7-O-Methylaloeresin A is 5-methylchromone glycoside isolated from Commiphora socotrana (Burseraceae)[1]. 7-O-Methylaloeresin A exhibits good activity against multiple drug resistant Staphylococcus aureus (NCTC 11994) and Salmonella typhimurium (ATCC 1255) with MIC values of 0.72 and 0.18 mM, respectively[2].7-O-Methylaloeresin A has antioxidant activities, gives IC50 values of 0.026 mM and 0.021 mM for DPPH and 2-deoxyribose degradation assay, respectively[2].
Antitubercular agent-32 is a derivate of Benzothiazinone (HY-13579A), inhibits M. tuberculosis, and shows improved metabolic stability and enhanced water solubility. Antitubercular agent-32 exerts antitubercular effect by targeting decaprenylphosphoryl-β-D-ribose 2’-oxidase (DprE1, IC50=3.9 μM)[1].
Protein kinase G inhibitor-2 (Compound 266) is a mycobacterial protein kinase G inhibitor, with an IC50 of 3 μM. Protein kinase G inhibitor-2 can be used for mycobacterial infection research[1].
Pipemidic acid trihydrate, a derivative of Piromidic acid, is an antibacterial agent. Pipemidic acid trihydrate inhibits DNA gyrase. Pipemidic acid trihydrate is active against gram-negative bacteria including Pseudomonas aeruginosa as well as some gram-positive bacteria. Pipemidic acid trihydrate can be used for the research of intestinal, urinary, and biliary tract infections[1][2].
Chartreusin is an antibiotic that is active against certain Gram-positive organisms and mycobacteria. Chartreusin is also active against the Micrococcus fiyogenes v. aureus phage[1].
Balofloxacin dehydrate is a quinolone antibiotic, inhibiting the synthesis of bacterial DNA by interference with the enqyme DNA gyrase[1].
Erythromycin thiocyanate is a macrolide antibiotic produced by actinomycete Streptomyces erythreus with a broad spectrum of antimicrobial activity. Erythromycin thiocyanate acts by binding to bacterial 50S ribosomal subunits and inhibits RNA-dependent protein synthesis by blockage of transpeptidation and/or translocation reactions, without affecting synthesis of nucleic acid[1].
Propargyl-PEG8-acid is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). The ADCs can be used in bacterial infections caused by Gram-negative bacteria[1].
PR-39, a natural proline- and arginine-rich antibacterial peptide, is a noncompetitive, reversible and allosteric proteasome inhibitor. PR-39 reversibly binds to the α7 subunit of the proteasome and blocks degradation of NF-κB inhibitor IκBα by the ubiquitin-proteasome pathway. PR-39 stimulates angiogenesis, inhibits inflammatory responses and significant reduces myocardial infarct size in mice[1][2].
DprE1-IN-4 is a potent and orally active noncovalent DprE1 inhibitor with an IC50 of 0.90 μg/mL. DprE1-IN-4 exhibits potent in vitro activity against M. tuberculosis H37Rv and drug-resistant tuberculosis strain with MIC values of 0.12 μg/mL and 0.24 μg/mL, respectively. DprE1-IN-4 displays acceptable pharmacokinetic property and shows significant bactericidal activity in an acute mouse model of tuberculosis[1].
Ergosterol peroxide is a steroid derivative and can be isolated from a variety of fungi, yeast, lichens or sponges. Ergosterol peroxide has anti-tumour, proapoptotic, anti-inflammatory, anti-mycobacterial, and anti-proliferative activities[1][2].
Mram 8 is a cyclotide isolated from Viola philippica, a plant from the Violaceae family[1].
ATD-3169 is a ROS generator with antibacterial activity.
Clofoctol is a bacteriostatic antibiotic. It is used in the treatment of respiratory tract and ear, nose and throat infections caused by Gram-positive bacteria. It is only functional against Gram-positive bacteria, It penetrates into human lung tissue.
Calcimycin hemicalcium salt (A-23187 hemicalcium salt) is an antibiotic and a unique divalent cation ionophore (like calcium and magnesium). Calcimycin hemicalcium salt induces Ca2+-dependent cell death by increasing intracellular calcium concentration. Calcimycin hemicalcium salt inhibits the growth of Gram-positive bacteria and some fungi. Calcimycin hemicalcium salt also inhibits the activity of ATPase and uncouples oxidative phosphorylation of mammalian cells. Calcimycin hemicalcium salt induces apoptosis[1][2][3][4].
CHRG01 is a biological active peptide. (CHRG01 is derived from human b-defensin 3 (hBD3) C-terminal amino acids 54 to 67, with all Cys residues substituted with Ser. This substitution removes all disulfide bond linkages within the sequence. CHRG01, like hBD3, displays electrostatic-dependent antimicrobial properties.)
