GW779439X is a pyrazolopyridazine identified in an inhibitor of the S. aureus PASTA kinase Stk1. GW779439X potentiates the activity of β-lactam antibiotics against various MRSA and MSSA isolates, some even crossing the breakpoint from resistant to sensitive. GW779439X is an AURKA inhibitor and induces apoptosis by the caspases 3/7 pathway[1][2]. MRSA:methicillin-resistant S. aureus; MSSA: methicillin-sensitive S. aureus
Penamecillin (Wy 20788) an acetoxymethyl ester of Penicillin G (HY-N7139). Penamecillin is an orally active antibacterial agent[1][2].
Eckol is a potent hMAO-A (Mixed) and hMAO-B (non-competitive) inhibitor with IC50s of 7.20 and 83.44 μM, respectively. Eckol shows stimulatory effects in maize and can be used as a plant biostimulant. Eckol also shows antiallergic and antiviral effects[1][2][3][4].
Aztreonam (lysine) is a monocyclic beta-lactam antibiotic, and has a very high affinity for penicillin-binding protein 3 (PBP-3). Aztreonam (lysine) is active against Gram-negative aerobic bacteria[1][2].
Benzoyleneurea possesses anti-bacterial activity. Benzoyleneurea scaffold can be used in the synthesis of novel protein geranylgeranyltransferase-I (PGGTase-I) inhibitors[1].
Defensin NP-3A (NP-3A; Corticostatin 1) is a human granulocyte peptide, with anti-ACTH activity. Defensins are antimicrobial peptides with and cytotoxic activity[1][2].
Ribocil is a highly selective chemical modulator of bacterial riboflavin riboswitches. Ribocil strongly inhibits GFP expression, achieving a 50% effective concentration (EC50) of 0.3 μM.Target: in vitro: Ribocil is a highly specific bioactive synthetic mimic of FMN, which competes with the natural ligand to inhibit FMN riboswitch-mediated expression of ribB and inhibits bacterial growth. Ribocil-B demonstrates superior microbiological activity as compared to Ribocil-A (minimum inhibitory concentration (MIC) = 1 μg/ml versus MIC ≥ 64 μg/ml), inhibition of riboflavin synthesis (IC50 = 0.13 μM versus IC50 > 26 μM), and binding affinity to the E. coli FMN aptamer (Kd = 6.6 nM versus Kd ≥ 10,000 nM).[1]
VT-1598 is a potent, high-affinity, oral inhibitor of fungal sterol 14α-demethylase (CYP51B) with Kd of 13 nM; is more selective for fungal CYP51 than related human CYP enzymes such as CYP3A4; exhibits excellent potency against yeast, dermatophyte, and mold fungal pathogens.
Bombinin H2 is an antimicrobial peptide derived from the skin of moth Bombina variegata[1].
Posaconazole hydrate is a broad-spectrum, second generation, triazole compound with antifungal activity.
SARS-CoV-2 3CLpro-IN-7 is a reversible covalent SARS-CoV-2 3CL protease inhibitor with an IC50 value of 1.4 µM[1].
AFN-1252(Debio 1452) is a potent inhibitor of enoyl-acyl carrier protein reductase (FabI), inhibited all clinical isolates of Staphylococcus aureus and Staphylococcus epidermidis at concentrations of ≤0.12 μg/ml. IC50 value:Target: Antibiotic agentAFN-1252 was inactive (MIC90, >4 μg/ml) against clinical isolates of Streptococcus pneumoniae, beta-hemolytic streptococci, Enterococcus spp., Enterobacteriaceae, nonfermentative gram-negative bacilli, and Moraxella catarrhalis. These data support the continued development of AFN-1252 for the treatment of patients with resistant staphylococcal infections.
Methyl Paraben, isolated from the barks of Tsuga dumosa the methyl ester of p-hydroxybenzoic acid, is a standardized chemical allergen. Methyl Paraben is a stable, non-volatile compound used as an antimicrobial preservative in foods, drugs and cosmetics. The physiologic effect of Methyl Paraben is by means of increased histamine release, and cell-mediated immunity[1].
WQ3810 is an orally active fluoroquinolone, with potent antibacterial activities.
GST-HG131 is a specific inbihitor of hepatitis B virus (HBV) surface antigen, belongs to dihydrobenzopyridooxazepine (DBP) series. GST-HG131 exhibits excellent and specific HBV antigens inhibition with EC50 of 28.2 nM (HBsAg) and 16.0 nM (HBeAg), respectively, but also it is safety for animal[1].
