HA5 inhibits Streptococcus mutans biofilm with an IC50 value of 6.42 μM, without affecting its growth. HA5 also inhibits Streptococcus mutans glucan production and eDNA levels[1].
SARS-CoV-2 3CLpro-IN-3 (Compound 3d) is a SARS CoV-2 3CLpro inhibitor with antiviral, antibacterial and antifungal activities[1].
Avibactam free acid is a covalent, reversible β-lactamase inhibitor, inhibits β-lactamase TEM-1 and CTX-M-15 with IC50 of 8 nM and 5 nM, respectively.
Pentamidine (MP-601205) dimesylate is an antimicrobial agent and interferes with DNA biosynthetics. Pentamidine dimesylate inhibits parasite Leishmania infantum with an IC50 of 2.5 μM. Pentamidine dimesylate is a potent and selective protein tyrosine phosphatases (PTPases) and phosphatase of regenerating liver (PRL) inhibitor. Pentamidine dimesylate has the potential for Gambian trypanosomiasis, antimony-resistant leishmaniasis, and Pneumocystis carinii pneumonia treatment. Antitumor and antibacterial activities[1][2][3][4].
Antitubercular agent-39 (Compound P1) is a potent antitubercular agent. Antitubercular agent-39 is active against drug-resistant strains and drug-susceptible clinical isolates. Antitubercular agent-39 inhibits Mtb strain H37Rv with a MIC less than 1 μM[1].
Sisomicin is a broad-spectrum aminoglycoside antibiotic produced by Micromonospora inyoensis. sisomicin has great activity against gram-positive bacteria[1][2].
Maximin H3 is an antimicrobial peptide derived from the skin secretions of Chinese red belly toad Bombina maxima. Maximin H3 has activity against Escherichia coli ATCC25922, Staphylococcus aureus ATCC2592, Bacillus pyocyaneus CMCCB1010 and Candida albicans ATCC2002, the MIC values are 20, 10, 20, 5 μg/ml, respectively[1].
Antimicrobial agent-1 (compound 6C) possesses potent activity against TolC mutant E. coli with an MIC value of 2 μg/mL. Antimicrobial agent-1 and Colistin exhibit synergistic activity against Gram-negative bacteria. Antimicrobial agent-1 has no cytotoxicity on mammalian cell lines, with MICs > 128 μg/mL in Caco-2 and Vero cell lines[1].
Cefteram (T-2525) is the free acid of Cefteram pivoxil (HY-106571), which is an orally active cephalosporin ester. Cefteram potently targets to the enteropathogenic Enterobacteriaceae and Vibrionaceae[1].
Poly(hexamethylenebiguanide) hydrochloride is an antimicrobial agent, which can be used in medical, apparel, and household textile sectors[1].
PF 03709270 is an orally available ester prodrug form of sulopenem, with broad-spectrum antibacterial activity against most gram-positive and gram-negative bacteria.
LL-37(17-32) is a biological active peptide. (This peptide is an active segment of LL-37, a peptide derived from the C-terminal domain of human cathelicidin antimicrobial peptide. It has been reported that the LL17-32 peptide exhibits reversal effect on ABCG2-mediated multidrug resistance in cancer cell lines.)
Avenaciolide is an antifungal bis-γ-lactone found in Aspergillus avenaceus. Avenaciolide has also antibacterial action. Avenaciolide is a specific inhibitor of glutamate transport in rat liver mitochondria. Avenaciolide interferes with the ability of ADP to stimulate the rate of glutamate oxidation[1][2].
Lomefloxacin HCl is a fluoroquinolone antibiotic.Target: AntibacterialLomefloxacin is a bactericidal fluoroquinolone agent with activity against a wide range of gram-negative and gram-positive organisms. The bactericidal action of lomefloxacin results from interference with the activity of the bacterial enzymes DNA gyrase and topoisomerase IV, which are needed for the transcription and replication of bacterial DNA. DNA gyrase appears to be the primary quinolone target for gram-negative bacteria. Topoisomerase IV appears to be the preferential target in gram-positive organisms. Interference with these two topoisomerases results in strand breakage of the bacterial chromosome, supercoiling, and resealing. As a result DNA replication and transcription is inhibited [1].
