pyrazinamide

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。

Pyrazinamide-d3 是 Pyrazinamide 的氘代化合物。Pyrazinamide 的 CAS 号为 98-96-4。Pyrazinamide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。

Pyrazinamide-KLH 是 Pyrazinamide 与 血蓝蛋白 (KLH) 结合形成的抗原-佐剂偶联物。此偶联物可通过缀合抗原与蛋白佐剂来增强疫苗模型中抗原特异性抗体的产生，同时不影响蛋白质折叠及不破坏主要表位。它还能增强交叉呈递及抗原特异性 T 细胞的产生。

Pyrazinamide-BSA 是由 Pyrazinamide与牛血清白蛋白 (BSA) 缀合形成的抗原-佐剂偶联物。通过这种缀合方式，能够增强疫苗模型中抗原特异性抗体的生成。此缀合物保持蛋白质折叠的完整性，不破坏主要表位，并促进交叉呈递和抗原特异性 T 细胞的产生。

5-Hydroxypyrazine-2-Carboxylic Acid is a metabolite of anti-tuberculosis drug pyrazinamide.

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.