Nimbin is a intermediate limonoid isolated from Azadirachta. Nimbin prevents tau aggregation and increases cell viability. Nimbin is effective inhibits the envelope protein of dengue virus. Nimbin has anti-inflammatory, antipyretic, antifungal, antihistamine, antiseptic, antioxidant, anti-cancer and anti-viral properties. Nimbin can across blood-brain barrier[1][2][3].
EFdA-TP is a potent nucleoside reverse transcriptase (RT) inhibitor. EFdA-TP inhibits RT-catalyzed DNA synthesis as an effective immediate or delayed chain terminator (ICT or DCT). EFdA-TP inhibits HIV-1 RT with multiple mechanisms[1].
T-705RTP is a selective and GTP-competitive influenza virus RNA polymerase inhibitor with an IC50 of 0.14 μM and a Ki of 1.52 μM. T-705RTP is the active triphosphate metabolite of T-705 and has potent anti-influenza virus activity[1][2].
HIV-1 inhibitor-43 (compound 12) is a potent HIV-1 inhibitor with an EC50 of 21.3 nM, 6.2 nM, < 0.7 nM and < 0.7 nM for Y188L, K103N-Y181C, K103N and Y181C, respectively. HIV-1 inhibitor-43 can reduce HIV-1 RNA and protein p24[1].
Alamifovir (LY582563; MCC-478), a purine nucleotide analogue prodrug, shows potent activity against wild type and lamivudine resistant hepatitis B virus (HBV). Alamifovir has high activity against HBV replication and sustained antiviral effect[1][2].
Neamine tetrahydrochloride, a degradation product of Neomycin, is a broad-spectrum aminoglycoside antibiotic. Neamine tetrahydrochloride is an anti-angiogenesis agent targeting angiogenin. Neamine tetrahydrochloride has potent antibacterial, antitumor and neuroprotective activities[1][2].
Norchelerythrine is an alkaloid isolated from the roots of Zanthoxylum capense with antibacterial activity against gram-positive and gram-negative bacteria. Norchelerythrine exhibits inhibitory activity against Staphylococcus aureus, Pseudomonas aeruginosa, and Enterococcus faecalis and Escherichia coli with MIC values >50 µg/mL[1].
Oleuropeic acid 8-O-glucoside is a terpenic compound, that can be isolated from twigs with leaves of Juniperus communis var. depressa. Oleuropeic acid 8-O-glucoside shows antibacterial activity against three strains of Helicobacter pylori (NCTC11637, NCTC11916, and OCO1), with MIC of 100 μg/mL all[1].
Decoquinate is a coccidiostat used in veterinary medicine.
Decamethoxine (Septefril) is a cationic gemini surfactant. Decamethoxine exhibits strong bactericidal and fungicidal effects. Decamethoxine modifies the permeability of the microbial cell membrane, resulting in the destruction and death of diverse microorganisms[1][2].
Neomycin sulfate is an aminoglycoside antibiotic used for preventing or treating bacterial infections.
Narasin sodium is a cationic ionophore and coccidiostat agent. Narasin inhibits NF-κB signaling and induces tumor cells apoptosis. Narasin sodium has antimicrobial and anticancer activity[1].
Octenidine is a potent antibacterial agent, possessing activity against multidrug-resistant Gram-negative pathogens. Octenidine can inhibit the expression of biofilm genes and destroy the formation of biofilms[1][3].
Methylisothiazolinone hydrochloride is the constituent of the biocide Kathon CG. Methylisothiazolinone hydrochloride is an isothiazolone derivative widely used as a preservative. Methylisothiazolinone hydrochloride is also a moderate sensitizer and reacts with GSH[1][2].
Dinitolmide is a fodder additive for poultry, used to prevent coccidiosis infections.
Dehydroglaucine is a potent antimicrobial alkaloid[1].
Tetrazolast is a HCV inhibitor with the inhibitory activity ranging from 5% to 20%, extracted from patent WO2005030774.
ddUTP (2′,3′-Dideoxyuridine-5′-triphosphate) is a selective HIV and AMV reverse transcriptase inhibitor with Ki values of 0.05 µM and 1 µM, respectively. ddUTP is incorporated into the growing DNA strand primarily at dTTP sites and inhibits further elongation[1].
