c[Arg-Arg-Arg-Arg-Nal-Nal-Nal] (Compound 9C) shows broad-spectrum activity against drug-resistant Gram-positive and Gram-negative bacteria, with MICs of 3.1, 3,1, 12.5, and 25 μg/mL for MRSA (ATCC BAA-1556), S. aureus (ATCC 29213), P. aeruginosa (ATCC 27883), and E. coli (ATCC 25922), respectively[1].
Sulfanilamide is a competitive inhibitor for bacterial enzyme dihydropteroate synthetase with IC50 of 320 μM.Target: dihydropteroate synthetase; AntibacterialSulfanilamide containing the sulfonamide functional group displays inhibitory activity for dihydropteroate synthetase partially purified from Escherichia coli which normally uses para-aminobenzoic acid (PABA) for synthesizing the necessary folic acid acting as a coenzyme in the synthesis of purine, pyrimidine and other amino acids, exhibiting an IC 50 of 320 μM for dihydropteroate synthetasea and Km of 2.5 uM for PABA [1]. Sulfanilamide shows IC50 of 286.8 μg/mL for recombinant S. cerevisiae strains with wild-type FOL1 genes, but the single mutation 55Trp to 55Ala or 57Pro to 57Ser within the putative active site of the fungal DHPS confers resistance to Sulfanilamide with IC50 of >800 μg/mL [2]. Administration of Sulfanilamide with the dosage of 100 mg/kg/day is effective in the prevention of P. carinii infection in the immunosuppressed rat model. When the dosage of sulfaguanidine and Sulfanilamide reduced to 10 mg/kg/day, breakthrough P. carinii infection occurs in the rats [3].
Ecubectedin is a derivative. Ecteinascidins is a family of tetrahydroisoquinoline alkaloids with wide range of antitumor and antimicrobial activities[1].
Ribostamycin is a broad-spectrum antimicrobial, inhibits bacterial protein synthesis at the level of 30S and 50S ribosomal subunit binding, also inhibits the chaperone activity of protein disulfide isomerase (PDI), used in pharmacokinetic and nephrotoxicity studies
Spergualin trihydrochloride is a natural product that first identified as an antibiotic from culture filtrates of Bacillus laterosporus BMG162-aF2[1].
Cefalonium hydrate is the first-generation β-lactam cephalosporin antibiotic that is widely used to research bovine mastitis caused by Gram-positive bacteria including staphylococci[1][2][3].
Tulathromycin B (CP 547272) is an isomer of Tulathromycin (a macrolide antibiotic)[1].
Sarecycline is an orally effective narrow-spectrum tetracycline derivative antibiotic. Sarecycline has anti-inflammatory activity. Sarecycline inhibits the activity of Gram-positive bacteria and several types of keratobacterium acnes. Sarecycline interferes with tRNA accommodation and tethers mRNA to the 70S ribosome. Sarecycline can be used to study moderate to severe acne[1][2][3][4][5][6].
Isobutylparaben (Isobutyl 4-hydroxybenzoate) is a constitutive androstane receptor (CAR) activator. Isobutylparaben has a broad-spectrum antimicrobial activity and widely used in personal care products and cosmetics[1].
A40926, the precursor of Dalbavancin, is a second-generation glycopeptide antibiotic. A40926 inhibits gram-positive bacteria, and is very active against Neisseria gonorrhoeae[1].
BioA-IN-13 is a potent, cell permeable and whole-cell active inhibitor of Mycobacterium tuberculosis BioA enzyme[1].
Doxycycline calcium, an antibiotic, is an orally active and broad-spectrum metalloproteinase (MMP) inhibitor[1]. Doxycycline calcium shows antibacterial activity and anti-cancer cell proliferation activity[1][2][3][4][5].
Cefamandole is a second-generation broad-spectrum cephalosporin antibiotic. As the antibiotic is broken down in the body, it releases free NMTT, which can cause hypoprothrombinemia.
Blasticidin A ((+)-Blasticidin A) is an inhibitor of Aflatoxin production by Aspergillus parasiticus. Blasticidin A almost completely inhibits Aflatoxin production at 0.5 μM[1]. Blasticidin A is a potent antibiotic produced by Streptomyces, inhibits Aflatoxin production without strong growth inhibition toward Aflatoxin-producing fungi[2].
FPI-1523, a derivative of Avibactam, is a potent β-lactamase inhibitor, with Kds of 4 nM and 34 nM for CTX-M-15 and OXA-48, respectively. FPI-1523 also inhibits PBP2, with an IC50 of 3.2 μM. FPI-1523 exhibits considerable antimicrobial activity[1].