(S)-Lansoprazole (Levolansoprazole) is an isoform of Lansoprazole (HY-13662), which is an orally active proton pump inhibitor which prevents the stomach from producing acid. Lansoprazole (AG 1749) is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor)[1][2].
Herbimycin A, an ansamycin antibiotic, acts as a Src family kinase inhibitor. Herbimycin A binds to the SH domain and inhibits the activity of p60v-src and p210BCR-ABL. Herbimycin A inhibits Hsp90 and impairs recovery from heat shock. Herbimycin A exhibits antiangiogenic activity in endothelial cells in vitro.
3-O-cis-p-Coumaroyl maslinic acid (compound 16) is a natural compound isolated from the ethyl acetate extract of leaves of Miconia albicans.3-O-cis-p-Coumaroyl maslinic acid can inhibit PTP1B, with the IC50 of 0.46 μM, and shows antimicrobial activity on Gram-positive bacteria and yeasts[1][2].
Cefadroxil is a broad-spectrum antibiotic of the cephalosporin type, effective in Gram-positive and Gram-negative bacterial infections.
AVX 13616 shows the potent in vivo antibacterial activity of Avexa’s lead antibacterial candidate; particularly against drug-resistant Staphylococcus pathogens.IC50 value: 2-4 ug/ml (MICs)Target: antibacterial agent AVX13616 was as active as mupirocin in a nasal decolonization model but required only a single application. The compounds are being developed for topical indications and/or wound infection/catheter-related infections. AVX13616 and other compounds showed broad spectrum antibacterial activity against a range of isolates with MICs of 2-4 micrograms per millilitre against S. aureus, coagulase negative staphylococci, enterococci, MRSA, VISA and VRSA. A single application of 5% (w/w) AVX13616 (approximately equimolar to 2% mupirocin) was as effective as 2% mupirocin administered twice a day for five days in nasal decolonisation of MRSA in mice.
Cefoperazone-d5 is deuterium labeled Cefoperazone. Cefoperazone, a semisynthetic cephalosporin, has a broad spectrum of antibacterial activity[1].
Nilofabicin is an enoyl-(acyl-carrier protein) reductase (FabI) inhibitor. Nilofabicin had an MIC(90) of 0.5 microg/ml for Staphylococcus aureus strains and was more potent than either linezolid or vancomycin[1].
Triamcinolone is a long-acting synthetic corticosteroid.Target: Glucocorticoid ReceptorDimethyl fumarate is an anti-inflammatory. It is indicated for multiple sclerosis patients with relapsing forms and is also being investigated for the treatment of psoriasis. The mechanism of action of dimethyl fumarate in multiple sclerosis is not well understood. It is thought to involve dimethyl fumarate degradation to its active metabolite monomethyl fumarate (MMF) then MMF up-regulates the Nuclear factor (erythroid-derived 2)-like 2 (Nrf2) pathway that is activated in response to oxidative stress [1]. The mean duration of follow-up was 40 months. The rate of decline in the FEV1 after bronchodilator use was similar in the 559 participants in the triamcinolone group and the 557 participants in the placebo group (44.2+/-2.9 vs. 47.0+/-3.0 ml per year, P= 0.50). Members of the triamcinolone group had fewer respiratory symptoms during the course of the study (21.1 per 100 person-years vs. 28.2 per 100 person-years, P=0.005) and had fewer visits to a physician because of a respiratory illness (1.2 per 100 person-years vs. 2.1 per 100 person-years, P=0.03). Those taking triamcinolone also had lower airway reactivity in response to methacholine challenge at 9 months and 33 months (P=0.02 for both comparisons) [2].
Tricyclazole is a pentaketide-derived melanin biosynthesis inhibitor and a unique fungicide for control of Pyricularia oryzae on rice[1][2].
Carabrone is isolated from the fruits of Carpesium abrotanoides , is a well-known sesquiterpene and exhibits significant anti-bacterial and anti-tumor activities[1].Carabrone exhibits antifungal activities in vitro and in vivo against Botrytis cinerea, Colletotrichum lagenarium(EC50=7.10 μg/mL) and Erysiphe graminis[2].
Ceftobiprole is a broad-spectrum cephalosporin with activity against Methicillin-resistant staphylococcus aureus (MRSA) with the MIC90 value of 2 mcg/mL.
4-Ethoxycoumarin is an antimicrobial[1].
Flucloxacillin sodium is a highly active antibiotic against Gram-positive and Gram-negative bacteria.
Taniborbactam is a potent inhibitor of β-lactamase, with IC50s of <100 nM for SHV-5, KPC-2, VIM-2, and AmpC β-lactamase, and 0.1 to 1 μM for OXA-1 β-lactamase, used in the research of bacterial infections[1].