Amustaline (S-303) dihydrochloride, a nucleic acid-targeted alkylator, is an efficient pathogen inactivation agent for blood components containing red blood cells. Amustaline dihydrochloride has three components: an acridine anchor (an intercalator that targets nucleic acids non-covalently), an effector (a bis-alkylator group that reacts with nucleophiles), and a linker (a small flexible carbon chain containing a labile ester bond that hydrolyzes at neutral pH to yield non-reactive breakdown products)[1][2].
Rivabazumab pegol is a PcrV protein antibody that can be used to study the phase II pegylated Fab of chronic Pseudomonas aeruginosa infection[1].
Bisdionin C is a potent GH18 chitinases inhibitor, with an IC50 of 0.2 μM for A. fumigatus ChiB1 (AfChiB1). Bisdionin C inhibits HCHT (human macrophage chitotriosidase) and acidic mammalian chitinase (AMCase) with IC50s of 8.3 and 3.4 μM, respectively[1].
Dipyrithione is a potent antimicrobial agent. Dipyrithione shows antifungal activity and antiproliferative activity. Dipyrithione induces apoptosis and cycle arrest at G1 phase. Dipyrithione shows anti-inflammatory activity in vivo. Dipyrithione shows anti-tumor activity. Dipyrithione has the potential for the research of dermatophytosis[1][2][3].
Flomoxef is a oxacephem group antibiotic, with excellent activity against various Gram-positive bacteria[1][2].
Rifaximin(Xifaxan) is an orally administered, semi-synthetic, nonsystemic antibiotic derived from rifamycin SV with antibacterial activity.IC50 Value:Target: RNA polymerase; antibacterialRifaximin is a semisynthetic, rifamycin-based non-systemic antibiotic, meaning that very little of the drug will pass the gastrointestinal wall into the circulation as is common for other types of orally administered antibiotics. It is used in the treatment of traveler's diarrhea and hepatic encephalopathy, for which it received orphan drug status from the U.S. Food and Drug Administration in 1998. Rifaximin interferes with transcription by binding to the β-subunit of bacterial RNA polymerase. This results in the blockage of the translocation step that normally follows the formation of the first phosphodiester bond, which occurs in the transcription process. From Wikipedia.
Omadacycline hydrochloride is novel, aminomethyl tetracycline antibiotic being developed for the treatment of community-acquired bacterial infections. The ED50 for Escherichia coli is 2.02 mg/kg.
Trimipramine is a 5-HT receptor antagonist, with pKi binding values of 6.39, 8.10, 4.66 for 5-HT1C, 5-HT2 and 5-HT1A, respectively. Trimipramine is also a potent and selective inhibitor targeting human noradrenaline (hNAT), serotonin (hSERT) and organic cation transporters (hOCT1, hOCT2) with IC50 values of 4.99 μM, 2.11 μM, 3.72 μM, 8.00 μM, respectively. Trimipramine has vascular activity and anxiolytic efficacy[1][2][3].
Tibezonium iodide, an oropharyngeal disinfectant, has antibacterial activity for the prevention of mouth infections[1].
Saccharin sodium hydrate is an orally active, non-caloric artificial sweeteners (NAS). Saccharin sodium hydrate has bacteriostatic and microbiome-modulating properties[1].
Zidebactam sodium salt (WCK-5107 sodium salt) is a potent β-lactamase inhibitor[1]. Zidebactam also is a penicillin-binding protein2 (PBP2) inhibitor with an IC50 of 0.26 μg/mL[2].
Tilapia piscidin 3 is an antimicrobial peptide with antibacterial activity against gram-positive and -negative bacteria (MIC: 2.44, 2.44, 9.78, 19.55, 0.61 μg/mL for V. vulnificus 204, V. alginolyticus, S. agalactiae 819, E. faecalis BCRC 10066, S. agalactiae BCRC 10787). Tilapia piscidin 3 has hemolytic activity in fish red blood cells[1].
Faropenem daloxate is the first oral penem in a new class of beta-lactam antibiotics.IC50 Value: Target: AntibacterialFaropenem daloxate is useful for penem and antibiotics. Faropenem medoxomil has excellent in vitro activity against Streptococcus pneumoniae, Haemophilus influenzae and other key pathogens implicated in acute bacterial rhinosinusitis. Clinical studies have demonstrated that, in the treatment of acute bacterial rhinosinusitis in adults, 7 days of treatment with faropenem medoxomil is as clinically and bacteriologically effective as 10 days of treatment with cefuroxime axetil. One study showed faropenem medoxomil to be superior to cefuroxime axetil. Overall, the safety profile of faropenem medoxomil is similar to that of most comparators.
