116-9e (MAL2-11B) is a Hsp70 co-chaperone DNAJA1 inhibitor. 116-9e inhibits Simian Virus 40 (SV40) replication and DNA synthesis. 116-9e inhibits tumor antigen (TAg)’s endogenous ATPase activity and the TAg-mediated activation of Hsp70[1][2].
Ethambutol is a bacteriostatic antimycobacterial agent, which obstructs the formation of cell wall by inhibiting arabinosyl transferases.Target: AntibacterialEthambutol directly affects two polymers, arabinogalactan (AG) and lipoarabinomannan (LAM) in Mycobacterium smegmatis. In M. smegmatis, Ethambutol inhibits synthesis of arabinan completely and inhibits AG synthesis most likely as a consequence of this; more than 50% of the cell arabinan is released from the bacteria following Ethambutol treatment, whereas no galactan is released. Ethambutol main targets against embB gene product in M. avium. Ethambutol induces 60% changes in the embB gene in M. tuberculosis resistant mutants [1]. Ethambutol is effective against actively growing microorganisms of the genus Mycobacterium, including M. tuberculosis. Nearly all strains of M. tuberculosis and M. kansasii as well as a number of strains of the M. aviumcomplex (MAC) are sensitive to Ethambutol. [1] Ethambutol is potency against M. tuberculosis (H37Rv) with MIC of 0.5 μg/mL in vitro [2]. Ethambutol is efficient on treatment of mycobacterial-infected macrophages. When M. tuberculosis infected macrophages are treated with 6 μg/mL Ethambutol, the log CFUs following treatment for 3 days is 4.17, while value in control group is 4.8. The MICs for M. avium (MTCC 1723) and M. smegmatis (MTCC 6) are 15 μg/mL and 0.18 μg/mL, respectively. Ethambutol is efficient in animal model. 100 mg/kg Ethambutol given orally 15 days post i.v. infection 1 ×/week for 5 weeks, induces a lower log CFU compared with untreatment (4.59 vs 5.07) [3].
VEC-5 is a HIV-1 inhibitor. VEC5 have been evaluated for their inhibitory potential employing ligand receptor and protein-protein interactions studies. VEC-5 exhibited better interaction with Vif than RN18.
Faltan-d4 is the deuterium labeled Faltan[1]. Faltan is a dicarboximide fungicide, widely used on vines and several vegetable crops, and is also cytotoxic effect on human bronchial epithelial cells[2].
Bulaquine (CDRI 80/53) is a potent antimalarial agent which is an analogue of Primaquine (HY-12651A). Bulaquine affects multiple metabolism pathways and shows inhibition effect on Plasmodium cynomolgi infection. Bulaquine can be used for the research of malaria[1][2][3].
Policresulen is a potent inhibitor of DENV2 NS2B/NS3 protease (IC50 of 0.48 μg/mL). Policresulen inhibits DENV2 replication in BHK-21 cells with IC50 of 4.99 μg/mL. Policresulen acts as a competitive inhibitor of the protease, and slightly affects the protease stability[1].
Polymyxin B nonapeptide TFA is a cyclic peptide obtained from Polymyxin B by proteolytic removal of its terminal amino acyl residue[1]. Polymyxin B nonapeptide TFA is less toxic, lacks bactericidal activity, and retains its ability to render gram-negative bacteria susceptible to several antibiotics by permeabilizing their outer membranes[2].
Bio-AMS is a chemical inhibitor of Mycobacterium tuberculosis biotin protein ligase ( MtBPL) with Kd of 0.865 nM; possesses selective activity against Mycobacterium tuberculosis ( Mtb) and arrests fatty acid and lipid biosynthesis, enhances tuberculosis chemotherapy (rifampicin and ethambutol).
HCV-IN-35 (Compound (R)-3h) is a potent inhibitor of HCV. HCV-IN-35 has the potential for the research infection diseases[1].
1-Tetradecanol, isolated from Myristica fragrans, is a straight-chain saturated fatty alcohol. 1-Tetradecanol possesses antibacterial and anti-inflammatory (periodontitis) activity[1].
Isoscopoletin (6-Hydroxy-7-methoxycoumarin) is an active constituent in Artemisia argyi leaves. Isoscopoletin shows substantial inhibition against cell proliferation, with IC50s of 4.0 μM and 1.6 μM for human CCRF-CEM leukaemia cells and multidrug resistant subline CEM/ADR5000, respectively[1]. Isoscopoletin (6-Hydroxy-7-methoxycoumarin) possesses inhibitory activity against HBV replication[2].
