殖、迁移和侵袭。 表现出抗肿瘤和抗结核和 MRSA 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.

Sativan possesses a broad spectrum of antimicrobial activity against bacteria and phytopathogenic fungi, it exhibits antituberculosis activity against Mycobacterium tuberculosis H37Rv, with the MIC value of 50 ug mL.

HT1171 是一种高效且具选择性的结核分枝杆菌蛋白酶体抑制剂。对结核分枝杆菌 H37Rv 具有显著的抗结核活性，MIC90为 2 μg mL，MIC为 4 μg mL。浓度为 100 μM 时，对人正常肝细胞 L02 的抑制率为 53.8%。HT1171 可用于抗结核药物研究。

Carbazomycin A is a bacterial metabolite that has been found in Streptomyces and has diverse biological activities.1,2It is active againstS. aureus,T. asteroides, andT. mentagrophytes(MIC = 12.5 μg ml for all), as well as the plant pathogenic fungusP. oryzae(MIC = 25 μg ml). Carbazomycin A is cytotoxic to MCF-7, KB, NCI H187, and Vero cells (IC50s = 26.2, 30.1, 18.4, and 32.6 μg ml, respectively).2 1.Sakano, K.-I., Ishimaru, K., and Nakamura, S.New antibiotics, carbazomycins A and B. I. Fermentation, extraction, purification and physico-chemical and biological propertiesJ Antibiot. (Tokyo)33(7)683-689(1980) 2.Intaraudom, C., Rachtawee, P., Suvannakad, R., et al.Antimalarial and antituberculosis substances from Streptomyces sp. BCC26924Tetrahedron67(39)7593-7597(2011)

Antitubercula agent-38，一种具有效抗结核活性的口服苯并噻嗪酮(BTZ)衍生物，其特点为低心脏毒性和低细胞毒性。