Hetacillin potassium is a broad-spectrum treatment for use against a wide range of common Gram-positive and Gram-negative bacteria.
Pristimerin is a potent and reversible monoacylglycerol lipase (MGL) inhibitor with an IC50 of 93 nM.
Amphotericin B methyl ester hydrochloride is the methyl ester derivative of the polyene antibiotic Amphotericin B (A634250). Amphotericin B methyl ester hydrochloride is the cholesterol-binding compound possesses significant antifungal activity. Amphotericin B methyl ester hydrochloride disrupts HIV-1 particle production and potently inhibits HIV-1 replication[1][2].
Aurein 5.2 is an antibiotic antimicrobial peptide[1].
Parasin I is a 19-amino acid histone H2A-derived peptide isolated from the skin of the catfish, and shows antimicrobial activity.
Zalcitabine is a potent nucleoside analogue reverse transcriptase inhibitor used in the treatment of HIV infection.
Polymyxin B1 is a potent antimicrobial lipopeptide first derived from Bacilus polymyxa. Polymyxin B1 is the major component in Polymyxin B (HY-A0248). Polymyxin B1 can induce lysis of bacterial cells through interaction with their membranes. Polymyxin B1 has the potential for multidrug-resistant Gram-negative bacterial infections treatment[1][2].
Urechistachykinin II (Uru-TK II), an invertebrate tachykinin-related peptides (TRPs) isolated from echiuroid worms, shows antimicrobial activities without a hemolytic effect[1][2].
Pyraclostrobin is a strobilurin fungicide that inhibits mitochondrial complex III of fungal and mammalian cells. Pyraclostrobin induces triglyceride accumulation and triglyceride accumulation in 3T3-L1 cells.
Sulfamonomethoxine sodium is a long acting sulfonamide?antibacterial?agent, used in blood kinetic studies,and blocks the synthesis of folic acid by inhibiting synthetase of dihydropteroate[1].
Metronidazole Benzoate, derives from a metronidazole and a benzoic acid, has a role as an antibacterial, antimicrobial, antiparasitic, and antitrichomonal agent[1].
Matairesinoside is a lignan with antibacterial and antioxidant activities. Matairesinoside also shows virus-cell fusion inhibitory activity[1][2].
BPH-715 is a bisphosphonate, inhibits Plasmodium liver-stage growth, with an IC50 of 10 μM for Plasmodium exoerythrocytic forms in HepG2 cells[1].
Midecamycin, an acetoxy-substituted macrolide antibiotic, is tested against gram-positive and gram-negative bacteria.
Tiamulin (Thiamutilin) is a diterpenic veterinary drug widely used in swine for the control of infectious diseases, including swine dysentery and enzootic pneumonia[1][2][3].
9-Oxonerolidol is a farnesane-type sesquiterpenoid with anti-pathogens activity. 9-Oxonerolidol can be isolated from Chiliadenus lopadusanus. 9-Oxonerolidol acts as a post-infectional inhibitor from plants, and inhibits Gram+ and Gram? bacteria resistant to the antibiotic[1][2].
Antifungal agent 20 exhibits remarkable antifungal activity against Colletotrichum gloeosprioides, Rhizoctonia solani, Phytophthora nicotianae var. nicotianae, Diplodia pinea, Colletotrichum acutatum, and Fusarium oxysporum f. sp. niveum.
Nonanoic acid-d17 is the deuterium labeled Nonanoic acid. Nonanoic acid is a naturally-occurring saturated fatty acid with nine carbon atoms. Nonanoic acid significantly reduces bacterial translocation, enhances antibacterial activity, and remarkably increases the secretion of porcine β-defensins 1 (pBD-1) and pBD-2[1].
KW-8232, an orally active anti-osteoporotic agent, and can reduces the biosynthesis of PGE2[1].
XT-2 peptide is an antimicrobial peptide derived from skin secretions of Xenopus tropicalis. XT-2 peptide has strong activity against E.coli, the vaule of MIC is 8 μM[1].
Swietemahalactone is a natural compound isolated from Swietenia mahagoni. Swietemahalactone exhibits antibacterial activity aganist E. coli[1].
Bicyclomycin benzoate is an antibiotic exhibiting activity against a broad spectrum of Gram-negative bacteria and against the Gram-positive bacterium.
Praziquantel D11 is the deuterium labeled Praziquantel, which is an anthelmintic.
Norethindrone is a female progestin approved by FDA for the treatment of endometriosis, uterine bleeding caused by abnormal hormone levels, and secondary amenorrhea.
