antimicrobial compound 1

Antimicrobial Compound 1 是一种烷基吡啶鎓化合物，尾部为 12C，头部为 4-羧基。 Antimicrobial Compound 1 对枯草芽孢杆菌和大肠杆菌具有抗菌活性。

Chlamydia pneumoniae-IN-1 是一种对衣原体有抑制作用的苯并咪唑类化合物，在低浓度下即可对肺炎衣原体产生抑制作用。Chlamydia pneumoniae-IN-1 具有抗菌活性，对CV-6菌株的 MIC 为12.6 μM，可用于研究肺部感染。

Linalool (Linalol) 是存在芫荽等植物中的单萜类天然产物，是竞争性NMDA 受体拮抗剂，具有抗肿瘤和抗心脏毒性的作用。它通过激活 Nrf2 诱导抗氧化防御和通过抑制 NF-κB 减少炎症反应来保护其免受 LPS GalN 诱导的肝损伤，具有镇痛、抗菌和抗炎的特性。

Antimicrobial agent-34（compound 4h）是一种高效抗菌剂，其MIC值为1-4 μg mL，clogP为9.14。该化合物在血浆中展示出优异的稳定性，其HC50值为131.1 μg mL，并且具有出色的膜选择性（HC50 MIC比值为65.6），能够迅速杀灭细菌。Antimicrobial agent-34的抗菌机制涉及破坏细菌的细胞膜完整性，增加细胞内活性氧的生成，以及导致蛋白质和DNA的泄漏，最终引致细菌死亡。在金黄色葡萄球菌ATCC43300引起的小鼠败血症模型中，Antimicrobial agent-34表现出显著的体内抗菌效果。

ChlaDUB1-IN-1 (Compound 8) 为针对衣原体去泛素化酶 1 (ChlaDUB1) 的抑制剂，并可应用于抗菌研究领域。

1-Amino-2,5-anhydro-1-deoxy-D-mannitol展现出对多种革兰氏阳性细菌的卓越抗菌效果，特别是对耐甲氧西林金黄色葡萄球菌（MRSA）和耐万古霉素肠球菌（VRE），显示了其潜力作为对抗抗药性细菌感染的有效方案。这一化合物在开发新型抗菌药物方面具有重要的应用前景，可能为临床上抗菌治疗提供新的策略。

Metallo-β-lactamase-IN-16 (compound 18) 作为一种含砜基团的抑制剂，针对多种金属-β-内酰胺酶展示出显著的抗菌活性。该化合物有效抑制 NDM-1（新德里金属-β-内酰胺酶-1）、IMP-1（亚胺培南酶-1）、VIM-1（维罗纳整合子编码的金属-β-内酰胺酶）及 VIM-2，其IC50值分别为 0.16 nM、0.23 nM、0.31 nM 和 1.0 nM，表现出其对这些酶的高效抑制能力。

Antibacterialagent 119 (Compound 21 g) 是一种抗耐Methicillin金黄色葡萄球菌的候选抗菌剂，其对测试菌株的MIC小于1 μg mL。该化合物能够诱导ROS产生，并作用于细菌细胞膜，使其破裂。Antibacterialagent 119 显示出强效抗菌活性、低细胞毒性、快速杀菌能力以及良好的体内抗菌效果。

Antibacterialagent 258 (Compound 11e) 是一种能破坏细菌细胞膜的抗菌剂，对多种革兰氏阳性菌有抑制作用 (对Staphylococcus aureus的MIC为1-2 μg mL)。该化合物具有低溶血活性和低细胞毒性，并在小鼠模型中显示出抗感染活性。

Biotin protein ligase-IN-1 (Compound Bio-9) 是一种生物素蛋白连接酶 (BPL) 抑制剂，Kd值为7 nM。它显示出对金黄色葡萄球菌（包括MRSA和MSSA）及结核分枝杆菌的抗菌活性，MIC值分别为0.2 μM和20 μM。

Antimicrobial-IN-1 (compound 17) 表现出对金黄色葡萄球菌 (S. aureus) 和大肠杆菌 (E. coli) 的强效抗菌活性，抑菌圈直径分别为 18 mm mg 和 16 mm mg。

IKD-8344 is a macrocyclic dilactone originally isolated from an actinomycete species and has diverse biological activities, including anticancer, antimicrobial, and anthelmintic properties.1,2,3 It is cytotoxic to L5178Y murine leukemia cells (IC50 = 0.54 ng ml).1 IKD-8344 inhibits growth of the mycelial form of C. albicans (MIC = 6.25 μg ml) and potentiates the activity of polymyxin B against the multidrug-resistant pathogenic bacterium B. cenocepacia.2,3 It is active against T. spiralis in vitro and in vivo.1 |1. Minami, Y., Yoshida, K., Azuma, R., et al. Structure of a novel macrodiolide antibiotic IKD-8344. Tetrahedron Lett. 33(48), 7373-7376 (1992).|2. Hwang, E.I., Yun, B.S., Yeo, W.H., et al. Compound IKD-8344, a selective growth inhibitor against the mycelial form of Candida albicans, isolated from Streptomyces sp. A6792. J. Microbiol. Biotechnol. 15(4), 909-912 (2005).|3. Loutet, S.A., El-Halfawy, O.M., Jassem, A.N., et al. Identification of synergists that potentiate the action of polymyxin B against Burkholderia cenocepacia. Int. J. Antimicrob. Agents 46(4), 376-380 (2015).

