3α-Akebonoic acid is a α-glucosidase inhibitor with an IC50 value of 0.035 mM. 3α-Akebonoic acid shows antibacterial activity and cytotoxicity[1].
Antitubercular agent-19 (Compound 1c) is an antitubercular agent. Antitubercular agent-19 shows excellent activity against MTB H37Rv and MDR-MTB strains (MIC: ＜0.016 µg/ml). Antitubercular agent-19 shows low cytotoxicity and relatively high acute lethal toxicity in BALB/c mice[1].
Albofungin (Antibiotic P-42-1) is isolated from the culture filtrate of Actinomyces tumemacerans strain INMI.P-42. Albofungin shows highly active on a wide variety of gram-positive bacteria and fungi. Albofungin shows cytotoxic to HeLa cell cultures and exhibited antitumor activity on EHRLICH ascites tumor in mice.
Licoflavonol, a minor flavone from the roots of Glycyrrhiza uralensis, is an inhibitor of the Salmonella type III secretion system (T3SS)[1][2].
GVLSNVIGYLKKLGTGALNAVLKQ is an antimicrobial peptide with 24-amino acid. GVLSNVIGYLKKLGTGALNAVLKQ can potentially form α-helix. GVLSNVIGYLKKLGTGALNAVLKQ (PGQ) has activity against Gram-negative, Gram-positive bacteria and the yeast Candida albicans[1].
Cilastatin-15N,d3 is a 15N-labeled and deuterium labeled Cilastatin (MK0791) is a reversible, competitive renal dehydropeptidase I inhibitor with an IC50 of 0.1 μM. Cilastatin inhibits the bacterial metallob-lactamase enzyme CphA with an IC50 of 178 μM. Cilastatin is an antibacterial adjunct[1][2][3].
Aditoprime (Aditoprim), a selective bacterial dihydrofolate reductase (DHFR) inhibitor, inhibits the transformation of dihydrofolic acid to tetrahydrofolic acid. Aditoprime inhibits E.coli and L.casei DHFR with IC50 of 47 and 520 nM, respectively. Aditoprime has a broad antimicrobial spectrum, good antibacterial activity and excellent pharmacokinetics[1][2][3].
Lasalocid is an antibacterial agent and a coccidiostat, used in the feed additives
Ertapenem sodium is a new long-acting 1-β-methyl carbapenem antibiotic with a broad antibacterial spectrum including common aerobic and anaerobic bacteria and organisms with extended-spectrum β-lactamases.
Chrysomycin A (Chr-A), an antibiotic, can be obtained from Streptomyces. Chrysomycin A exhibits antitumor and anti-tuberculous and MRSA activities. As for glioblastoma, Chrysomycin A inhibits the proliferation, migration, and invasion of cancer cells through the Akt/GSK-3β/β-catenin signaling pathway[1].
8-Hydroxy-9,10-diisobutyryloxythymol is a natural monoterpenoid with antibacterial properties. 8-Hydroxy-9,10-diisobutyryloxythymol against S. aureus, S. flexneri, and S. paratyphi-B with MIC values of 6.25 μg/mL[1].
Ampicillin sodium is a broad-spectrum beta-lactam antibiotic against a variety of gram-positive and gram-negative bacteria.
Levopimaric acid is a type of diterpene resin acid produced by plants. Levopimaric acid induces cancer cell apoptosis and has anticancer, antioxidant, antibacterial and cardiovascular activities[1].
GSK2556286 (GSK286) is an orally active inhibitor of M. tuberculosis. GSK2556286 inhibits growth within human macrophages (IC50 = 0.07 μM). GSK2556286 is effective against both multidrug-resistant (MDR) or extensively drug-resistant (XDR) and drug-sensitive (DS) M. tuberculosis[1].
Aurantimycin A (Adipogen), a depsipeptide antibiotic, displays strong activity against Gram-positive bacteria. Aurantimycin A is a substrate of the LieAB transporter[1][2].
Cefpodoxime Proxetil is a first oral and broad spectrum antibiotic that belongs to the third generation of cephalosporin. Cefpodoxime Proxetil binds to penicillin binding proteins (PBPs), which inhibits peptidoglycan synthesis, finally results in interfering bacterial cell wall biosynthesis[1].