Cephaeline hydrochloride ((-)-Cephaeline hydrochloride) is a phenolic alkaloid in Indian Ipecac roots. Cephaeline hydrochloride exhibits potent inhibition of both Zika virus (ZIKV) and Ebola virus (EBOV) infections[1][2].
3,4,5-Trimethoxybenzaldehyde is an intermediate for the synthesis of various pharmaceuticals, especially for trimethoprim used to treat bacterial infections, including urinary tract pathogens infection[1].
Oleanolic acid is a triterpenoid, inhibits infection by HIV-1 in in vitro infected PBMC, naturally infected PBMC and monocyte/macrophages with EC50 of 22.7 mM, 24.6 mM and 57.4 mM, respectively. Besides,it has IC50 of 17μM for the production of leukotriene B4 from rat peritoneal leukocytes.IC50:17μM(The production of leukotriene B4 from rat peritoneal leukocytes)[1]IC50:22.7 mM, 24.6 mM and 57.4 mM(in vitro infected PBMC, naturally infected PBMC and monocyte/macrophages by HIV-1, respectively.[2]In vitro: The highest of the four tested doses (100 μM), showed only a slight inhibition approximately, 30%. In contrast, the more powerful effect of oleanonic acid in this system, suggests that it acts through a mechanism related to the inhibition of 5-lipoxygenase, either directly or interfering with some of the mechanisms that participate in the complex activation of this enzyme. Oleanonic acid also acts by reducing prostaglandin synthesis.[1]Oleanolic acid inhibits the HIV-1 replication in all the cellular systems used (EC50 values: 22.7 microM, 24.6 microM and 57.4 microM for in vitro infected PBMC, naturally infected PBMC and M/M, respectively). As regards the mechanism of action, oleanolic acid inhibits in vitro the HIV-1 protease activity.[2]In vivo: Oleanonic acid exerted no activity on the oedema induced by application of ethyl phenylpropiolate after a pre-treatment of 16 h. In the TPA ear oedema test, it showed a non-significant 28% inhibition. However, when assayed on the ear oedema induced by DPP, oleanonic acid reduced the swelling by 40%, an effect similar to that of the standard carbamazepine. In the mouse model of delayed hypersensitivity induced by dinitrofluorobenzene, oleanonic acid was ineffective at both 24 and 96 h, while oleanolic acid reduced non-significantly the oedema at 96 h by 32%.In the TPA model of chronic inflammation induced by multiple applications, oleanonic acid showed a significant effect, with 45% inhibition. In contrast, oleanolic acid was inactive. Both inhibited the neutrophil infiltration measured as myeloperoxidase activity by 84% and 67%, respectively. The inhibition observed for dexamethasone on the swelling and myeloperoxidase activity was around 90%. The histological study of ears treated only with repeated doses of TPA showed an extensive diffusive inflammatory lesion with microabscesses affecting dermis and epidermis. The main infiltrating cells in the skin were neutrophils and epithelial thickness was 6.6±1.0 cells. In the tissues treated only with the solvent acetone, epithelial thickness was 2.1±0.5 and no signs of lesion or leukocyte infiltration were detectable. The multidose treatment with oleanonic acid reduced both the intensity and extension of the damage produced by TPA, as this was localized in the dermis, where the main infiltrating cells were lymphocytes, and where fibrosis was observed. In this case, epithelium thickness was 4.4±0.7 cells. The ears treated with dexamethasone showed minimal inflammatory lesions and sometimes none at all, and the epithelium thickness was 4.3±0.7 cells.The paw oedema induced by bradykinin was significantly reduced (61%) by oleanonic acid, whereas isoprenaline had a slightly lower effect (52%). Both oleanolic and oleanonic acid also reduced the paw oedema induced by phospholipase A2; the latter showing its strongest effect at 60 min, with an 84% inhibition, and maintaining activity at 90 min. Oleanolic acid also had its maximum effect at 60 min, vanishing at 90 min, while the activity of cyproheptadine was uniform along the experiment, ranging 80–90% inhibition .[1]
Antibacterial agent 33, an antibacterial agent, significantly lowers MIC value of antibacterial agent Ceftazidime[1].
Isookanin, isolated from the leaves of Clinacanthus nutans, can be used for the research of various illnesses including cancers, skin rashes, snake and insects bites, diabetes mellitus, diarrhoea, as an anti-viral agent against HSV and varicella-zoster virus (VZV)[1].
Dihydropteroate synthase-IN-1 (compound 5g) is a potent dihydropteroate synthase (DHPS) inhibitor. Dihydropteroate synthase-IN-1 shows antimicrobial activities and antifungal activity. Dihydropteroate synthase-IN-1 inhibits cytochromes P450. Dihydropteroate synthase-IN-1 can bu used as diagnostic radio imaging material[1].