Gemifloxacin, a fluoroquinolone, is a potent and orally active antipneumococcal agent. Gemifloxacin shows bactericidal activity against highly quinolone-resistant pneumococci.Gemifloxacin can be used for the research of respiratory infections, such as community-acquired pneumonia (CAP) and acute exacerbation of chronic bronchitis (AECB)[1][2].
Aztreonam-d6 is deuterium labeled Aztreonam. Aztreonam (SQ-26,776) is a synthetic monocyclic beta-lactam antibiotic, which has a very high affinity for penicillin-binding protein 3 (PBP-3).
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.
Quinocetone is a potent synthetic antimicrobial agent that is used for improving the feed efficiency and controlling dysentery in food-producing animals[1].
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
LpxH-IN-AZ1, a sulfonyl piperazine compound, is a potent UDP-2,3-diacylglucosamine pyrophosphate hydrolase LpxH inhibitor. LpxH-IN-AZ1 is a potent inhibitor of Klebsiella pneumoniae LpxH with IC50 of 0.36 μM [1].
Ethylhydrocupreine (Optochin) is a quinine derivate with antimicrobial activity against S. pneumoniae. Ethylhydrocupreine also possesses antimalarial activity against Plasmodium falciparum, with an IC50 of 25.75 nM. Ethylhydrocupreine is a Gallus gallus taste 2 receptors (ggTas2r1, ggTas2r2 and ggTas2r7) agonist[1][2][3][4].
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].
Antibacterial agent 61 (example 27) is a antibacterial agent (extracted from patent WO2013030735A1)[1].
Cyclo(Phe-Gly) is a cyclodipeptides with antimicrobial and anticancer activities, isolated from broth culture of endophytic Streptomyces YIM 64018 associated with Paraboea sinensis[1].
Tet-20 is a biological active peptide. (Tet-20, is a synthetic cathelicidin-derived peptide. It was tested as infection-resistant coating for medical devices. When tethered on an implant surface Tet-20 exhibited broad antimicrobial activities both in vivo and in vitro. It can stop biofilm formation and appears to be non-toxic to eukaryotic cells)
Effusanin A is a natural product that can be found in Isodon rugosus. Effusanin A exhibits DNA-damaging and antibacterial activities[1].
Nifursol is a nitrofuran antibiotic which inhibits the growth of Histomonas meleagridis but is not lethal to the flagellated protozoan. Target: AntibacterialNifursol can be analyzed and detected in tissues using intact 3,5-dinitrosalicylic acid hydrazide side chains along with electron-capture GC, spectrophotometric detection, and HPLC with ultraviolet light detection. In tissues, it has been observed that Nifursol is tightly bound to proteins and requires basic solutions such as ammonia to break the bonds between the two.
Antibacterial agent 35, an antibacterial agent, significantly lowers MIC value of antibacterial agent Ceftazidime[1].
Methyl anthranilate, a plant spice extract, is a quorum sensing inhibitor and anti-biofilm agent against Aeromonas sobria. Methyl anthranilate has been widely employed for the preparation of edible flavor and food additives in food processing industries[1].
Mafenide is a sulfonamide-type medication.Target: AntibacterialMafenide is a sulfonamide-type medication. Mafenide works by reducing the bacterial population present in the avascular tissues of burns and permits spontaneous healing of deep partial-thickness burns. It is used to treat severe burns. It is used topically as an adjunctive therapy for second- and third-degree burns. It is bacteriostatic against many gram-positive and gram-negative organisms, including Pseudomonas aeruginosa. Some sources state that mafenide is more appropriate for non-facial burns, while chloramphenicol/prednisolone or bacitracin are more appropriate for facial burns [1-3].
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].
Nitrofural is a bactericidal compound used as an antibiotic most commonly in the form of ointments.Target: AntibacterialNitrofurazone, a nitroaromatic drug, is a broad spectrum antibiotic which has until now been considered as activated in bacteria by nitroreductases. Its use in medicine has become less frequent as safer and more effective products have become available, and it has been discontinued in the US.Nitrofurazone (NF) and its derivative, hydroxymethylnitrofurazone (NFOH), have presented antichagasic activity. In vitro cruzain inhibition tests were performed for both compounds, and the 50% inhibitory concentration (IC50) for NF and NFOH presented values of 22.83 ± 1.2 μM and 10.55 ± 0.81 μM, respectively. AM1 semi-empirical molecular modeling studies were performed to understand the activity of the compounds, corroborating the observed cruzain inhibitory activity.
(R)-Eucomol, a flavonoid derivative, displays marginal antibacterial activity. (R)-Eucomol shows cytotoxic activity against KB and P-388 cells[1].
Omiganan is a cationic antimicrobial peptide. Omiganan as an analogue of indolicidin shows activity against gram-positive and gram-negative bacteria but also Candida spp. isolates. Omiganan can be used for the research of alcohol nose and acne[1][2].
Helvolic acid (Fumigacin) is an antibiotic isolated from Xylaria sp, active against the Gram-positive bacteria[1].
Antimycobacterial agent-4 is a 2-amino-4-(2-pyridyl) thiazole derivative, with antimycobacterial activity, antiplasmodial activity, and cytotoxicity on a mammalian cell line[1][2].
CRAMP-18 (mouse) is an antibiotic peptide without hemolytic activity. CRAMP-18 (mouse) has good inhibitory activity against Gram-negative bacteria, such as S. typhimurium and P. aeruginosa. CRAMP-18 (mouse) has the potential to study antifungal, antibacterial and antitumor[1][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].
Sulfanitran is a sulfonamide antiinfective drug.
Sultamicillin is an orally active double prodrug of Ampicillin/Sulbactan. Sulbactam is a semisynthetic beta-lactamase inhibitor which, in combination with Ampicillin, extends the antibacterial activity of the latter to include some beta-lactamase-producing strains of bacteria that would otherwise be resistant[1].
3-Chlorogentisyl alcohol is a potent E. coli β-glucuronidase inhibitor with an IC50 value of 0.74 µM, an Ki value of 0.58 µM. 3-Chlorogentisyl alcohol shows antiproliferative activity. 3-Chlorogentisyl alcohol has the potential for the research of anti-cancer and anti-inflammatory therapies[1].