LP11 is a fatty acid-conjugated lipopeptide. LP11 is a potent inhibitor of HIV. LP11 has highly enhanced α-helicity and thermalstability[1].
Ascaridole is an anthelmintic and also has antimalarial activity[1].
DHODH-IN-5 is a potent human dihydroorotate dehydrogenase (DHODH) inhibitor, with a pIC50 of 7.8 for human recombinant DHODH. DHODH-IN-5 inhibits measles virus replication, with a pMIC50 of 8.8[1].
Linezolid D3 is a deuterium labeled Linezolid (PNU-100766). Linezolid is a synthetic antibiotic that acts by inhibiting the initiation of bacterial protein synthesis[1].
3-Pentanol-d5 is the deuterium labeled 3-Pentanol[1]. 3-Pentanol is an active organic compound produced by plants and is a component of emitted insect sex pheromones. 3-pentanol elicits plant immunity against microbial pathogens and an insect pest in crop plants[2].
Ranitidine bismuth citrate is an orally active Histamine H2-receptor antagonist with an IC50 of 3.3 μM. Ranitidine bismuth citrate has high selectivity for SARS-CoV-2-infected cells. Ranitidine bismuth citrate is a commonly used agent anti-Helicobacter pylori infection with an MIC90 value of 16 ng/L[1][2][3].
Ethambutol Dihydrochloride 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].
4-Hydroxycoumarin, a coumarin derivative, is one of the most versatile heterocyclic scaffolds and is frequently applied in the synthesis of various organic compounds. 4-Hydroxycoumarin possesses both electrophilic and nucleophilic properties. 4-Hydroxycoumarin derivatives are employed as the anticoagulant, antibacterial, antifungal, antiviral, antitumor, antiprotozoal, insecticidal, antimycobacterial, antimutagenic, antioxidant, anti-inflammatory agents, HIV protease inhibitors and tyrosine kinase inhibitors[1].
Trovirdine inhibits HIV-1 RT with an IC50 of 7 nM when employing heteropolymeric primer/template (oligo-DNA/ribosomal RNA)and dGTP as substrate.IC50 value: 7 nMTarget: HIV-1Trovirdine is currently in phase I clinical trials for potential use in thetreatment of AIDS.
(6E,12E)-Tetradecadiene-8,10-diyne-1,3-diol is an antibacterial compound. (6E,12E)-Tetradecadiene-8,10-diyne-1,3-diol can be isolated from the roots of Atractylodes japonica. (6E,12E)-Tetradecadiene-8,10-diyne-1,3-diol has anti-methicillin-resistant Staphylococcus aureus (MRSA) activity with MIC values of 4-32 μg/mL. (6E,12E)-Tetradecadiene-8,10-diyne-1,3-diol can be used for the research of bacterial infection[1].
Polyketide synthase 13-IN-2 (comp 42) is a polyketide synthase 13 inhibitor against Mycobacterium tuberculosis, with an MIC of 0.25 μg/mL[1].
HIV-1 inhibitor-54 is a potent HIV-1 inhibitor. HIV-1 inhibitor-54 has anti-HIV activity in MT-4 cells against WT HIV-1 (strain IIIB) with an EC50 value of 0.032 μM. HIV-1 inhibitor-54 can be used for the research of virus infection[1].
Dermaseptin-S1 is an antimicrobial peptide derived from frog skin against filamentous fungi[1].
Caracemide (NSC-253272) is a novel anticancer agent derived from a hydroxamic acid. Caracemide inactivates R1 by covalent modification at the substrate-binding site and inhibits the enzyme ribonucleotide reductase of Escherichia coli. Caracemide has demonstrated to produce severe central nervous system (CNS) toxicity. Caracemide has a toxic metabolite, methylisocyanate (MIC), in vivo[1][2].
Ledipasvir is an inhibitor of the hepatitis C virus NS5A, with EC50s of 34 pM and 4 pM against genotype 1a and 1b replicon, respectively.
Enfuvirtide is an anti-HIV-1 fusion inhibitor peptide. Sequence: Ac-Tyr-Thr-Ser-Leu-Ile-His-Ser-Leu-Ile-Glu-Glu-Ser-Gln-Asn-Gln-Gln-Glu-Lys-Asn-Glu-Gln-Glu-Leu-Leu-Glu-Leu-Asp-Lys-Trp-Ala-Ser-Leu-Trp-Asn-Trp-Phe-NH2.
Sulopenem (CP-70429) is an orally active, parenteral penem antibiotic with broad-spectrum activities against Gram-positive and Gram-negative bacteria. Sulopenem has the potential for urinary tract infections and intra-abdominal infections treatment. Sulopenem is inactive against Pseudomonas aeruginosa and Xanthomonas maltophilia[1][2][3].
SARS-CoV-2 nsp3-IN-2 is a macrodomain (Mac1) inhibitor with IC50 value of 180 μM. SARS-CoV-2 nsp3-IN-2 is a small molecule chemical probe and can be used for the research of viral[1].
Crotamiton is a drug that is used both as a scabicidal (for treating scabies) and as a general antipruritic. It is a prescription lotion based medicine that is applied to the whole body to get rid of the scabies parasite.
Caerulomycin A (Cerulomycin; Caerulomycin), an antifungal compound, induces generation of T cells, enhances TGF-β-Smad3 protein signaling via suppressing interferon-γ-induced STAT1 signaling. Antifungal and antibiotic activity, and used in autoimmune diseases[1].
Nesbuvir is a nonnucleoside inhibitor of the hepatitis C virus (HCV) nonstructural protein 5B (NS5B) polymerase.
Cyclophilin inhibitor 3 (compound 7c) is a potent cyclophilin A (CypA) inhibitor with an potent anti-HCV activity (EC50 of 4.2 μM)[1].
(-)-Corynoxidine is an acetylcholinesterase inhibitor with an IC50 value of 89.0 μM, isolated from the aerial parts of Corydalis speciosa[1].(-)-Corynoxidine exhibits antibacterial activities against Staphylococcus aureus and methicillin-resistant S. aureus strains in different degrees[2].
Tryglysin B is an antimicrobial peptide inhibits the growth of other streptococci[1].
HSV-1 Protease substrate is a peptide substrate for HSV-1 (Herpes Simplex Virus Type 1) protease, and the specificity constant (kcat/Km) at pH 7.5 for cleavage is 5.2 M-1 s-1[1].
Niazinin is a thiocarbamate glycoside with antileishmanial activities, with an IC50 value of 5.25 μM. Niazinin also shows a binding affinity with the target protein 3CL protease. Niazinin has promising leishmanicidal, anti-inflammatory and anti-pyretic activity[1][2].
Bromfenac is a potent and orally active inhibitor of COX, with IC50s of 5.56 and 7.45 nM for COX-1 and COX-2, respectively. Bromfenac can be used in ocular inflammation research[1].
Isopropyl 4-hydroxybenzoate (Isopropylparaben) is an antimicrobial and antioxidant agent[1].
Radezolid is a novel oxazolidinone antibiotic agent.