Acivicin hydrochloride (AT-125 hydrochloride), a natural product produced by Streptomyces sviceus, is a γ−glutamyl transpeptidase (GGT) inhibitor. Acivicin hydrochloride can across the blood-brain barrier and has anti-cancer, anti-parasitic properties[1][2].
Platencin is a natural, broad spectrum Gram-positive antibiotic isolated from S. platensis. Platencin inhibits β-ketoacyl-ACP synthases II and III (FabF and FabH, respectively) with IC50s of 1.95 and 3.91 μg/ml, respectively[1].
(S)-Dinotefuran ((S)-MTI-446), a neonicotinoid pesticide, is toxic by binding to α8 subunit of nAChR of honeybee Apis mellifera (Apis mellifera Linnaeus). (S)-Dinotefuran shows more toxic than R-dinotefuran to honeybee Apis mellifera[1].
Imipenem (N-Formimidoyl thienamycin, MK0787), a stable crystalline derivative of thienamycin, is an antibiotic and has the excellent activity against a broad range of gram-positive and gram-negative aerobic and anaerobic bacteria. Imipenem (N-Formimidoyl thienamycin, MK0787) can be used for carbapenem-nonsusceptible and P. aeruginosa biofilm infections [1][2][3].
Staphyloferrin A is a siderophore protein that can be combined with antibiotics to study drug-resistant bacteria that cause skin diseases[1].
Ascamycin is a 5'-O-sulfonamide ribonucleoside antibiotic produced by Streptomyces sp. JCM9888. Ascamycin has a selective antibacterial activity against Xanthomonas species with MIC values of 0.4 μg/mL, 12.5 μg/mL and 12.5 μg/mL for Xanthomonas citri, Xanthomonas oryzae and Mycobacterium phlei, respectively[1][2][3].
Isochondrodendrine ( Isochondrodendrin) is a class of bisbenzylisoquinoline alkaloid isolated from Isolona ghesquiereina. Isochondodendrine has strong antiplasmodial activity against Plasmodium falciparum[1].
β-Hederin, a saponin isolated from Hedera helix L.(Araliaceae), possesses antileishmanial activity. β-Hederin exhibits IC50 values of 1.5 μM, 68 nM and 4.57 μM in L. Mexicana promastigotes, L. mexicana amastigotes and THP1 cells, respectively[1][2].
Corilagin, a gallotannin, is isolated from Caesalpinia coriaria (Jacq.) Willd. Corilagin inhibits activity of reverse transcriptase of RNA tumor viruses. Corilagin inhibits the growth of Staphylococcus aureus with a MIC of 25 μg/mL. Corilagin shows good anti-tumor activity on hepatocellular carcinoma and ovarian cancer. Corilagin shows a low level of toxicity toward normal cells and tissues[1].
Tegobuvir is a specific, covalent inhibitor of the HCV NS5B polymerase.
Sambutoxin is a mycotoxin. Sambutoxin can be isolated from wheat culture of Fusarium sambucinum[1].
DL-3-Phenyllactic acid is a broad-spectrum antimicrobial compound.
Sitafloxacin (DU6859a) hydrochloride is a potent, orally active fluoroquinolone antibiotic. Sitafloxacin hydrochloride shows antichlamydial activity and antibacterial activities against a broad range of gram-positive and gram-negative bacteria, including anaerobic bacteria, as well as against atypical pathogens. Sitafloxacin hydrochloride can be used for the research of respiratory tract infection and urinary tract infection[1][2].
Antibacterial agent 122 (compound 15) is a thiourea derivative with anti-mycobacterial activity and low cytotoxicity. Antibacterial agent 122 can be used for tuberculosis-related studies[1].
AB-423 is an inhibitor of HBV capsid assembly, and potent inhibits HBV replication with EC50/EC90 of 0.08-0.27 μM/0.33-1.32 μM in cells.
Pneumocandin B0(L-688786), a key intermediate in the synthesis of the antifungal agent, Cancidas, has led to the identification of several materials with potential for improved performance.
STING agonist-27 (CF509) is a non-nucleotide small-molecule STING agonist. STING agonist-23 activates STING, exhibits activity against SARS-CoV series strains[1].
Yatein is a lignan isolated from A. chilensis, with antiproliferative activity[1]. Yatein suppresses herpes simplex virus type 1 (HSV-1 ) replication by interruption the immediate-early gene expression[2].
B220 is an antiviral agent which can inhibit the growth of HSV-1, HSV-2 and human cytomegalovirus (CMV).
Pyrithione is a compound with antibacterial and antifungal activity[1].
