antituberculosis

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-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-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-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-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-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。

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。

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。

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.

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。

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

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.

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。

MptpB-IN-2（化合物20）是一种高选择性的结核分枝杆菌蛋白酪氨酸磷酸酶B（MptpB）抑制剂，其对MptpB、MptpA和PTP1B的IC50值分别为0.64 μM、4.06 μM和4.14 μM。此化合物对Mtb H37Rv表现出较低的抗结核活性，MIC为64.9 μM。

DHFR-IN-10（化合物4c）是针对结核分枝杆菌DHFR的高效抑制剂，其IC50为4.21 μM，显示出卓越的抗结核活性。

Golotimod (SCV 07) hydrochloride 是一种免疫调节肽，具抗菌活性，能显著提升抗结核疾病研究效果。该化合物通过刺激胸腺和脾细胞增殖、改善巨噬细胞功能，展现其生物调节能力。此外，Golotimod hydrochloride 通过抑制STAT3信号传导，有效调节接受放疗或与顺铂联用治疗动物模型中的口腔粘膜炎持续时间和严重程度。还显示出对研究复发性生殖器单纯疱疹病毒 2 型 (HSV-2) 具有潜在应用价值。

Carbazomycin D is a bacterial metabolite that has been found inStreptomycesand has diverse biological activities.1,2It is active against the fungiT. asteroidesandT. mentagrophytes(MIC = 100 μg ml for both) and the bacteriumM. tuberculosis(IC50= 25 μg ml). Carbazomycin D is cytotoxic to MCF-7, KB, NCI H187, and Vero cells (IC50s = 21.3, 33.2, 12.9, and 34.3 μg ml, respectively).2 1.Naid, T., Kitahara, T., Kaneda, M., et al.Carbazomycins C, D, E and F, minor components of the carbazomycin complexJ. Antibiot. (Tokyo)40(2)157-164(1987) 2.Intaraudom, C., Rachtawee, P., Suvannakad, R., et al.Antimalarial and antituberculosis substances from Streptomyces sp. BCC26924Tetrahedron67(39)7593-7597(2011)

Danshenxinkun D has antituberculosis H_(37)Rv activity in vitro.

Steviolbioside (CCRIS-6025) 是一种存在于甜菊叶中的罕见甜味剂。它对几种人类癌细胞有抑制作用，对乳腺癌具有潜在的研究价值。