Antimicrobial agent-3 (Compound U10) is an antimicrobial agent against bacterial, fungal and tubercular infections[1].
Ketotifen (HC 20-511) is an orally active second-generation noncompetitive histamine 1 (H1) receptor blocker and mast cell stabilizer. Ketotifen can block 6-phosphogluconate dehydrogenase (PGD) in vitro. Ketotifen also has antiviral activity against SARS-CoV-2 and Influenza virus. Ketotifen can be used to the research of autoimmune encephalomyelitis (EAE) and asthma attack prevention[1][2][3][4].
c[Arg-Arg-Arg-Arg-Nal-Nal-Nal] (Compound 9C) shows broad-spectrum activity against drug-resistant Gram-positive and Gram-negative bacteria, with MICs of 3.1, 3,1, 12.5, and 25 μg/mL for MRSA (ATCC BAA-1556), S. aureus (ATCC 29213), P. aeruginosa (ATCC 27883), and E. coli (ATCC 25922), respectively[1].
Aleurodiscal is an fungal inhibitor that can be obtained from cultures of Aleurodiscus mirabilis. Aleurodiscal can be used in the study of fungal infections[1].
Sulfanilamide is a competitive inhibitor for bacterial enzyme dihydropteroate synthetase with IC50 of 320 μM.Target: dihydropteroate synthetase; AntibacterialSulfanilamide containing the sulfonamide functional group displays inhibitory activity for dihydropteroate synthetase partially purified from Escherichia coli which normally uses para-aminobenzoic acid (PABA) for synthesizing the necessary folic acid acting as a coenzyme in the synthesis of purine, pyrimidine and other amino acids, exhibiting an IC 50 of 320 μM for dihydropteroate synthetasea and Km of 2.5 uM for PABA [1]. Sulfanilamide shows IC50 of 286.8 μg/mL for recombinant S. cerevisiae strains with wild-type FOL1 genes, but the single mutation 55Trp to 55Ala or 57Pro to 57Ser within the putative active site of the fungal DHPS confers resistance to Sulfanilamide with IC50 of >800 μg/mL [2]. Administration of Sulfanilamide with the dosage of 100 mg/kg/day is effective in the prevention of P. carinii infection in the immunosuppressed rat model. When the dosage of sulfaguanidine and Sulfanilamide reduced to 10 mg/kg/day, breakthrough P. carinii infection occurs in the rats [3].
Ecubectedin is a derivative. Ecteinascidins is a family of tetrahydroisoquinoline alkaloids with wide range of antitumor and antimicrobial activities[1].
Ribostamycin is a broad-spectrum antimicrobial, inhibits bacterial protein synthesis at the level of 30S and 50S ribosomal subunit binding, also inhibits the chaperone activity of protein disulfide isomerase (PDI), used in pharmacokinetic and nephrotoxicity studies
Spergualin trihydrochloride is a natural product that first identified as an antibiotic from culture filtrates of Bacillus laterosporus BMG162-aF2[1].
NVR 3-778 is a first-in-Class and oral bioavailable HBV CAM (capsid assembly modulator) belonging to the SBA (sulfamoylbenzamide) class, with anti-HBV activity[1].
Fangchinoline is isolated from Stephania tetrandra with extensive biological activities, such as enhancing immunity, anti-inflammatory sterilization and anti-atherosclerosis. Fangchinoline, a novel HIV-1 inhibitor, inhibits HIV-1 replication by impairing gp160 proteolytic processing[1]. Fangchinoline targets Focal adhesion kinase (FAK) and suppresses FAK-mediated signaling pathway in tumor cells which highly expressed FAK[2]. Fangchinoline induces apoptosis and adaptive autophagy in bladder cancer[3].
Cefalonium hydrate is the first-generation β-lactam cephalosporin antibiotic that is widely used to research bovine mastitis caused by Gram-positive bacteria including staphylococci[1][2][3].
Tulathromycin B (CP 547272) is an isomer of Tulathromycin (a macrolide antibiotic)[1].