Reltecimod (AB-103) is a T-cell-specific surface glycoprotein CD28 (TP44) antagonist. Reltecimod has beneficial effects against different bacterial infections, their exotoxins and endotoxins, and ionizing radiation. Reltecimod modulates the inflammatory response by targeting and attenuating the critical CD28/B7-2 co-stimulatory pathway, without inhibiting it. Reltecimod can be used to research necrotizing soft-tissue infections (NSTIs)[1][2].
Betonicine (Achilleine), an alkaloid, has cell protectant activity. Betonicine protects Bacillus subtilis against extremes in osmolarity and growth temperatures[1].
Lauric acid-13C is the 13C labeled Lauric acid. Lauric acid is a middle chain-free fatty acid with strong bactericidal properties. The EC50s for P. acnes, S.aureus, S. epidermidis, are 2, 6, 4 μg/mL, respectively.
Cefuroxime-d3 is deuterium labeled Cefuroxime (sodium). Cefuroxime sodium is an orally active second-generation cephalosporin antibiotic with increased stability to β-lactamase. Cefuroxime sodium has a broad spectrum activity against Gram-positive and Gram-negative bacteria[1].
Ceftolozane (CXA-101) sulfate is an antipseudomonal cephalosporin. Ceftolozane sulfate inhibits P. aeruginosa PAO1 with an MIC of 0.5 μg/mL. Ceftolozane sulfate can also inhibit β-lactam-resistant P. aeruginosa[1][2].
Clindamycin (hydrochloride) is a semisynthetic lincosamide antibiotic, which inhibits protein synthesis by acting on the 50S ribosomal.
Cephaloridine hydrate is a broad-spectrum antibacterial antibiotic. Cephaloridine has certain dose-related nephrotoxicity[1][2].
Demeclocycline is an orally active tetracycline antibiotic. Demeclocycline impairs protein synthesis by binding to the 30S ribosomal subunit to inhibit binding of aminoacyl tRNA. Demeclocycline shows anti-bacterial activitise to a wide variety of bacterial infections[1][2].
LeuRS-IN-1 hydrochloride is a potent, orally active M. tuberculosis leucyl-tRNA synthetase (M.tb LeuRS) inhibitor. LeuRS-IN-1 hydrochloride has IC50 and Kd values of 0.06 μM, 0.075 μM for M.tb LeuRS, respectively[1]. LeuRS-IN-1 hydrochloride inhibits human cytoplasmic LeuRS (IC50=38.8 μM), and HepG2 protein synthesis (EC50=19.6 μM)[2].
Capreomycin is a macrocyclic peptide antibiotic. Capreomycin can be used for anti-multidrug-resistant-tuberculosis research. Capreomycin can inhibit phenylalanine synthesis in in mycobacterial ribosomes translation[1][2]
Estradiol is a steroid sex hormone vital to the maintenance of fertility and secondary sexual characteristics in females.
IDR-1 is an antimicrobial peptide that is active against Gram-positive and Gram-negative bacteria. IDR-1 counters infection by selective modulation of innate immunity without obvious toxicities. IDR-1 has anti-inflammatory and anti-infective properties, enhances the levels of monocyte chemokines, and attenuates pro-inflammatory cytokine release[1][2].
Potassium guaiacolsulfonate hemihydrate is an orally active expectorant used for acute respiratory tract infections. Potassium guaiacolsulfonate hemihydrate helps loosen mucus and used for a cough caused by the common cold, infections or allergies in combination with other drugs[1][2].
Bethoxazin(Bethoguard) is a new broad spectrum industrial microbicide with applications in material and coating preservation.IC50 value:Target: MicrobicideBethoxazin potently inhibited the catalytic activity of yeast DNA topoisomerase II and the growth of yeast BY4742 cells at low micromolar concentrations. bethoxazin may exert its microbicidal action by reacting with sensitive endogenous sulfhydryl biomolecules of microbial cells.
Nybomycin, an antibiotic, exhibits antiphage and antibacterial properties. Nybomycin binds to DNA and induces a unique morphological change to mycobacterial bacilli leading the bacterial cell death[1][2].
Urease-IN-8 (Compound 5e) is a competitive Urease inhibitor (IC50: 3.51 μM, Ki: 3.11 μM). Urease-IN-8 can be used for research of peptic and gastric ulcers[1].