Thymol-d13 is the deuterium labeled Thymol[1]. Thymol is the main monoterpene phenol occurring in essential oils isolated from plants belonging to the Lamiaceae family, and other plants such as those belonging to the Verbenaceae, Scrophulariaceae, Ranunculaceae and Apiaceae families. Thymol has antioxidant, anti-inflammatory, antibacterial and antifungal effects[2].
N-Decyl-N,N-dimethyldecan-1-aminium chloride (Didecyldimethylammonium chloride) is a dialkyl-quaternary ammonium compound that is used in numerous products for its bactericidal, virucidal and fungicidal properties[1].
Antibacterial agent 106 (compound 8) is an orally active and potent antibacterial agent with antibiofilm activity. Antibacterial agent 106 shows potent antibacterial effect against multi-drug resistant (MDR)-Gram positive pathogens. Antibacterial agent 106 is highly effective in clearing 99.7% of the intracellular methicillin-resistant S. aureus (MRSA) harbored inside macrophages[1].
HadAB-IN-1 is a potent HadAB inhibitor. HadAB-IN-1 inhibits HadAB enzyme complexes activity with an IC50 value of 0.03 μM. HadAB-IN-1 also affects mycolic acid biosynthesis in Mycobacterium tuberculosis (Mtb). HadAB-IN-1 can be used for the research of tuberculosis (TB)[1].
Methyl gallate is a plant phenolic with antioxidant, anticancer, and anti-inflammatory activities. Methyl gallate also shows bacterial inhibition activity.
S-Pantoprazole (sodium trihydrate) is related to Pantoprazole (HY-17507) that plays an important roles in gastric acid secretion disorder-related diseases, or as proton pump inhibitor[1].
WU-FA-01, a hydrogenated derivative of WU-FA-00, is an antibacterial agent that exhibits high levels of antibacterial activity against Gram-positive strains and also has some anti-inflammatory activity[1].
Atuzaginstat (COR388) is an effective small-molecule bacterial protease lysine gingipain inhibitor and can be used for the research of Alzheimer's disease[1][2].
TAPI-0 is a TACE (TNF-α converting enzyme; ADAM17) inhibitor with an IC50 of 100 nM. TAPI-0 is a MMP inhibitor and also attenuates TNF-α processing[1][2].
Ro 20-0657/000 is a metabolite of Trimethoprim. Trimethoprim is a dihydrofolate reductase inhibitor, used as an antibacterial agent in human and veterinary medicine[1][2][3].
GlyRS-IN-1 is a glycyl-tRNA synthase (GlyRS) inhibitor extracted from patent WO 2017066459 A1. GlyRS-IN-1 can also inhibit the growth of bacteria.
Terbinafine lactate (TDT 067 lactate) is an orally active and potent antifungal agent. Terbinafine lactate is a potent non-competitive inhibitor of squalene epoxidase from Candida, with a Ki of 30 nM. Terbinafine lactate also shows antibacterial activity against certain Gram-positive and Gram-negative bacteria[1][2][3].
Kanamycins sulfate is a broad-spectrum antibiotic, can be used in certain severe staphylococcal or Gram-negative bacillary infections. Kanamycin sulfate has certain ototoxicity[1][2].
Colistin methanesulfonate sodium salt exhibits MIC values ranged from 4 to 16 mg/liter against susceptible strains (P. aeruginosa)[1].
HSGN-94 is a potent antimicrobial agent with lipoteichoic acid (LTA) biosynthesis inhibition. HSGN-94 inhibits drug-resistant Gram-positive bacteria with MIC values of 0.25-2 μg/mL. HSGN-94 inhibits biofilm formation of MRSA and Vancomycin-resistant Enterococci. HSGN-94 also inhibits pro-inflammatory cytokines, exhibits in vivo efficacy in an MRSA murine wound infection model[1].
Idarubicin is an orally active and potent anthracycline antileukemic agent. Idarubicin inhibits the topoisomerase II interfering with the replication of DNA and RNA transcription. Idarubicin shows induction of DNA damage. Idarubicin inhibits DNA synthesis and of c-myc expression. Idarubicin inhibits the growth of bacteria and yeasts[1][2][3][4][5].
Clofazimine is a fat-soluble iminophenazine dye, has a marked anti-inflammatory effect, has been used in combination with other antimycobacterial drugs to treat AIDS and Crohn's disease.
