Nifurtimox, an antiprotozoal agent, which is generally used for the treatment of infections with Trypanosoma cruzi, has been used in the therapy of neuroblastoma. Nifurtimox affects enzyme activity of lactate dehydrogenase (LDH).
Isavuconazole D4 (BAL-4815 D4) is a deuterium labeled Isavuconazole (BAL-4815). Isavuconazole is a triazole prodrug with antifungal activity against yeasts, molds, and dimorphic fungi[1].
Clotrimazole is an imidazole derivative, an antifungal compound and is a CYP (cytochrome P450) inhibitor.Target: Antifungal; CYPClotrimazole (brand name Canesten or Lotrimin) is an antifungal medication commonly used in the treatment of fungal infections (of both humans and other animals) such as vaginal yeast infections, oral thrush, and ringworm. It is also used to treat athlete's foot and jock itch.It is commonly available as an over-the-counter substance in various dosage forms, such as a cream, and also (especially in the case of ear infection) as a combination medicine. It is also available as a troche or throat lozenge (prescription only). For ear infection, it is often applied in liquid form, as ear drops.The antimycotic drug clotrimazole inhibits the function of the gastric H,K-ATPase in a manner similar to that observed for the Na,K-ATPase. Because of the high hydrophobicity of the compound, the interaction between clotrimazole and the ion pump occurs at the membrane domain in the apolar core of the membrane. The enzymatic activity was inhibited with a half-saturating concentration of 5.2 microM. Various partial reactions of the pump cycle were analyzed with the electrochromic styryl dye RH421 that has been widely used to study the transport mechanism of P-type ATPases.
Rilpivirine (R278474) hydrochloride is a potent and specific diarylpyrimidine (DAPY) non-nucleoside reverse transcriptase inhibitor (NNRTI). Rilpivirine hydrochloride has high antiviral activity against wild-type HIV (EC50=0.4 nM) and mutant viruses (EC50=0.1-2.0 nM). Rilpivirine hydrochloride has a high genetic barrier to resistance development of HIV[1][2].
α-Isolupanine is an alkaloid. α-Isolupanine can be isolated from Narrow-Leafed Lupin (PLupinus angustifolius L.). α-Isolupanine can be used for the research of anthracnose[1].
ITMN 4077 is a macrocyclic inhibitor against Hepatitis C Virus (HCV) NS3 protease (EC50: 2131 nM)[1][2].
Aflavarin is produced from cluster 39 expressed mainly in sclerotia. Aflavarin exhibits anti-insectan activity [1].
Isopropyl ((R)-(perfluorophenoxy)(phenoxy)phosphoryl)-L-alaninate can be used to synthesis Sofosbuvir (HY-15005) to avoid the production of sofibuvir degradation impurities[1].
Kojic acid is a natural substance produced by Aspergillus oryzae, also used as an anti-oxidant and radio-protective agent[1].
Dunnianol is a natural sesqui-neoligan with moderate antibacterial activity. Dunnianol inhibits Staphylococcus aureus and methicillin-resistant Staphylococcus aureus (MRSA).
Deoxyshikonin is isolated from Lithospermum erythrorhizon Sieb with antitumor activity. Deoxyshikonin increases the expression of VEGF-C and VEGF-A mRNA in HMVEC-dLy, promotes HIF-1α and HIF-1β subunit interaction and binds to specific DNA sequences targeted by HIF, indicates a prolymphangiogenesis as well as a proangiogenesis effect in vitro[1]. Deoxyshikonin shows significant synergic antimicrobial activity with tetracycline against S. pneumonia (MIC=17 μg/mL), also shows significantly inhibitory activities against MRSA[2].
Cefozopran Hcl(SCE 2787 Hcl) is a fourth-generation cephalosporin.Target: AntibacterialCefozopran is a fourth-generation cephalosporin.
