L-K6L9 shows antimicrobial and antibiofilm activities against P. aeruginosa from cystic fibrosis patients. L-K6L9 is stable and resistant to degradation by cystic fibrosis sputum proteases and will not induce bacterial resistance [1].
Zidovudine is a nucleoside reverse transcriptase inhibitor (NRTI), widely used to treat HIV infection. Zidovudine increases CRISPR/Cas9-mediated editing frequency.
Questin is an antibacterial agent isolated from marine Aspergillus flavipes. Questin exhibits antibacterial activity against V. harveyi, V. anguillarum, V. cholerae, and V. parahemolyticus with MIC values of 31.25 µg/mL, 62.5 µg/mL, 62.5 µg/mL, and 125 µg/mL[1].
Macrocarpal A (10-epi-Eucarobustol F) is an antibacterial agent isolated from the leaves of Eucalyptus macrocarpa. Macrocarpal A inhibits the growth of Bacillus subtilis PCI219 (minimum inhibitory concentration below 0.2 µM) and Staphylococcus aureus FDA209P (minimum inhibitory concentration is 0.4 µM)[1].
Gramicidin B is a nonribosomal peptide antibiotic[1].
α-Artemether is an antimalarial compound[1].
Hepatitis B Virus Core (128-140) is a peptide of hepatitis B virus core protein.
HIV-1 inhibitor-29 (compound 14d2) is a potent HIV-1 inhibitor with an EC50 of 2.18 μM for HIV-1 IIIB. HIV-1 inhibitor-29 has high anti-resistance profile toward F227L/V106A strain (EC50 = 0.974 μM), and exhibits low cytotoxicity in MT-4 cells (CC50 = 211 μM). HIV-1 inhibitor-29 can be used for researching AIDS[1].
Cefpodoxime proxetil impurity B is an impurity of Cefpodoxime proxetil (HY-N7101). Cefpodoxime Proxetil is a first oral and broad spectrum antibiotic that belongs to the third generation of cephalosporin[1].
Azidamfenicol is a broad-spectrum chloramphenicol-like antibiotic. Azidamfenicol inhibits ribosomal peptidyltransferase (Ki=22 µM)[1].
Lithium chloride hydrate, an orally active mood stabilizer, is a potent virus inhibitor and effective immunomodulatory agent. Lithium chloride hydrate has antidepressant activity by inhibiting GSK3β and promoting neurogenesis. Lithium chloride hydrate alleviates cognition dysfunction and the symptoms of acute mania and depression. Lithium chloride hydrate can also be used for research of virus infection and Alzheimer's disease[1][2][3].
Maximin 1 is an antimicrobial peptide derived from skin secretions of Bombina maxima. Maximin 1 has cytotoxicity on tumor cells and spermicidal effect[1].
Azidocillin, a semi-synthetic Penicillin, is an orally active β-lactam antibiotic. Azidocillin bears an azide functionality and retains on-target activity within bacteria. Azidocillin can be used to research osteitis caused by dental surgery, otitis media, enterococcal septicemia and other bacterial infectious diseases[1][2][3].
STING agonist-25 (CF505) is a non-nucleotide small-molecule STING agonist. STING agonist-23 activates STING, increases phosphorylation of STING, TBK1 and IRF3. STING agonist-23 promotes the levels of IFN-β, IL-6, CXCL-10, TNF-α, ISG-15, and CCL-5 in tumor cells. STING agonist-23 exhibits activity against SARS-CoV series strains[1].
Aripiprazole (OPC-14597) monohydrate, an atypical antipsychotic, is a potent and high-affinity dopamine D2 receptor partial agonist. Aripiprazole monohydrate is an inverse agonist at 5-HT2B and 5-HT2A receptors and displays partial agonist actions at 5-HT1A, 5-HT2C, D3, and D4 receptors. Aripiprazole monohydrate can be used for the research of schizophrenia and COVID19[1][2][3][4].
Nemonoxacin (TG-873870) malate is a nonfluorinated quinolone antibiotic. Nemonoxacin malate has broad-spectrum activity against Gram-positive, Gram-negative and atypical pathogens. Nemonoxacin malate can inhibit drug-resistant Streptococcus pneumoniae and (HY-121544) Methicillin-resistant Staphylococcus aureus. Nemonoxacin malate can be used for the research of community-acquired pneumonia[1][2].
