Dapsone is a sulfone active against a wide range of bacteria but mainly employed for its actions against mycobacterium leprae.Target: AntibacterialDapsone is an antibacterial most commonly used in combination with rifampicin and clofazimine as multidrug therapy (MDT) for the treatment of Mycobacterium leprae infections (leprosy). Dapsone antagonized all of the I/R end points measured, showing a remarkable ability to decrease markers of damage through antioxidant, antiinflammatory, and anti-apoptotic effects [1]. As an antibacterial, dapsone inhibits bacterial synthesis of dihydrofolic acid, via competition with para-aminobenzoate for the active site of dihydropteroate synthetase. Dapsone has anti-inflammatory and immunomodulatory effects [2].
Acetaminophen (paracetamol) is a selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 25.8 μM; is a widely used antipyretic and analgesic drug.
Neorauflavene is a phenolic neorautanenia isoflavanoid isolated from Neorautanenia edulis. Neorauflavene shows antibacterial activities against E. faecalis, S. suis, S. agalactiae, P. aeruginosa, B. subtilis, and R. anatipestifer[1][2].
Terizidone is an antibacterial agent, and shows bacteriostatic activity. Terizidone can be used in tuberculosis (TB) research[1].
GlcN-6-P Synthase-IN-1 (Compound 4d) is a Glucosamine-6-phosphate (GlcN-6-P) synthase inhibitor with an IC50 of 3.47 μM. GlcN-6-P Synthase-IN-1 exhibits significant antimicrobial activity. GlcN-6-P Synthase-IN-1 has good penetration in the CNS and is able to inhibit the cytochrome P450, CYP3A4 isoform[1].
Bactenecin 7 is an antibacterial peptide active against the growth of Enterobacter cloacae (MICs, 25 to 200μg/ml)[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].
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].
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.
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.
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].
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.
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].
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].
Antibacterial agent 125 is an antibacterial agent. Antibacterial agent 125 has a potent antimicrobial activity against clinically relevant Gram-positive pathogens with MIC50 values range from 0.25 - 8 μM. Antibacterial agent 125 can be used for the research of antimicrobial resistance[1].
Atuzaginstat (COR388) hydrochloride is an effective small-molecule bacterial protease lysine gingipain inhibitor and can be used for Alzheimer's disease research[1][2].
ND-011992 is a reversible, selective quinazoline-type inhibitor targeting quinone reductases and quinol oxidases. ND-011992 inhibits respiratory complex I and bo3 oxidase in addition to bd-I and bd-II oxidases in E. coli strain BL21*Δcyo with the IC50 of 0.12, 2.47, 0.63 and 1.3 μM, respectively. ND-011992 can be used for tuberculosis study[1].
Benzimidazole is a heterocyclic aromatic organic compound and acts as an important pharmacophore in medicinal chemistry. Benzimidazole derivatives have been reported to possess various biological activities such as anti-cancer, anti-viral, anti-bacterial, anti-fungal, anti-helmintic, anti-inflammatory, proton pump inhibitor and anti-coagulant property[1][2][3].
Cyclo(L-Pro-L-Val) is a 2,5-diketopiperazine, with toxic activity against phytopathogenic microorganisms (such as R. fascians LMG 3605). Cyclo(L-Pro-L-Val) shows toxicity similar to Chloramphenicol (HY-B0239) with comparable concentration. Cyclo(L-Pro-L-Val) can also inhibit gram-positive phytopathogenic bacterium. Cyclo(L-Pro-L-Val) has potential development as biopesticide[1].
lsocryptomerin is a membrane-active antifungal compound that can be isolated from Selaginella tamariscina. lsocryptomerin can depolarize fungal plasma membrane. lsocryptomerin also shows anticancer and antibacterial activities[1][2].
Moenomycin complex is a potent transglycosylase inhibitor. Moenomycin complex inhibits bacterial growth by blocking the transglycosylase activity of class A penicillin-binding proteins (PBPs)[1].
OYYF-175, an antimicrobial antifolate, is a dihydrofolate reductase (DHFR) inhibitor with an IC50 of 2.36 nM for Escherichia coli DHFR. OYYF-175 exhibits potent broad-
Cephradine monohydrate (Cefradine monohydrate) is a first generation cephalosporin, which is active against a wide range of Gram positive and Gram-negative bacteria[1].
[1-13Cglc]Lactose monohydrate is an isotopic labeling drug[1].
Ticarcillin disodium is an injectable antibiotic for the treatment of Gram-negative bacteria, particularly Pseudomonas aeruginosa. It is also one of the few antibiotics capable of treating Stenotrophomonas maltophilia infections.
β-Lactamase-IN-4 is a β-lactamase inhibitor extracted from patent WO2013149121A1, compound 708. β-Lactamase-IN-4 can be used for the research of bacterial infections[1].
TP0480066 is a selective topoisomerase II inhibitor with IC50s of 1.10 and 62.89 nM for DNA gyrase and topo IV, respectively. TP0480066 shows good activity of againsting various bacterial species including drug-resistant strains. TP0480066 also exhibits potent inhibitory activity to N. gonorrhoeae, can be used in study of gonorrhea[1][2].