Methyl gallate is a plant phenolic with antioxidant, anticancer, and anti-inflammatory activities. Methyl gallate also shows bacterial inhibition activity.
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].
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].
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].
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].
Cefprozil Monohydrate (Cefzil) is a second-generation cephalosporin type antibiotic.Target: AntibacterialCefprozil, sometimes spelled cefproxil and marketed under the trade name Cefzil, is a second-generation cephalosporin type antibiotic. In Europe it is marketed using the trade names Procef and Cronocef. It can be used to treat bronchitis, ear infections, skin infections, and other bacterial infections. It comes as a tablet and as a liquid suspension. From Wikipedia.
Pz-Pro-Leu-Gly-Pro-d-Arg is a synthetic substrate of bacterial collagenase. Pz-Pro-Leu-Gly-Pro-d-Arg can be used to test bacterial collagenase activity[1].
Ofloxacin is a fluoroquinolone whose primary mechanism of action is inhibition of bacterial DNA gyrase.Target: DNA gyrase Ofloxacin is a fluoroquinolone whose primary mechanism of action is inhibition of bacterial DNA gyrase. In vitro it has a broad spectrum of activity against aerobic Gram-negative and Gram-positive bacteria, although it is poorly active against anaerobes [1]. Ofloxacin, like other 4-quinolones, is unusual among front line drugs available to treat bacterial infections since it affects bacterial DNA synthesis, rather than cell wall or protein synthesis [2].Ofloxacin (20 mg/kg), norfloxacin (40 mg/kg), pefloxacin mesylate dihydrate (40 mg/kg)and ciprofloxacin (50 mg/kg) were administered by gavage twice daily for three consecutive weeks. 6 weeks after treatment, the test animals were euthanised and Achilles tendon specimens were collected. A computer monitored tensile testing machine was utilised for biomechanical testing. The mean elastic modulus of the control group was significantly higher than that of the norfloxacin and pefloxacin groups (p<0.05 and p<0.01, respectively). The mean yield force (YF) of the control group was significantly higher than those of ciprofloxacin, norfloxacin and pefloxacin groups (p<0.001, p<0.05 and p<0.01, respectively). The mean ultimate tensile force (UTF) of the control group was significantly higher than of the ciprofloxacin, norfloxacin, and pefloxacin groups (p<0.001, p<0.05 and p<0.01, respectively). Hyaline degeneration and fibre disarrangement were observed in the tendons of the ciprofloxacin, pefloxacin, and ofloxacin treated-groups, whereas myxomatous degeneration was observed only in the ciprofloxacin and pefloxacin groups [3].Clinical indications: Bacterial infection; Bacterial respiratory tract infection; Bacterial urinary tract infection Toxicity: tendinopathy; hepatotoxicity; dysglycemia
Astodrimer (SPL7013 free base) is a large (3-4 nm, ~ 16.5 kDa), negatively charged, highly-branched dendrimer, is a potent virucidal agent. Astodrimer shows antiviral and virucidal activity against a broad spectrum of viruses, including SARS-CoV-2, HIV-1, HSV-1, HSV-2, HPV. Astodrimer also has antibacterial properties[1][2][3].
Diethyl butylmalonate-d9 is the deuterium labeled Diethyl butylmalonate[1]. Diethyl butylmalonate exhibits toxicity to T. pyriformis, with a log(IGC50-1) of 0.557[2].
Benzoic Acid is an aromatic alcohol existing naturally in many plants and is a common additive to food, drinks, cosmetics and other products. It acts as preservatives through inhibiting both bacteria and fungi.
Anti-inflammatory agent 15 (compound 29) is a potent antimycobacterial and anti-inflammatory agent. Anti-inflammatory agent 15 inhibits Mtb H37Rv and M299 growth, with MIC50 (minimum inhibitory concentration 50%) of 2.3 and 7.8 μM, respectively. Anti-inflammatory agent 15 inhibits NO through the suppression of iNOS expression, and also inhibited the production of TNF-α and IL-1β. Anti-inflammatory agent 15 can be used for tuberculosis (TB) research[1].
Clindamycin-13C,d3 is the 13C- and deuterium labeled. 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].
A201A is a aminoacylnucleoside antibiotic with antibacterial activities. A201A is highly effective against Gram-positive and most Gram-negative anaerobic bacteria. A201A inhibits tRNA accommodation during translation[1][2].