CRS400393 is a potent antimycobacterial agent, with MIC of 0.03, 2, and ≤ 0.12 µg/mLagainst M. abs., M. avium, M. intracellulare, and M. tuberculosis, respectively[1].
FR182024 is a cephem derivative with potent anti-Helicobacter pylori activities[1].
Triclosan D3 is the deuterium labeled Triclosan. Triclosan is an antibacterial and antifungal agent found in consumer products, including soaps, detergents, toys, and surgical cleaning treatments[1][2].
DG70 (GSK1733953A), a biphenyl amide, is a respiration inhibitor in Mycobacterium tuberculosis, inhibits MenG activity with an IC50 value of 2.6 ± 0.6 μM. DG70 inhibits the catalytic methylation of Mycobacterium tuberculosis demethylmenaquinone methyltransferase enzymes. DG70 can be used for Tuberculosis (TB) research[1][2][3].
D-(+)-Phenyllactic acid is an anti-bacterial agent, excreted by Geotrichum candidum, inhibits a range of Gram-positive from humans and foodstuffs and Gram-negative bacteria found in humans[1].
Neuchromenin is a microbial melabolite that can be isolated from the culture broth of Eupenicillium javanicum var. meloforme PFll81. Neuchromenin induces neurite outgrowth of PC12 cells[1].
Cinnamaldehyde is a major and a bioactive compound isolated from the leaves of Cinnamomum osmophloeum kaneh. Cinnamaldehyde is a cytokine production inhibitor. Cinnamaldehyde has anti-bacteria, anti-oxidation, and anti-inflammatory properties[1].
Antofloxacin is a well tolerate, orally active and broad-spectrum 8-amino-fluoroquinolone with potent antibacterial activities. Antofloxacin shows superior antibacterial activity against gyrA mutation-positive H. pylori strains, especially in Asn87- mutated strains, compared to levofloxacin. Antofloxacin is a weak, reversible inhibitor of CYP1A2 for the treatment of infections caused by a diverse group of bacterial species[1][2][3].
Glepidotin B is a dihydroflavonol compound isolated from the extracts of American licorice, Glycyrrhiza lepidota (Leguminosae). Glepidotin B is an antimicrobial agent[1].
A potent chelator of iron that arrests late stages of cytokinesis by blocking the physical process of constriction in dividing cells; also is a small molecule inhibitor of bacterial divisome assembly; downregulates the transcription of genes encoding proteins involved in cell division, reduce protein biosynthesis, and affects the spatiotemporal localization of the division machinery.
4-Chloroguaiaco (4-Chloro-2-methoxyphenol) is a phenol derivative, with antimicrobial activity. 4-Chloroguaiaco shows inhibition against S. aureus and E. coli with MICs both of 110μg/mL[1].
Prussian blue insoluble (Iron(III) ferrocyanide) is a good adsorbent to be used as antidotes for poisoning with cesium or thallium ions. Prussian blue insoluble (Iron(III) ferrocyanide) has anticancerous and antibacterial properties. Prussian blue insoluble (Iron(III) ferrocyanide) can be used as a contrast agent in photoacoustic and magnetic resonance imaging (MRI). Prussian blue insoluble can be used for contrast agents, antidotes and cancer research[1][2][3][4].
Oxytetracycline hydrochloride is an antibiotic belonging to the tetracycline class. Oxytetracycline hydrochloride potent inhibits Gram-negative and Gram-positive bacteria. Oxytetracycline hydrochloride is a protein synthesis inhibitor and prevents the binding from aminoacil-tRNA to the complex m-ribosomal RNA. Oxytetracycline hydrochloride also possesses anti-HSV-1 activity[1][2][3].
Ceftriaxone sodium salt is an antibiotic useful for the treatment of a number of bacterial infections.Target: AntibacterialCeftriaxone inhibits bacterial cell wall synthesis by means of binding to the penicillin-binding proteins (PBPs). Inhibition of PBPs would in turn inhibit the transpeptidation step in peptidoglycan synthesis which is required for bacterial cell walls. Like other cephalosporins, ceftriaxone is bacteriocidal and exhibits time-dependent killing. Ceftriaxone, one of the beta-lactam antibiotics, is a stimulator of EAAT2 expression with neuroprotective effects in both in vitro and in vivo models based in part on its ability to inhibit neuronal cell death by glutamate excitotoxicity. Based on this consideration and its lack of toxicity, ceftriaxone has potential to manipulate glutamate transmission and ameliorate neurotoxicity [1].
Sulfaclozine sodium (Sulfachloropyrazine sodium) is an efficacious sulphonamide derivative with antibacterial and anticoccidial effects. Sulfaclozine sodium is commonly used for the treatment of various poultry diseases (particularly, collibacteriosis, fowl cholera and coccidiosis)[1].