t 3788

M-5011 is a non-steroidal anti-inflammatory drug and immunomodulator potentially for the treatment of inflammation and pain. M-5011 had an effective antinociceptive activity (ED50 value) of 0.63 mg/kg. M-5011 partially inhibits the generalized bone loss a

Rehmannioside A 是从中药地黄中提取的环烯醚萜苷,具有神经保护活性，通过抑制 NF-κB 和 MAPK 信号通路发挥作用。

1-Dodecylimidazole 是溶酶体活性洗涤剂。1-Dodecylimidazole 通过在溶酶体中的酸依赖性积累、溶酶体膜的破坏和半胱氨酸蛋白酶释放到细胞质中而导致细胞死亡。它显示出降胆固醇和广谱抗真菌活性。

1-Heptadecanol 是分离自Solena amplexicaulis 的长链伯醇，显示出抗菌活性。

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.

Oritavancin is a novel semisynthetic glycopeptide antibiotics. On August 6, 2014, the FDA approved oritavancin for treatment of skin infections. Oritavancin possesses potent and rapid bactericidal activity in vitro against a broad spectrum of both resistant and susceptible Gram-positive bacteria, including Staphylococcus aureus, MRSA, enterococci, and streptococci.

(E)-3,4-Dimethoxycinnamic acid 是天然化合物 3,4-dimethoxycinnamic acid 的活性较弱的异构体，来源于 Securidaca inappendiculata Hassk。其通过 ROS 介导信号通路在 L-02 细胞中发挥抗凋亡作用，在炎症与免疫研究中具有潜在应用。

(S)-Enzaplatovir ((S)-BTA-C585) is the S-enantiomer of Enzaplatovir. (S)-Enzaplatovir shows antiviral activities with an EC50 of 56 nM for respiratory syncytial viral (RSV)[1].

1,3-Dilinoleoyl-2-oleoyl-rac-glycerol is a triacylglycerol that contains linoleic acid at the sn-1 and sn-3 positions and oleic acid at the sn-2 position. It has been found in grape seed, pumpkin seed, soybean, sunflower, and wheat germ oils, with the highest content in grape seed oil.

Desacetyl cefapirin is an active metabolite of the cephalosporin antibiotic cefapirin .1 Desacetyl cefapirin is active against E. coli, K. pneumoniae, P. mirabilis, and S. aureus with MIC values of 120, 24, 34, and 0.42 μg/ml, respectively.References1. Jones, R.N., and Packer, R.R. Cefotaxime, cephalothin, and cephapirin: Antimicrobial activity and synergy studies of cephalosporins with significant in vivo desacetyl metabolite concentrations. Diagn. Microbiol. Infect. Dis. 2(1), 65-68 (1984). Desacetyl cefapirin is an active metabolite of the cephalosporin antibiotic cefapirin .1 Desacetyl cefapirin is active against E. coli, K. pneumoniae, P. mirabilis, and S. aureus with MIC values of 120, 24, 34, and 0.42 μg/ml, respectively. References1. Jones, R.N., and Packer, R.R. Cefotaxime, cephalothin, and cephapirin: Antimicrobial activity and synergy studies of cephalosporins with significant in vivo desacetyl metabolite concentrations. Diagn. Microbiol. Infect. Dis. 2(1), 65-68 (1984).

BHBM is an acylhydrazone with antifungal activity.1,2 It is active against C. neoformans in vitro (MIC80 = 1 μg/ml).2 BHBM (0.25, 1, and 4 μg/ml) inhibits the synthesis of glucosylceramide, which is essential to fungal cell division, in C. neoformans but not J774 murine macrophages.1 In vivo, BHBM (1.2 mg/kg per day) increases survival in a mouse model of C. neoformans infection. |1. Haranahalli, K., Lazzarini, C., Sun, Y., et al. SAR studies on aromatic acylhydrazone-based inhibitors of fungal sphingolipid synthesis as next-generation antifungal agents. J. Med. Chem. 62(17), 8249-8273 (2019).|2. Lazzarini, C., Haranahalli, K., Rieger, R., et al. Acylhydrazones as antifungal agents targeting the synthesis of fungal sphingolipids. Antimicrob. Agents Chemother. 62(5), e00156-00118 (2018).