Delamanid, a newer mycobacterial cell wall synthesis inhibitor, inhibits the synthesisi of mucolic acids, cruciala component of the cell wall of the Mycobacterium tuberculosis complex.In vitro: inhibits the synthesisi of mucolic acids, cruciala component of the cell wall of the Mycobacterium tuberculosis complex.[1]In in-vitro studies, delamanid shows more potent antibacterial activity against drug-susceptible and drug-resistant strains of M. tuberculosis.[2] Delamanid do not affect rifampin, pyrazinamide, and isoniazid exposure; the ethambutol AUCτ and Cmax values are about 25% higher with delamanid coadministration. [3] In vivo: Twice-daily oral dosing of delamanid at 30 mg kg-1 for 5 days resulted in sterile cures in a mouse model of VL. [4]
Thalrugosaminine is a benzylisoquinoline alkaloid isolated from the roots of Thalictrum minus. Thalrugosaminine shows good antibacterial activity with MIC values of 64-128 µg/ml[1].
4-Chlorosalicylic acid is a pharmaceutical intermediate. Inhibits monophenolase and diphenolase activity with IC50s of 1.89 mM and 1.10 mM. Potent antimicrobial activity. Against E. coli with the MIC of 250 μg/mL and with the MBC of 500 μg/mL.
Actinomycin D inhibits DNA repair with an IC50 of 0.42 μM.
Trovafloxacin is a broad-spectrum quinolone antibiotic with potent activity against Gram-positive, Gram-negative and anaerobic organisms. Trovafloxacin blocks the DNA gyrase and topoisomerase IV activity. Trovafloxacin is also a potent, selective and orally active pannexin 1 channel (PANX1) inhibitor with an IC50 of 4 μM for PANX1 inward current. Trovafloxacin does not inhibit connexin 43 gap junction or PANX2. Trovafloxacin leads to dysregulated fragmentation of apoptotic cells by inhibiting PANX1[1][2][3].
Amikacin sulfate(BAY416651 sulfate) is a semi-synthetic aminoglycoside antibiotic derived from kanamycin A.Target: AntibacterialAmikacin disrupts bacterial protein synthesis by binding to the 30S ribosome of susceptible organisms. Binding interferes with mRNA binding and tRNA acceptor sites leading to the production of non-functional or toxic peptides. Other mechanisms not fully understood may confer the bactericidal effects of amikacin. Amikacin is also nephrotoxic and ototoxic. Amikacin is useful against gentamicin-resistant gram-negative bacilli and also in the treatment of infections caused by susceptible Nocardia and nontuberculous mycobacteria.[1].
Astromicin (KW-1070) is a water-soluble aminoglycoside antibiotic that can be isolated from the genus Micromonospora. Astromicin exhibits broad spectrum antibacterial activity against gram positive and negative bacteria[1][2][3].
Cefepime Dihydrochloride Monohydrate is a broad-spectrum cephalosporin with enhanced coverage against Gram-positive and Gram-negative bacteria.Target: AntibacterialCefepime is an extended-spectrum parenteral cephalosporin antibiotic active in vitro against a broad spectrum of gram-positive and gram-negative aerobic bacteria. Cefepime dosing was 1-4 g/day (0.5-2.0 g twice daily) for adults; ceftazidime dosing was 1-6 g/day (0.5 g every 12 hours to 2.0 g every 8 hours). A limited number of cefepime-treated patients received 2 g every 8 hours. The median length of dosing for both cefepime and ceftazidime was 7 days [1]. Cefepime has a decreased propensity to induce beta-lactamases compared with other beta-lactam antibiotics. Cefepime has a pharmacokinetic disposition similar to that of other renally eliminated cephalosporins, with a half-life of approximately 2 hours. Cefepime has demonstrated clinical efficacy against a variety of infections, including urinary tract infections, pneumonia, and skin and skin structure infections. Cefepime is generally well tolerated [2].
Gentamicin C1a is the precursor of the semi-synthetic antibiotic Etimicin, and has antibacterial activity. Gentamicin C1a is the major component of the Gentamicin complex[1][2].
Azithromycin is a macrolide antibiotic useful for the treatment of a number of bacterial infections.
Temporin L is a potent antimicrobial peptide and is active against Gram-negative bacteria and yeast strains. Temporin L also has antiendotoxin properties[1][2].
Antibacterial agent 83 (compound 17h) displays potent antibacterial activity against various vancomycin-resistant Enterococcus faecalis (VRE) and methicillin-resistant Staphylococcus aureus (MRSA). Antibacterial agent 83 can significantly reduce the biofilm formation of MRSA and exhibited promising selectivity. Antibacterial agent 83 is metabolically stable in human liver microsomes[1].
Antibiotic A-338533, an antibiotic, can be isolated from Streptomyces strain. Antibiotic A-338533 has anti-bacterial activity against Staphylococcus aureus, Mycoplasma gallisepticum with MIC values of 2 μg/mL and ≤1.56 μg/mL, respectively[1].