2'-Deoxy-β-L-uridine is a nucledside analogue and a specific substrate for the viral enzyme, shows no stereospecificity against herpes simplex 1 (HSV1) thymidine kinase (TK). 2′-Deoxy-β-L-uridine exerts antiviral activity via the interation of 5'-triphosphates with the viral DNA polymerase[1][2].
Macranthoside B, isolated from Flos Lonicerae, possesses anti-bacterial activity[1].
Rediocide A is a highly modified daphnane with potent insecticidal activity. Rediocide A can be isolated from Trigonostemon reidioides[1].
Cyclothialidine ( Ro 09-1437) is a potent DNA gyrase inhibitor isolated from Streptomyces filipinensisNR0484[1].
Hepatitis Virus C NS3 Protease Inhibitor 2 is a product-based peptide inhibitor of hepatitis C virus (HCV) NS3 protease, with a Ki of 41 nM[1].
Carvone is a ketone monoterpene found mostly in the essential oils from plants of the genus Mentha. Carvone is widely used in the pharmaceutical industry, cosmetics and agriculture. Carvone has such effects as antimicrobial, antioxidant, anti-inflammatory, antispasmodic, antinociceptive, anticonvulsant[1].
Nuezhenidic acid, isolated from the fruits of Ligustrum lucidum, posseses inhibitory activities against influenza A virus[1].
BMS-790052 is a highly selective inhibitor of HCV NS5A with EC50 of 9-50 pM, for a broad range of HCV replicon genotypes and the JFH-1 genotype 2a infectious virus in cell culture.IC50 Value: 9-50 pMTarget: HCV NS5ABMS-790052 has broad genotype coverage and exhibits picomolar in vitro potency against genotypes 1a (EC50 50pm) and 1b (EC50 9pm). BMS-790052 produces a robust decline in HCV RNA (-3.6 logs after 48 hours from a single 100 mg) dosefollowing a single dose in patients chronically infected with HCV genotype 1.
RVG (RVG29) is a peptide derived from Rabies Virus Glycoprotein that binds to the α-7 subunit of nicotinic acetylcholine receptors (AchR) of neuronal cells. RVG enhances delivery of Mycobacterium tuberculosis antigens to antigen-presenting cells[1].
Nerol is a constituent of neroli oil. Nerol Nerol triggers mitochondrial dysfunction and induces apoptosis via elevation of Ca2+ and ROS. Antifungal activity[1][2].
Hispidulin 4'-O-β-D-glucopyranosid, a natural compound, may serve as a potential COVID-19 main protease inhibitor[1].
Secnidazole (RP-14539) hemihydrate is an orally active azole antibiotic and a imidazole mitigator of Serratia marcescens virulence. Secnidazole (hemihydrate), as an analog of acylhomoserine lactones, effectively inhibits QS resulting in the attenuation of Pseudomonas aeruginosa pathogenesis. Secnidazole (hemihydrate) has antimicrobial activity against many anaerobic Gram-negative and Gram-positive bacterial species in vitro. Secnidazole (hemihydrate) can be used for the research of various diseases, such as amoebiasis and giardiasis, and bacterial vaginitis[1][2][3].
Magainin 2 is an antimicrobial peptide discovered in the skin of Xenopus laevis.
Ceftiofur sodium is an antibiotic of the cephalosporin type (third generation), licensed for use in veterinary medicine.
Nebacumab (HA-1A) is a monoclonal antibody that binds to lipid A portion of endotoxin. Nebacumab can be used of research of sepsis[1][2].
CP-28888 is an interferon inducer, more potent in mice, but is less active in man and devoid of antirhinovirus effects.
Kulactone, a natural bioflavonoid and an inhibitor against jRdRp, possesses antifungal, antibacterial and antiplasmodial activities. Kulactone exhibit no crossing through Blood Brain Barrier (BBB)[1][2].
Alexidine, a bis-biguanide, exhibits antifungal and antibiofilm activity against a diverse range of fungal pathogens. Alexidine is an anticancer agent that targets a mitochondrial tyrosine phosphatase, PTPMT1, in mammalian cells and causes mitochondrial apoptosis[1].