Amprenavir (Agenerase) is a HIV protease inhibitor(Ki=0.6 nM) used to treat HIV infection.IC50 Value: 0.6 nM (Ki); Against wild-type clinical HIV isolates:14.6 +/- 12.5 ng/mL (mean +/- SD) [1].Target: HIV proteasein vitro: Amprenavir has an enzyme inhibition constant (Ki = 0.6 nM) that falls within the Ki range of the other protease inhibitors. Amprenavir's in vitro 50% inhibitory concentration (IC50) against wild-type clinical HIV isolates is 14.6 +/- 12.5 ng/mL (mean +/- SD) [1]. Amprenavir had direct inhibitory effects on invasion of Huh-7 hepatocarcinoma cell lines, inhibiting MMP proteolytic activation [2].in vivo: Amprenavir was able to promote regression of hepatocarcinoma growth in vivo by anti-angiogenetic and overall anti-tumor activities, independently by PI3K/AKT related pathways that at today is one of the more suggestive hypothesis to explain the anti-tumor effects of the different protease inhibitors [2]. Amprenavir efficiently activated PXR and induced PXR target gene expression in vitro and in vivo. Short-term exposure to amprenavirsignificantly increased plasma total cholesterol and atherogenic low-density lipoprotein cholesterol levels in wild-type mice, but not in PXR-deficient mice [3]. Amprenavir has been approved for adults and children; the recommended capsule doses are 1200 mg twice daily for adults and 20 mg/kg twice daily or 15 mg/kg 3 times daily for children < 13 years of age or adolescents < 50 kg [1].Clinical trial: A Study to Compare Three Doses of T-20 When Given in Combination With Abacavir, Amprenavir, Ritonavir, and Efavirenz to HIV-Infected Adults. Phase 2
APX2039 is an orally active and potent inhibitor of the fungal Gwt1 enzyme. APX2039 has extremely potent anticryptococcal activity against C. neoformans and C. gattii. APX2039 blocks the localization of GPI (glycosylphosphatidyl inositol)-anchored cell wall mannoproteins. APX2039 can be used for Cryptococcal meningitis (CM) research[1][2].
Elsulfavirine is a reverse transcriptase inhibitors for HIV-1 infection and is a new anti-HIV drug[1].
Cipargamin (NITD609) is an potent antimalarial compound, with IC50 of appr 1 nM against P. falciparum.
Ibuprofen ((±)-Ibuprofen) L-lysine is a potent orally active, selective COX-1 inhibitor with an IC50 value of 13 μM. Ibuprofen L-lysine inhibits cell proliferation, angiogenesis, and induces cell apoptosis. Ibuprofen L-lysine is a nonsteroidal anti-inflammatory agent and a nitric oxide (NO) donor. Ibuprofen L-lysine can be used in the research of pain, swelling, inflammation, infection, immunology, cancers[1][2][3][4][5][6][7][8].
4'-Hydroxy-3'-methylacetophenone, a phenolic volatile compound, is isolated from Hawaiian green coffee beans (Coffea Arabica L.). 4'-Hydroxy-3'-methylacetophenone has potent antioxidant activities. 4'-Hydroxy-3'-methylacetophenone also can be used to synthesize heterocyclic compounds which have antimycobacterial activity[1][2].
Spirolaxine is a plant growth inhibitor and possess significant anti-Helicobacter pylori activity. Spirolaxine exhibits cholesterol-lowering activity[1].
Spectinomycin Dihydrochloride is a new parenteral antibiotic prepared from Streptomyces spectabilis.Target: AntibacterialSpectinomycin is an antibiotic produced by Streptomyces spectabilis. It is active against gram-negative bacteria and used for the treatment of gonorrhea. Spectinomycin binds to the 30S subunit of the bacterial ribosome and interrupts protein synthesis. One form of resistance has emerged in the 16S ribosomal RNA in Pasteurella multocida [1]. It is given by injection to treat gonorrhea, especially in patients who are allergic to penicillins. A resistance-conferring gene for spectinomycin can also be used as a selection marker in bacteria for molecular cloning purposes. Furthermore, Spectinomycin is used as a selection agent for transformed plant cells that contain the selectable marker gene Spcr [2].
KIN1408 is an antiviral small molecule compound, as agonists of the RLR pathway.Target: KIN1408 activate IRF3 through MAVS, thereby inhibiting infection by viruses of the families Flaviviridae (West Nile virus, dengue virus and hepatitis C virus), Filoviridae (Ebola virus), Orthomyxoviridae (influenza A virus), Arenaviridae (Lassa virus) and Paramyxoviridae (respiratory syncytial virus, Nipah virus) .
AZD-7295 is a HCV NS5A protein inhibitor, with an EC50 of 7 nM for GT-1b replicon[1][2].