Tulathromycin A is a macrolide antibiotic.IC50 Value: 1 microg/ml (MIC90 for Pasteurella multocida) [2]Target: Antibacterialin vitro: Two highly pathogenic strains of M. bovis (with minimum inhibitory concentration values for tulathromycin of 1 and >64 microg/ml) were inoculated into 145 calves. Four days after inoculation, calves with clinical BRD were treated subcutaneously with saline or tulathromycin (2.5 mg/kg). Compared with saline, BRD-related withdrawals, peak rectal temperatures, and lung lesion scores were significantly lower for tulathromycin-treated calves (P < .01). Tulathromycin was highly effective in the treatment of BRD due to M. bovis in calves regardless of the minimum inhibitory concentration of the challenge strain (1 or >64 microg/ml) [1]. The lowest concentrations inhibiting the growth of 90% of isolates (MIC90) for tulathromycin were 2 microg/ml for Mannheimia (Pasteurella) haemolytica, 1 microg/ml for Pasteurella multocida (bovine), and 2 microg/ml for Pasteurella multocida (porcine) and ranged from 0.5 to 4 microg/ml for Histophilus somni (Haemophilus somnus) and from 4 to 16 microg/ml for Actinobacillus pleuropneumoniae [2]. in vivo: Each study randomly allocated 250 calves to receivetulathromycin at 2.5 mg/kg and 250 calves to receive either tilmicosin at 10 mg/kg (Colorado site) or florfenicol at 40 mg/kg (Idaho and Texas sites) on arrival at the feedlot. Calves were housed by treatment group in pens with 50 calves/pen [3]. The treatment groups were physiologic saline (n = 160) given SC at 0.02 ml/kg, tulathromycin (n = 320) given SC at 2.5 mg/kg, and tilmicosin (n = 320) given SC at 10 mg/kg [4].Tulathromycin is a triamilide antimicrobial that has been approved for use in the treatment and prevention of bovine respiratory disease and the treatment of swine respiratory disease. Toxicity: No adverse events related to tulathromycin were reported [4].Clinical trial:
Tylosin Tartrate is an antibiotic with a large macrocyclic lactone ring.Target: AntibacterialTylosin is a bacteriostat food additive used in veterinary medicine. It has a broad spectrum of activity against gram-positive organisms and a limited range of gram-negative organisms. There is no significant evidence that tylosin resistant staphylococci of animal origin have endangered human health. Tylosin is not effective against the gram-negative intestinal flora, which thus does not lead to selection of R-factors by conjugation. From the human medical stand point, there is no reason that precludes the use of tylosin as a fee additive in animal feeds [1]. Minimum inhibitory concentrations for tylosin tartrate and other commonly used antibiotics were determined for 103 isolates. Most (82.61%) of the isolates not exposed to antibiotics in the 3 months before submission were sensitive to tylosin tartrate. These findings suggest that tylosin tartrate warrants further study as a first-line option for the treatment of dogs initially presenting with pyoderma [2].
Antibacterial agent 30 demonstrates excellent in vitro activity against Xoo with EC50 value of 1.9 μg/mL.
Cefdinir (Omnicef) is a semi-synthetic, broad-spectrum antibiotic, which is proved to be effective for common bacterial infections of the ear, sinus, throat, and skin.Target: AntibacterialCefdinir is a third generation oral cephalosporin antibiotic. Cefdinir (Omnicef) is a semi-synthetic, broad-spectrum antibiotic in the third generation of the cephalosporin class, which is proved to be effective for common bacterial infections of the ear, sinus, throat, and skin. It can be used to treat infections caused by several Gram-negative and Gram-positive bacteria. It is available in US as Omnicef by Abbott Laboratories and in India as Cednir by Abbott, Kefnir by Glenmark and Cefdiel by Ranbaxy. As of 2008, cefdinir was the highest-selling cephalosporin antibiotic in the United States, with more than US$585 million in retail sales of its generic versions alone.Cefdinir, a new oral 2-amino-5-thiazolyl cephalosporin, inhibited the luminol-amplified chemiluminescence (LACL) response of human neutrophils stimulated by PMA but not opsonized zymosan, in a concentration-dependent but not time-dependent manner. The LACL response to opsonized zymosan in cytochalasin B-treated neutrophils was, however, inhibited by cefdinir. Furthermore, cefdinir inhibited LACL generation in cell-free systems consisting of H2O2, NaI, and either horseradish peroxidase or a myeloperoxidase-containing neutrophil extract. Orthodianisidine oxidation in these two acellular systems was inhibited by cefdinir.
Maximin 8 is a antimicrobial peptide that can be found in B. maxima[1].
Norbatzelladine L (Compound 2) is an inhibitor of the catalytic and functional activity of Pdr5p transporter. Norbatzelladine L inhibits Pdr5p ATPase activity with an IC50 of 3.8 µM. Norbatzelladine L shows antifungal, antiparasitic, antiviral, antibacterial and antitumoral activities[1].
Pinobanksin 5-methyl ether can be isolated from Georgian Propolises. Pinobanksin 5-methyl ether has anti-helicobacter activity. Pinobanksin 5-methyl ether is effective inducer of CYP9Q enzyme[1].
Methicillin is a β-lactam antibiotic which acts by inhibiting penicillin-binding proteins that are involved in the synthesis of peptidoglycan.
Brevianamide M (compound 4) is a metabolite of Aspergillus versicolor. This is an endophytic fungus isolated from the marine brown alga Sargassum. Brevianamide M has antimicrobial activity against Escherichia coli and Staphylococcus aureus[1].
Nifurpirinol (P-7138) is a nitroaromatic antibiotic and acts as a novel substrate for the bacterial nitroreductase (NTR) enzyme. Nifurpirinol is a more potent prodrug compared to Metronidazole to trigger cell-ablation in nitroreductase expressing transgenic models[1].
Lugdunin is an antibiotic peptide. Lugdunin inhibits bacteria by dissipating their membrane potential. Lugdunin is active against Gram-positive bacteria, such as S. aureus, and reduces S. aureus skin and nasal colonization. Lugdunin induces LL-37 and CXCL8/MIP-2 in human keratinocytes and mouse skin[1].
Grepafloxacin (OPC-17116) hydrochloride is an oral actively fluoroquinolone antibiotic with potent activity against community-acquired respiratory pathogens including Streptococcus pneumonia. Grepafloxacin hydrochloride has high tissue penetration and a promising pharmacodynamic profile[1][2][3][4].
Kushenol W is a prenylated flavonoid that can be isolated from the root of Sophora flavescens. Kushenol W has antimicrobial effect, with a MIC of 10 μg/mL for Staphylococcus aureus[1].