Cefamandole Sodium Salt is a second-generation broad-spectrum cephalosporin antibiotic.
Antibacterial agent 160 is a potent antibacterial agents. Antibacterial agent 160 can rapidly kill bacterial and inhibits bacterial biofilm formation. Antibacterial agent 160 affects the normal function of DNA and leads cell death[1].
Peptide 5e is an antimicrobial peptide. Peptide 5e inhibits E. coli, S. aureus, and C. albicans with MIC values of 30, 5, 25 μg/mL respectively[1].
Sulfadimethoxypyrimidine D4 is a deuterium labeled Sulfadimethoxypyrimidine. Sulfadimethoxypyrimidine is a sulfonamide antibiotic with a broad-spectrum antibacterial effect[1].
Hexetidine is an anti-bacterial and anti-fungal agent commonly used in both veterinary and human medicine, is a local anesthetic.
Cefalexin hydrochloride is a cephalosporin antibiotic.Target: AntibacterialCefalexin (INN, BAN) or cephalexin (USAN, AAN) is a first-generation cephalosporin antibiotic introduced in 1967 by Eli Lilly and Company. It is an orally administered agent with a similar antimicrobial spectrum to the intravenous agents cefalotin and cefazolin. It was first marketed as Keflex (Lilly), and is marketed under several other trade names. As of 2008, cefalexin was the most popular cephalosporin antibiotic in the United States, with more than 25 million prescriptions of its generic versions alone, for US$255 million in sales (though less popular than two other antibiotics, amoxicillin and azithromycin, each with 50 million prescriptions per year).Cefalexin is marketed by generic pharmaceutical manufacturers under a wide range of brand names, including: Apo-Cephalex, Biocef, Cefanox, Ceforal, Cephabos, Cephalexin, Cephorum, Ceporex, Cilex, Ialex, Ibilex, Kefexin, Keflet, Keflex, Rekosporin, Keforal, Keftab, Keftal, Lopilexin, Larixin, Novo-Lexin, Ospexin, Tenkorex, Zephalexin, Panixine Disperdose, Rancef, Sialexin, Sporidex and Ulexin. A version of Keflex 750 mg capsules is marketed for twice-daily dosage, to improve compliance. However, it is not a sustained release formulation, and since it is more expensive than the older strengths, some physicians prescribe three 250 mg capsules to be taken twice daily, as a less expensive alternative.
(±)-Leucine-d7 is the deuterium labeled (±)-Leucine. (±)-Leucine (DL-Leucine), an isomer of Leucine, chemosterilant and dietary additive. (±)-Leucine inhibits growth of Escherichia coli HfrH by 92.08%[1].
Squalamine lactate is an aminosterol compound discovered in the tissues of the dogfish shark, with antimicrobial activity, and used for the treatment of neovascular age-related macular degeneration.
Cefalonium 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].
Eugenol is an essential oil found in cloves with antibacterial, anthelmintic and antioxidant activity. Eugenol is shown to inhibit lipid peroxidation.
Gageotetrin B has antimicrobial activities. Gageotetrin B is more active against fungi compared to bacteria with MIC values of 0.01-0.04 μM[1].
Omadacycline mesylate is a new tetracycline antibiotic in the pipeline, which can inhibit the 30s subunit of bacterial ribosome.IC50 Value: N/ATarget: Antibacterialin vitro: in vivo: Clinical trial: Phase III Study to Compare the Safety and Efficacy of PTK-0796 in Patients With Complicated Skin and Skin Structure Infection (CSSSI).
Tizoxanide D4 (TIZ D4) is the deuterium labeled Tizoxanide. Tizoxanide is the active metabolite of Nitazoxanide, which is a thiazolide anti-infective compound against anaerobic bacteria, protozoa, and a range of viruses. Tizoxanide has anti-HIV-1 activities[1][2].
(+)-Medioresinol is a furofuran type lignan with antifungal, antibacterial and lesishmanicidal activities. (+)-Medioresinol leads to intracellular ROS accumulation and mitochondria-mediated apoptotic cell death in Candida albicans. (+)-Medioresinol can reduce the cardiovascular disease risk[1][2].
Omadacycline-d9 is a deuterated aminomethylcycline omadacycline (HY-14865). Omadacycline is an orally active antibacterial agent and tetracycline antibiotic. Omadacycline binds to the 30S ribosomal subunit to inhibit bacterial protein synthesis. Omadacycline tosylate is indicated for the study of acute bacterial skin and skin structure infections, infectious pneumonia and urinary tract infections.
1-Methoxyphaseollidin, a flavonoid compound, is a lysoPAF acetyltransferase inhibitor, with an IC50 of 48 μM. 1-Methoxyphaseollidin exhibits anti-H.pylori activity against the CLAR and AMOX-resistant strain as well as four CLAR (AMOX)-sensitive strains[1][2][3].
AM-8191, a bacterial topoisomerase inhibitors, has broad-spectrum antibacterial activity.