Antibacterial agent 111 (Compound 3) is an antibacterial agent with MIC values of 3.90 μg/mL and 0.49 μg/mL against B. cereus and K. pneumonia, respectively. Antibacterial agent 111 firmly binds with tyrosyl-tRNA synthetase residues[1].
Pefloxacin mesylate is a an antibacterial agent and prevents bacterial DNA replication by inhibiting DNA gyrase (topoisomerse)Target: DNA gyrasePefloxacin is a synthetic chemotherapeutic agent used to treat severe and life-threatening bacterial infections. Pefloxacin is commonly referred to as afluoroquinolone (or quinolone) drug and is a member of the fluoroquinolone class of antibacterials. It is an analog of norfloxacin. It is a synthetic fluoroquinolone, belonging to the 3rd generation of quinolones. Pefloxacin is extensively prescribed in France. Pefloxacin has not been approved for use in the United States.The bactericidal action of pefloxacin results from interference with the activity of the bacterial enzymes DNA gyrase and topoisomerase IV, which are needed for the transcription and replication of bacterial DNA. DNA gyrase appears to be the primary quinolone target for gram-negative bacteria. Topoisomerase IV appears to be the preferential target in gram-positive organisms. Interference with these two topoisomerases results in strand breakage of the bacterial chromosome, supercoiling, and resealing. As a result DNA replication and transcription is inhibited.
Granilin, a sesquiterpene lactone, can be found in the flower buds of Carpesium triste. Granilin can be used as the bactericide and fungicide[1].
MurA-IN-2 (compound 37), a chloroacetamide fragment containing a primary aliphatic amine, is a potent MurA inhibitor with an IC50 value of 39 μM. MurA-IN-2 has antibacterial activity and inhibits the bacterial cell wall synthesis[1].
Golotimod (SCV-07), an immunomodulating peptide with antimicrobial activity, significantly increases the efficacy of antituberculosis therapy, stimulates thymic and splenic cell proliferation, and improves macrophage function. Golotimod (SCV-07) inhibits STAT3 signaling and modulates the duration and severity of oral mucositis in animal models that received radiation or a combination of radiation and Cisplatin. Golotimod (SCV-07) is a potential therapeutic for recurrent genital herpes simplex virus type 2 (HSV-2)[1][2][3].
Mab Aspartate Decarboxylase-IN-1 is a potent aspartate decarboxylase (PanD) inhibitor with an IC50 value of 56.3 µM. Mab Aspartate Decarboxylase-IN-1 shows antibacterial activity[1].
Apigravin is a potent antibacterial agent. Apigravin shows antibacterial activity against Bacillus subtilis with a MIC value of 61 μM[1].
MGB-BP-3 is an antibiotic that has been shown to be active against a broad range of important multi-resistant Gram-positive pathogens.
Rosuvastatin Calcium is a competitive inhibitor of HMG-CoA reductase with IC50 of 11 nM. IC50 Value: 11 nM [1]Target: HMG-CoA reductasein vitro: Rosuvastatin is relatively hydrophilic and is highly selective for hepatic cells; its uptake is mediated by the liver-specific organic anion transporter OATP-C. Rosuvastatin is a high-affinity substrate for OATP-C with apparent association constant of 8.5 μM [2]. Rosuvastatin inhibits cholesterol biosynthesis in rat liver isolated hepatocytes with IC50 of 1.12 nM. Rosuvastatin causes approximately 10 times greater increase of mRNA of LDL receptors than pravastatin [1]. Rosuvastatin (100 μM) decreases the extent of U937 adhesion to TNF-α-stimulated HUVEC. Rosuvastatin inhibits the expressions of ICAM-1, MCP-1, IL-8, IL-6, and COX-2 mRNA and protein levels through inhibition of c-Jun N-terminal kinase and nuclear factor-kB in endothelial cells [3].in vivo: Rosuvastatin (3 mg/kg) daily administration for 14 days decreases plasma cholesterol levels by 26% in male beagle dogs with normal cholesterol levels. In cynomolgus monkeys, Rosuvastatin decreases plasma cholesterol levels by 22% [1]. Rosuvastatin (20 mg/kg/day) administration for 2 weeks, significantly reduces very low-density lipoproteins (VLDL) in diabetes mellitus rats induced by Streptozocin [4]. Rosuvastatin shows antiatherothromhotic effects in vivo. Rosuvastatin (1.25 mg/kg) significantly inhibits thrombin-induced transmigration of monocvtes across mesenteric venules via inhibition of the endothelial cell surface expression of P-selectin, and increases the basal rate of nitric oxide in aortic segments by 2-fold times [5].
Sulfamonomethoxine-13C6 is the 13C6 labeled Sulfamonomethoxine. Sulfamonomethoxine is a long acting sulfonamide antibacterial agent, used in blood kinetic studies,and blocks the synthesis of folic acid by inhibiting synthetase of dihydropteroate.
Mosloflavone is a flavonoid isolated from Scutellaria baicalensis Georgi with anti-EV71 activity. Mosloflavone inhibits VP2 virus replication and protein expression during the initial stage of virus infection and inhibits viral VP2 capsid protein synthesis. Mosloflavone is a promising biocide and inhibits P. aeruginosa virulence and biofilm formation.