Lufenuron is a lipophilic benzoylurea insecticide and a chitin synthesis inhibitor that can used for flea and fish lice control. Lufenuron inhibits moulting of arthropods[1][2].
BVDU 5′-Triphosphate is an antivirus agent with 5′-Triphosphate label, targeting viral DNA polymerase. BVDU 5′-Triphosphate shows excellent selectivity against varicella-zoster virus (VZV) and herpes simplex virus type 1 (HSV-1), due to a specific phosphorylation by the virus-encoded thymidine kinase.
D-Ribonolactone is sugar lactone and an inhibitor of β-galactosidase of Escherichia coli with a Ki of 26 mM[1].
(+)-Thienamycin is a potent broad-spectrum antibacterial and β-lactamase inhibitor that can be from Streptomyces cattleya[1].
AN-12-H5 is a bifunctional, enviroxime-like anti-Enterovirus compound that inhibits replication and the early stage of enterovirus 71 infection with EC50 of 0.55 uM; mutations in capsid proteins (G3112A, VP1-Ala224Thr, and G2396A, VP3-Arg227Lys mutations) are resistant to AN-12-H5.
Thymol is the main monoterpene phenol occurring in essential oils isolated from plants belonging to the Lamiaceae family, and other plants such as those belonging to the Verbenaceae, Scrophulariaceae, Ranunculaceae and Apiaceae families. Thymol has antioxidant, anti-inflammatory, antibacterial and antifungal effects[1].
Diacetazotol inhibits dioxin-induced ethoxyresorufin-O-deethylase (EROD) activity with IC50 of 75±4 nM. Diacetazotol extracts from patent US20070032458, compound 3.
Dichlorophen is an anticestodal agent.
M2 ion channel blocker is capable of inhibiting and blocking the activity of M2 ion channel;Antiviral agent.
Acyclovir monophosphate is a potent anti-herpes simplex virus (HSV) agent. Acyclovir monophosphate blocks DNA synthesis through the inhibition of the viral DNA polymerase and terminates the chain elongation of the viral DNA. Acyclovir monophosphate shows antitumor activity[1][2].
Saquinavir(Ro 31-8959) is an HIV Protease inhibitor used in antiretroviral therapy. IC50 Value: Target: HIV ProteaseSaquinavir is a protease inhibitor. Proteases are enzymes that cleave protein molecules into smaller fragments. HIV protease is vital for both viral replication within the cell and release of mature viral particles from an infected cell. Saquinavir binds to the active site of the viral protease and prevents cleavage of viral polyproteins, preventing maturation of the virus. Saquinavir inhibits both HIV-1 and HIV-2 proteases.Studies have also looked at Saquinavir as a possible anti-cancer agent.
HBV-IN-39-d3 (Example 14) is a deuterated HBV-IN-39 (Example 13). HBV-IN-39 is an HBV inhibitor. HBV-IN-39-d3 has better oral bioavailability than HBV-IN-39[1].
INSCoV-614(1B) is a potent inhibitor of Mpro (3CLpro). Proteases (PL pro and 3CL pro) are involved with transcription and replication of the virus. INSCoV-614(1B) has the potential for the research of SARS-CoV-2 infection (extracted from patent WO2021219089A1)[1].
Pseudolaric Acid A is a diterpene acid isolated from Pseudolarix kaempferi, has antifungal, cytotoxic and antifertile activities[1][2][3].
AL-470 is a potent antiviral agent with EC50 values of 0.27, 0.63, and 0.35 µM against HIV-1, HIV-2, and EV-A71, respectively[1].
4-Aminosalicylic acid (ASA) is an orally active antibiotic and has the potential to treat tuberculosis[1].
2-Chloroacetamide is a preservative and is a herbicide for both uplands and paddy fields. 2-Chloroacetamide is a biocide in agriculture, glues, paints and coatings. 2-Chloroacetamide inhibits very-long-chain fatty acid elongase[1][2][3].
Fenpropidin is a sterol biosynthesis inhibitor fungicide[1].
Flucycloxuron (Andalin) is an insect growth regulator (IGR)[1].