Iboxamycin is a potent antibiotic candidate bearing a fused bicyclic amino acid residue. Iboxamycin is orally bioavailable, safe and effective in treating both Gram-positive and Gram-negative bacterial infections in mice[1][2].
Antitubercular agent-9 shows effective antitubercular activity with a MIC value of 1.03-2.32 μM.
Capreomycin is a peptide antibiotic, commonly grouped with the aminoglycosides, which is given in combination with other antibiotics for MDR-tuberculosis.IC50 value:Target: The drug should not be given with streptomycin or other drugs that may damage the auditory vestibular nerve. Patients on this drug will often require audiology tests. It is a cyclic peptide.Capreomycin is administered intramuscularly and shows bacteriostatic activity.
Antibacterial agent 41 (example 3) is a antibacterial agent (extracted from patent WO2013030735A1)[1].
Polistes mastoparan is an antimicrobial peptide. Polistes mastoparan increases S. aureus cell K+ efflux and inhibits cell viability with EC50 of 5 μM[1].
Clindamycin is an oral protein synthesis inhibitory agent that has the ability to suppress the expression of virulence factors in Staphylococcus aureus at sub-inhibitory concentrations (sub-MICs). Clindamycin resistance results from enzymatic methylation of the antibiotic binding site in the 50S ribosomal subunit (23S rRNA). Clindamycin decreases the production of Panton-Valentine leucocidin (PVL), toxic-shock-staphylococcal toxin (TSST-1) or alpha-haemolysin (Hla)[1].
Sulfisoxazole (Sulfafurazole) diethanolamine is an endothelin receptor antagonist with IC50 values of 0.60 μM and 22 μM against endothelin receptor A and endothelin receptor B, respectively. Sulfisoxazole diethanolamine is a sulfonamide antibacterial with an oxazole substituent. Sulfisoxazole diethanolamine inhibits breast cancer exosome release by targeting endothelin receptor A[1][2].
Antibacterial agent 143 (Compound 5a) is an antibacterial agent with MICs of 25, 25, 50 and 50 μg/mL against B. subtilis ATCC6633, . aureus ATCC6538, P. aeruginosa ATCC13525 and E. coli ATCC35218, respectively[1].
Murrayanol is a natural carbazole alkaloid with a variety of biological activities. Murrayanol shows anti-inflammatory, topoisomerase I and topoisomerase II (Topoisomerase) inhibition activities. Murrayanol also as a mosquitocidal and antimicrobial[1].
Chrysomycin B is an antibiotic isolated from a strain of Streptomyces. Chrysomycin B causes DNA damage in the human lung adenocarcinoma A549 cell line and inhibits topoisomerase II. Chrysomycin B suppresses the growth of transplantable tumors in mice.
Moxifloxacin-d3 is the deuterium labeled Moxifloxacin. Moxifloxacin is an orally active 8-methoxyquinolone antimicrobial for use in the treatment of acute bacterial sinusitis, acute bacterial exacerbations of chronic bronchitis, and community-acquired pneumonia.
Cephalexin-d5 is deuterium labeled Cephalexin. Cephalexin (Cefalexin; Cephacillin) is a potent, orally active and the first-generation cephalosporin antibiotic. Cephalexin kills gram-positive and some gram-negative bacteria by disrupting the growth of the bacterial cell wall. Cephalexin monohydrate is used for the research of pneumonia, strep throat, and bacterial endocarditis, et al[1].
Antibacterial agent 18 is a multi-arm AIE molecule extracted from patent CN110123801A, compound 23. Antibacterial agent 18 can be used for resisting Gram-positive and Gram-negative bacteria. Antibacterial agent 18 can be conjugated in the cell wall of rigid arm configuration insertion bacterium, and block cell wall turns sugar and turns peptide process, to inhibit or kill bacterium[1].
Penicillin V (Phenoxymethylpenicillin) is a potent and orally active antibiotic. Penicillin V shows antibacterial activity for Streptococci, Clostridium difficile and staphylococcus aureus. Penicillin V has the potential for the research of otitis, sinusitis, pharyngitis and tonsillitis[1][2][3][4].
Isoconazole nitrate is a broad-spectrum antimicrobial agent with a highly effective antimycotic and gram-positive antibacterial activity, a rapid rate of absorption and low systemic exposure potential. Isoconazole nitrate is effective against pathogens involved in dermatomycoses, with minimum inhibitory concentrations well below the concentration of ISN in skin and hair follicles.
Ornidazole-d5 is deuterium labeled Ornidazole.