Galanolactone is a natural product that can be isolated from the seeds of Alpinia galanga. Galanolactone shows antifungal activitie. Galanolactone shows cytotoxicity against KB cells with an EC50 of 38.5 µg/ml[1].
Yadanziolide B, a natural indole alkaloid, is a potential H5N1 neuraminidase inhibitor[1][2].
Paederoside is a monoterpene S-methyl thiocarbonate isolated from Paederia pertomentosa. Paederoside shows a high anti-tumor promoting activity against the Epstein-Barr virus activation[1].
Novel capsid targeted inhibitor of HIV-1 replication
Colistin (Polymyxin E) is an orally active polypeptide antibiotic and has excellent activity against various Gram-negative rod-shaped bacteria, including multidrug-resistant Pseudomonas aeruginosa, Acinetobacter baumannii and Klebsiella pneumoniae. Colistin (Polymyxin E) is associated with nephrotoxicity and can be used for the research of infections caused by Gram-negative bacilli[1][2].
Macrocarpal B is an antibacterial compounds. Macrocarpal B can be isolated from the branch of Eucalyptus globulus. Macrocarpal B can be used for the research of periodontal disease[1].
CDD-1845 is a non-covalent and non-peptide potent SARS-CoV-2 Mpro inhibitor with a Ki of 3 nM. CDD-1845 also inhibits ΔP168, A173V, and ΔP168/A173V Mpro variants[1].
TC14012, a serum-stable derivative of T140, is a selective and peptidomimetic inverse CXCR4 agonist with an IC50 of 19.3 nM. TC14012 is a potent CXCR7 agonist an EC50 of 350 nM for recruiting β-arrestin 2 to CXCR7. TC14012 has anti-HIV activity and anti-cancer activity[1][2].
5-Fluorouracil-13C4,15N2 is the 13C and 15N labeled 5-Fluorouracil[1]. 5-Fluorouracil (5-FU) is an analogue of uracil and a potent antitumor agent. 5-Fluorouracil affects pyrimidine synthesis by inhibiting thymidylate synthetase thus depleting intracellular dTTP pools. 5-Fluorouracil induces apoptosis and can be used as a chemical sensitizer[2][3]. 5-Fluorouracil also inhibits HIV[4].
Aromadendrene can be isolated from Eucalyptus globulus. Aromadendrene has antimicrobial activity[1].
Sulfadiazine is a sulfonamide antibiotic.Target: AntibacterialSulfadiazine eliminates bacteria that cause infections by stopping the production of folate inside the bacterial cell, and is commonly used to treat urinary tract infections (UTIs). In combination, sulfadiazine and pyrimethamine, can be used to treat toxoplasmosis, a disease caused by Toxoplasma gondii. From Wikipedia.The ulcers who treated with silver sulfadiazine cream responded rapidly, with one-third showing bacterial levels of less than 10(5) within three days, and half within a week [1].
Ertapenem (MK-0826) is a broad spectrum and long acting β-lactam antibiotic. Ertapenem has a broad-spectrum anti-anaerobic activity against a variety of anaerobes with a mode MIC of 0.12 μg/mL. Ertapenem can be used for the research of severe infections caused by bacteria in the skin, lungs, stomach, pelvis, and urinary tract[1][2].
Continentalic acid from Aralia continentalis has minimum inhibitory concentrations (MICs) of approximately 8-16 µg/mL against S. aureus, including the Methicillin susceptible Staphylococcus aureus (MSSA) and Methicillin-resistant Staphylococcus aureus (MRSA) standard strains[1].
Cap-dependent endonuclease-IN-23 is a potent inhibitor of cap-dependent endonuclease (CEN). Cap-dependent endonuclease-IN-23 inhibits the replication of influenza virus. ap-dependent endonuclease-IN-23 has the potential for the research of influenza virus infection (influenza A) (extracted from patent WO2021233302A1, compound 8A or 8B)[1].
Human β-defensin-3 (HβD-3) is an antibiotic anti-microbial peptide produced by epithelial cells with antimicrobial activities and reduces the effect of inflammatory cytokine responses. Human β-defensin-3 is against different microbes with IC90 values of 6-25 μg/ml[1].