Phenoxyethanol-d4 is the deuterium labeled Phenoxyethanol[1]. Phenoxyethanol has a broad spectrum of antimicrobial activity against various gram-negative and gram-positive bacteria. Phenoxyethanol is an uncouple agent in oxidative phosphorylation from respiration and competitively inhibits malate dehydrogenase. Phenoxyethanol is used as a preservative in cosmetic, vaccine, and textile, et al[2].
Syringic acid-d6 is the deuterium labeled Syringic acid[1]. Syringic acid is correlated with high antioxidant activity and inhibition of LDL oxidation[2][3].
Xinjiachalcone A is an active principle of Glycyrrhiza inflata Batalin. Xinjiachalcone A shows both a low MIC and a strong bactericidal activity against H. pylori, with MIC values ranged from 12.5 to 50 µM for seventeen H. pylori strains[1].
Isomagnolol is a lignan with antimicrobial activity. Isomagnolol can be isolated from the root of tea plant[1].
Tomopenem (CS-023; RO4908463; R-115685) is a longer-half-life parenteral carbapenem. Tomopenem shows broad activity against 63 reference species. The activity of tomopenem against 293 clinical isolates is potent (MIC90, 0.06 to 4 μg/mL). Antianaerobic activity[1].
Nemonoxacin (TG-873870) is an orally active and potent broad-spectrum antibiotic. Nemonoxacin shows good inhibitory activity against different species of staphylococci, streptococci, and enterococci, Neisseria gonorrhoeae, and Haemophilus influenza. Nemonoxacin can be used in the study of bacterial infections and community-acquired pneumonia[1][2][3].
Cefquinome sulfate is a cephem antibiotic, which inhibits members of the Enterobacteriaceae[1].
DuP 105 is an orally active oxazolidinone, a new class of synthetic antimicrobial agent with activity against gram-positive bacteria.
trans-Clopenthixol ((E)-Clopenthixol) dihydrochloride is an antibiotic agent, without neuroleptic effect. trans-Clopenthixol can be used to inhibit Pseudomonas aeruginosa and Plasmodium falciparum in vitro[1][2].
4-Aminosalicylic acid hemicalcium is an orally active antibiotic and has the potential for tuberculosis research[1].
Gamithromycin is an antimicrobial agent which can inhibit the growth of MmmSC strains B237 and Tan8 with MICs of 0.00012 and 0.00006 μg/mL, respectively.
Fidaxomicin-D7 (OPT-80-D7) is the deuterium labeled Fidaxomicin. Fidaxomicin (OPT-80), a macrocyclic RNA polymerase inhibitor, has a narrow spectrum of activity. Fidaxomicin selectively eradicates pathogenic Clostridium difficile with minimal disruption to the multiple species of bacteria that make up the normal, healthy intestinal flora[1][2].
Glicophenone is an antibacterial agent with MICs of both 32 μg/mL against MRSA OM481, MRSA OM505, MRSA OM584, MRSA OM623 and MSSA 209P[1].
Tosufloxacin (A-61827) is an orally active fluoroquinolone antibiotic. Tosufloxacin shows a broad spectrum of antibacterial activity against gram-positive and gram-negative bacteria[1][2].
Norfloxacin is a broad-spectrum antibiotic that is active against both Gram-positive and Gram-negative bacteria, which functions by inhibiting DNA gyrase.Target: DNA gyrase; AntibacterialNorfloxacin is a synthetic chemotherapeutic antibacterial agent occasionally used to treat common as well as complicated urinary tract infections. Norfloxacin is a broad-spectrum antibiotic that is active against both Gram-positive and Gram-negative bacteria. It functions by inhibiting DNA gyrase, a type II topoisomerase, and topoisomerase IV, enzymes necessary to separate bacterial DNA, thereby inhibiting cell division.There are currently three approved uses in the adult population (one of which is restricted) and the other ineffective due to bacterial resistance. Chibroxin (ophthalmic) is approved for use in children older than one year of age.Norfloxacin is associated with a number of rare serious adverse reactions as well as spontaneous tendon ruptures and irreversible peripheral neuropathy. Tendon problems may manifest long after therapy had been completed and in severe cases may result in lifelong disabilities. Hepatoxicity resulting in fatalities has also been reported with the use of norfloxacin.
DL-3-Phenyllactic acid is a broad-spectrum antimicrobial compound.
Pyrithione is a compound with antibacterial and antifungal activity[1].
N-Hexanoyl-DL-homoserine lactone is a bacterial quorum sensing molecule produced in the rhizosphere. N-Hexanoyl-DL-homoserine lactone, a bacterial quorum sensing signal, induces transcriptional changes in Arabidopsis and may contribute to tuning plant growth to the microbial composition of the rhizosphere[1].
Sulfapyridine(Dagenan) is a sulfonamide antibacterial.Target: AntibacterialSulfapyridine(Dagenan) is a sulfonamide antibacterial. Sulfapyridine is not prescribed for the treatment in humans any more. However, it may be used to treat Linear IgA Disease. It is a good antibacterial drug, but its water solubility is very dependent on PH. Thus, there is a risk of crystallization within the bladder or urethra, which could lead to pain or blockage. The drug sulfasalazine is structurally one molecule of mesalamine linked to one molecule of Sulfapyridine with an azo bond [1].