HIV-1 protease-IN-1 (Compound 1e) is a potent inhibitor of HIV-1 protease with an IC50 of 90 pM. HIV-1 protease-IN-1 demonstrates antiviral activity with EC50 value of 89 nM against B-HIV. HIV-1 protease-IN-1 exhibits activity with EC50 value of 13.59 nM against C-HIV strain ZM246. HIV-1 protease-IN-1 shows remarkable activity with EC50 value of 8.23 nM against C-HIV strain Indie[1].
Sarecycline is an orally effective narrow-spectrum tetracycline derivative antibiotic. Sarecycline has anti-inflammatory activity. Sarecycline inhibits the activity of Gram-positive bacteria and several types of keratobacterium acnes. Sarecycline interferes with tRNA accommodation and tethers mRNA to the 70S ribosome. Sarecycline can be used to study moderate to severe acne[1][2][3][4][5][6].
Mericitabine (R-7128) is a nucleoside inhibitor of the HCV NS5B polymerase that acts as an RNA chain terminator and prevents elongation of RNA transcripts during replication.
Isobutylparaben (Isobutyl 4-hydroxybenzoate) is a constitutive androstane receptor (CAR) activator. Isobutylparaben has a broad-spectrum antimicrobial activity and widely used in personal care products and cosmetics[1].
Isoprothiolane is a systemic fungicide. Isoprothiolane is a rice blast controlling agent against the fungal disease of rice planty Pyvioutavia oryzae Cav[1].
Caprochlorone has antiviral activity against orthopoxvirus. Caprochlorone can inhibit cell penetration by virus, also delays release of newly formed virus from the cell. Caprochlorone decreases the titers of influenza virus in infected-mice lungs[1][2][3].
A40926, the precursor of Dalbavancin, is a second-generation glycopeptide antibiotic. A40926 inhibits gram-positive bacteria, and is very active against Neisseria gonorrhoeae[1].
Ludaconitine, isolated from Aconitum spicatum (Bruhl) Stapf, exhibits antileishmanial activity with an IC50 of 36.10 μg/mL[1].
BioA-IN-13 is a potent, cell permeable and whole-cell active inhibitor of Mycobacterium tuberculosis BioA enzyme[1].
Doxycycline calcium, an antibiotic, is an orally active and broad-spectrum metalloproteinase (MMP) inhibitor[1]. Doxycycline calcium shows antibacterial activity and anti-cancer cell proliferation activity[1][2][3][4][5].
Merimepodib is a novel noncompetitive inhibitor of IMPDH (Inosine monophosphate dehydrogenase).
Cefamandole is a second-generation broad-spectrum cephalosporin antibiotic. As the antibiotic is broken down in the body, it releases free NMTT, which can cause hypoprothrombinemia.
Blasticidin A ((+)-Blasticidin A) is an inhibitor of Aflatoxin production by Aspergillus parasiticus. Blasticidin A almost completely inhibits Aflatoxin production at 0.5 μM[1]. Blasticidin A is a potent antibiotic produced by Streptomyces, inhibits Aflatoxin production without strong growth inhibition toward Aflatoxin-producing fungi[2].
FGI-106 is a broad-spectrum inhibitor of multiple blood-borne viruses (HCV, HBV, HIV) as well as emerging biothreats (Ebola, VEE, Cowpox, PRRSV infection) with EC50 of 0.2-10 uM; inhibits the interaction of TSG101 with its cognate viral ligands; displays an ability to prevent lethality from Ebola in vivo; well-tolerated and orally bioavailable.
FPI-1523, a derivative of Avibactam, is a potent β-lactamase inhibitor, with Kds of 4 nM and 34 nM for CTX-M-15 and OXA-48, respectively. FPI-1523 also inhibits PBP2, with an IC50 of 3.2 μM. FPI-1523 exhibits considerable antimicrobial activity[1].
Dermaseptin-S2 is an antimicrobial peptide derived from frog skin against filamentous fungi[1].
Proguanil is an antimalarial prodrug that is metabolized to the active metabolite cycloguanil, a dihydrofolate reductase (DHFR) inhibitor.
CRS400393 is a potent antimycobacterial agent, with MIC of 0.03, 2, and ≤ 0.12 µg/mLagainst M. abs., M. avium, M. intracellulare, and M. tuberculosis, respectively[1].