Antimicrobial Compound 1 is an alkylpyridinium compound, with antimicrobial activity.
NSC309401 is an inhibitor of E. coli DHFR (IC50: 189 nM, KD: 14.57 nM)[1].
Fiacitabine(NSC 382097; FIAC; FOAC) is a selective inhibitior of DNA replication of herpes simplex virus(HSV) with IC50 values of 2.5 nM and 12.6 nM for HSV1 and HSV2, respectively. IC50 value: 2.5/12.6 nM (HSV1/2) [2]Target: HSVFIAC suppressed by 90% the replication of various strains of herpes simplex virus types 1 and 2 at concentrations of 0.0025 to 0.0126 microM. Cytotoxicity was minimal, as determined by trypan blue dye exclusion with norman Vero, WI-38, and NC-37 cell proliferation; the 50% inhibitory dose was 4 to 10 microM in a 4-day assay. FIAC was active at much lower concentrations than arabinosylcytosine, iododeoxyuridine, and arabinosyladenine. It was slightly more active against herpes simplex virus type 1 than acycloquanosine and slightly more toxic to normal cells. FIAC was about 8,000 times more active against the replication of wild-type herpes simplex virus type 1 than against a mutant strain lacking the expression of virus-specified thymidine kinase [2].
c[Arg-Arg-Arg-Arg-Dip-Dip-Dip] (Compound 8C) shows broad-spectrum activity against drug-resistant Gram-positive and Gram-negative bacteria, with MICs of 3.1, 3,1, 12.5, and 12.5 μg/mL for MRSA (ATCC BAA-1556), S. aureus (ATCC 29213), P. aeruginosa (ATCC 27883), and E. coli (ATCC 25922), respectively[1].
MRV03-037 is a selective colibactin-activated peptidase (ClbP) inhibitor that blocks the genotoxic effect of Colibactin (HY-145930) on eukaryotic cells. MRV03-037 prevents gut bacterial genotoxin production[1].
UK-2A (Antibiotic UK 2A) is a potent antifungal antibiotic. UK-2A shows antifungal activity[1][2].
ML267 a potent Sfp phosphopantetheinyl transferase (PPTases) inhibitor with an IC50 of 0.29 μM. ML267 also inhibits AcpS-PPTase with an IC50 of 8.1 μM. ML267 possesses specific Gram-positive-targeted bactericidal activities[1].
Miltefosine is a broad spectrum antimicrobial, anti-leishmanial, phospholipid agent acting by inhibiting the PI3K/Akt activity.
TBA-354 is a potent anti-tuberculosis compound; maintains activity against Mycobacterium tuberculosis H37Rv isogenic monoresistant strains and clinical drug-sensitive and drug-resistant isolates.IC50 value:Target: Anti-tuberculosis agentin vitro: TBA-354 is narrow spectrum and bactericidal in vitro against replicating and nonreplicating Mycobacterium tuberculosis, with potency similar to that of delamanid and greater than that of PA-824. TBA-354 maintains activity against Mycobacterium tuberculosis H37Rv isogenic monoresistant strains and clinical drug-sensitive and drug-resistant isolates [1]. TBA-354 is 5 to 10 times more potent than PA-824, but selected mutants are cross-resistant to PA-824 and delamanid. TBA-354 is 2 to 4 times more potent than PA-824 when combined with bedaquiline, and when administered at a dose equivalent to that of PA-824, TBA-354 demonstrated superior sterilizing efficacy [2].in vivo: TBA-354 has high bioavailability and a long elimination half-life. In vitro studies suggest a low risk of drug-drug interactions. Low-dose aerosol infection models of acute and chronic murine tuberculosis reveal time- and dose-dependent in vivo bactericidal activity that is at least as potent as that of delamanid and more potent than that of PA-824.
Hygromycin B is an aminoglycoside antibiotic active against prokaryotic and eukaryotic cells.
4aα,7α,7aα-Nepetalactone exhibits antibacterial activity, and inhibits Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, Salmonella typhi and Enterococcus faecalis.
Rhuscholide A is a benzofuran lactone that shows significant anti-HIV-1 activity, with an EC50 of 1.62 μM[1].