Diallyl tetrasulfide is an organosulfur compound that has been found in A. sativum and has diverse biological activities, including antimicrobial, antioxidant, and anticancer properties.[1],[2],[3],[4] It is active against the bacteria S. aureus and methicillin-resistant S. aureus (MRSA; MICs = 0.5 and 2 mg L, respectively), as well as the fungi C. albicans, C. krusei, C. glabrata, A. niger, A. flavus, and A. fumigatus (MICs = 0.5, 4, 2, 1, 2, and 4 mg L, respectively).[1] It reduces cadmium-induced increases in hepatic levels of thiobarbituric acid reactive substances (TBARS) and increases cadmium-induced decreases in the hepatic activity of superoxide dismutase (SOD1), catalase, GST, and glucose-6-phosphate dehydrogenase (G6PDH) in rats when administered at a dose of 40 mg kg.[2] Diallyl tetrasulfide is cytotoxic to MCF-7 breast cancer cells (IC50 = 92 μM) and reduces tumor growth in a BGC-823 mouse xenograft model when administered at doses of 20, 30, and 40 mg kg for 32 days.[3],[4]

Kigamicins are natural antitumor antibiotics that selectively kill pancreatic cancer PANC-1 cells only under nutrient-starved conditions. They also show antimicrobial activity against Gram-positive bacteria, including methicillin-resistant S. aureus. Kigamicin C inhibits PANC-1 cell survival in nutrient-deprived media at a 100-fold lower concentration than that required for cells maintained in nutrient-rich media. A related compound, kigamicin D, is active in vivo, suppressing the tumor growth of several pancreatic cancer cell lines in nude mice. It blocks the activation of Akt induced in PANC-1 cells placed in nutrient-deprived media. Kigamicin can also induce necrosis in human myeloma cells, but not normal lymphocytes, maintained in nutrient-rich media (CC50 = 100 nM).

Lactoferricin B (4-14), bovine (TFA), is a peptide derived from bovine lactoferrin, specifically consisting of residues 4-14. This compound exhibits broad-spectrum antimicrobial activity against various microorganisms[1].

Brilacidin tetrahydrochloride (PMX 30063 tetrahydrochloride) is a defensin mimetic antibiotic compound, exhibiting potent anti-infective antimicrobial activity against a range of bacteria. It demonstrates MIC90 values of 1 μg mL and 8 μg mL against the Gram-positive bacteria Streptococcus pneumoniae and Streptococcus viridans, respectively. Additionally, it has a MIC90 value of 8 μg mL for the Gram-negative bacteria Haemophilus influenzae and a MIC90 value of 4 μg mL for Pseudomonas aeruginosa.

IDR-1 is an antimicrobial peptide with activity against both Gram-positive and Gram-negative bacteria. This compound modulates innate immunity to counter infections while avoiding evident toxicities. Additionally, IDR-1 exhibits anti-inflammatory and anti-infective properties, increases the levels of monocyte chemokines, and reduces the release of pro-inflammatory cytokines.

Antimicrobial agent-3 (Compound U10) 是一种用于细菌、真菌和结核感染的抗菌剂。

FabH-IN-1 (化合物 3f) 可有效对抗革兰氏阳性菌和革兰氏阴性菌，并且也是一种良好的抗氧化剂。FabH-IN-1 是细菌FabH 酶的抑制剂，该酶是一种广谱抗菌靶标。

Antimicrobial agent-2 (compound V-a) 是对多种革兰氏阳性和革兰氏阴性菌均有抑制作用，是一种低毒、无明显耐药性、生物利用度好的广谱抗菌剂。Antimicrobial agent-2 有效破坏细胞膜，并导致蛋白渗出，诱导活性氧的产生。Antimicrobial agent-2 可有效抑制耐甲氧西林金黄色葡萄球菌 (MRSA)，MIC 为 1 μg mL。

NusB-IN-1 (Compound 22r) is a highly effective bacterial rRNA synthesis inhibitor, administered orally. It exhibits potent antimicrobial activity against MRSA and VRSA [1].

Metallo-β-lactamase-IN-5 (compound 5c) is a powerful inhibitor of metallo-β-lactamases (MBLs). Its inhibitory activity against MBLs NDM-1 and VIM-1 has been demonstrated. With an IC50 value of 45 μg mL, Metallo-β-lactamase-IN-5 effectively inhibits HUVECs. Additionally, when combined with Imipenem, Metallo-β-lactamase-IN-5 exhibits synergistic antimicrobial activity [1].

Chitin synthase inhibitor 2 (compound 2b) is a highly potent inhibitor of chitin synthase, with an IC50 value of 0.09 mM and a K i value of 0.12 mM. This compound exhibits antimicrobial activities in vitro and demonstrates synergistic or additive effects when combined with fluconazole or polyoxin B [1].

Antimicrobial Agent-1 (compound 6C) shows strong activity (MIC = 2 μg mL) against TolC mutant E. coli. Additionally, it synergistically interacts with Colistin to exhibit enhanced activity against Gram-negative bacteria. Importantly, Antimicrobial Agent-1 exhibits no cytotoxic effects on mammalian cell lines. Its MIC values on Caco-2 and Vero cell lines are greater than 128 μg mL [1].