HCV-IN-29 is a hepatitis C virus (HCV) inhibitor exacted from patent US8329159B2, compound 1e[1].
NSC 108602 is a nucleoside HIV-1 reverse transcriptase inhibitor.
N-Hexanoyl-DL-homoserine lactone is a bacterial quorum sensing molecule produced in the rhizosphere. N-Hexanoyl-DL-homoserine lactone, a bacterial quorum sensing signal, induces transcriptional changes in Arabidopsis and may contribute to tuning plant growth to the microbial composition of the rhizosphere[1].
Sulfapyridine(Dagenan) is a sulfonamide antibacterial.Target: AntibacterialSulfapyridine(Dagenan) is a sulfonamide antibacterial. Sulfapyridine is not prescribed for the treatment in humans any more. However, it may be used to treat Linear IgA Disease. It is a good antibacterial drug, but its water solubility is very dependent on PH. Thus, there is a risk of crystallization within the bladder or urethra, which could lead to pain or blockage. The drug sulfasalazine is structurally one molecule of mesalamine linked to one molecule of Sulfapyridine with an azo bond [1].
PC-766B is a macrolide antibiotic. PC-766B is active against Gram-positive bacteria, and some fungi and yeasts, but inactive against Gram-negative bacteria. PC-766B shows antitumor activity against murine tumor cells. PC-766B has weak inhibitory activity against Na+, K+-ATPase[1][2].
3-Azaspiro[5.5]undecane (4,4-Pentamethylenepiperidine) hydrochloride is an inhibitor targeting the WT influenza A virus M2 (A/M2), with an IC50 of 1 μM[1].
Garenoxacin (BMS 284756) mesylate is an orally active quinolone antibiotic and Garenoxacin mesylate has a broad spectrum of activity against a wide array of gram-positive and gram-negative bacteria, anaerobes. Garenoxacin mesylate also inhibits Gyrase and TOPO IV[1][2][3][4].
HIV-1 integrase inhibitor 9 (compound 8a) is a potent HIV-1 RNase H inhibitor with an IC50 of 12.3 μM. HIV-1 integrase inhibitor 9 shows an antiviral activity[1].
Cenicriviroc is an orally active, dual CCR2/CCR5 antagonist, also inhibits both HIV-1 and HIV-2, and displays potent anti-inflammatory and antiinfective activity.
Isorhapontin is an antifungal agent. Isorhapontin inhibits the hydrolytic activity of Trichoderma cellobiohydrolase I (CBH I) with a Ki of 57.2 μM. Isorhapontin also inhibits the activity of Trichoderma endoglucanase I[1][2].
A small-molecule inhibitor of the interaction of the C. glabrata Pdr1 activation domain with the C. glabrata Gal11A KIX domain with Ki of 18 uM; blocks Gal11/Med15 recruitment and inhibits Pdr1-dependent gene activation and re-sensitizes drug-resistant C. glabrata to azole antifungals in vitro and in animal models for disseminated and urinary tract C. glabrata infection; a novel therapeutic strategy in fungal infectious disease.
5-Fluorouracil-13C,15N2 is the 13C and 15N labeled 5-Fluorouracil[1]. 5-Fluorouracil (5-FU) is an analogue of uracil and a potent antitumor agent. 5-Fluorouracil affects pyrimidine synthesis by inhibiting thymidylate synthetase thus depleting intracellular dTTP pools. 5-Fluorouracil induces apoptosis and can be used as a chemical sensitizer[2][3]. 5-Fluorouracil also inhibits HIV[4].
SARS-CoV-2 Mpro-IN-12 (compound D026) is a SARS-CoV-2 main protease (Mpro) inhibitor with antiviral activities[1].
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].
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].
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].
BPH-715 is a bisphosphonate, inhibits Plasmodium liver-stage growth, with an IC50 of 10 μM for Plasmodium exoerythrocytic forms in HepG2 cells[1].
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.
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].
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].
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]
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].
Aztreonam is a synthetic monocyclic beta-lactam antibiotic, which has a very high affinity for penicillin-binding protein 3 (PBP-3).Target: Penicillin-binding proteins 3 (PBP-3)Aztreonam is a synthetic monocyclic beta-lactam antibiotic (a monobactam), with the nucleus based on a simpler monobactam isolated from Chromobacterium violaceum. It was approved by the U.S. Food and Drug Administration in 1986. It is resistant to some beta-lactamases, but is inactivated by extended-spectrum beta-lactamases. Aztreonam has no useful activity against gram-positive or anaerobic microorganisms Aztreonam is similar in action to penicillin. It inhibits mucopeptide synthesis in the bacterial cell wall, thereby blocking peptidoglycan crosslinking. It has a very high affinity for penicillin-binding protein 3 (PBP-3) and mild affinity for PBP-1a. Aztreonam binds the penicillin-binding proteins of gram-positive and anaerobic bacteria very poorly and is largely ineffective against them. Aztreonam is bactericidal but less so than some of the cephalosporins
Thiamphenicol glycinate hydrochloride is a broad-spectrum antibacterial agent that can be used for respiratory tract infections research[1].