Tigecycline is a first-in-class, broad spectrum antibiotic with activity against antibiotic-resistant organisms.Target: AntibacterialTigecycline is active against a broad range of gram-negative and gram-positive bacterial species including clinically important multidrug-resistant nosocomial and community-acquired bacterial pathogens. Tigecycline has been shown to inhibit the translation elongation step by binding to the ribosome 30S subunit and preventing aminoacylated tRNAs to accommodate in the ribosomal A site [1]. Tigecycline has also been found to be effective for the treatment of community- as well as hospital-acquired and ventilator-associated pneumonia and bacteremia, sepsis with shock and urinary tract infections. Tigecycline appears to be a valuable treatment option for the management of superbugs, especially where conventional therapy has failed [2].Fifteen patients received tigecycline for 16 episodes of CPKP infection. The main infections were pneumonia (31%), urinary tract infection (31%), peritonitis (20%), catheter-related bacteraemia (12%), and meningitis (6%). Most infections were complicated with severe sepsis (44%), septic shock (12%), and/or bacteraemia (19%). The daily maintenance dose of tigecycline was 200 mg in 10 episodes and 100 mg in 6 episodes. The overall 30-day mortality rate was 25%. Univariate analysis showed that mortality was significantly associated (p < 0.01) with mean APACHE II and SOFA scores and the presence of immunosuppression, but not with the tigecycline dose [3].
Antibacterial agent 109 (Compound C-2) is a potent antibacterial agent against both gram-positive and gram negative bacteria, and non-mutagenic. Antibacterial agent 109 inhibits protein synthesis by blocking the extension of new peptide chains[1].
Tetracycline is a broad-spectrum antibiotic, exhibiting activity against a wide range of gram-positive and gram-negative bacteria.
Rifamycin S is a quinone and an antibiotic agnet against Gram-positive bacteria (including MRSA). Rifamycin S is the oxidized forms of a reversible oxidation-reduction system involving two electrons. Rifamycin S generates reactive oxygen species (ROS) and inhibits microsomal lipid peroxidation. Rifamycin S can be used for tuberculosis and leprosy[1][2][3].
Vulpinic acid, a lichen metabolite, decreases H2O2-induced ROS production, oxidative stress and oxidative stress-related damages in human umbilical vein endothelial cells (HUVEC). Vulpinic acid is active against staphylococci, enterococci, and anaerobic bacteria.Vulpinic acid has the potential for atherosclerosis research[1][2].
Anti-MRSA agent 8 (Compound 7g) is a DAPG derivative with strong antibacterial activity. Anti-MRSA agent 8 assertes its activity by targeting bacterial cell membranes. Anti-MRSA agent 8 can be used for the research of methicillin-resistant Staphylococcus aureus (MRSA)[1].
4-Hydroxybenzoic acid, a phenolic derivative of benzoic acid, could inhibit most gram-positive and some gram-negative bacteria, with an IC50 of 160 μg/mL.
HCV-IN-3 is a hepatitis C virus (HCV) NS3/4a protein inhibitor, with an IC50 of 20 μM, a Kd of 29 μM.
Fumagillin(NSC9168) is a complex biomolecule and used as an antimicrobial agent.Target: AntiparasiticFumagillin is an active amebicide and anti-infective isolated from the fungus Aspergillus fumigatus. Fumagillin does exhibit some side effects that have deterred its acceptance as a viable treatment, but the current body of research on the synthesis of novel analogs of this molecule shows an exciting and promising revival of this drug as both an anti-infective and antiangiogenic agent [1].
Cyclo(L-leucyl-L-valyl) inhibits Aflatoxin production by Aspergillus parasiticus.Cyclo(L-leucyl-L-valyl) inhibits transcription of the Aflatoxin-related genes aflR, hexB, pksL1, and dmtA.[1].
Limonin is a triterpenoid enriched in citrus fruits, which has antivirus and antitumor ability.IC50 Value: Target: HIV; anticancerLimonin is a triterpenoid aglycone that is a bitter principle of citrus fruits. Limonin is chemically induced carcinogenesis inhibitor and HIV-1 replication inhibitor. Limonin has anti-proliferative, proapoptotic activity on several cancer cell lines and inhibits azoxymethane-induced colon cancer in rats. Limonin also inhibits HIV-1 replication in culturedf monocytes, macrophages, and mononuclear cells, perhaps by inhibition of HIV-1 protease activity.
Azithromycin hydrate is a macrolide antibiotic useful for the treatment of a number of bacterial infections.
Ganoderic acid GS-1, a highly oxygenated lanostane-type triterpenoid, has anti-HIV-1 protease activities with an IC50 of 58 μM[1].
EACC is a reversible autophagy inhibitor, which can block autophagic flux. EACC selectively inhibits the translocation of autophagosome-specific SNARE Stx17 thereby blocking autophagosome-lysosome fusion[1].