urease

Urease is produced by many types of bacteria and is an effective virulence factor for some pathogenic bacteria. Urease is also central to the metabolism and virulence of Helicobacter pylori, helping it colonize the stomach lining [1] .

Urease Inhibitor 07 is an isosubstituted metalloproteinase inhibitor with potential activity against Mycobacterium tuberculosis strain H37Rv.

Urease-IN-9 (Compound 1e), an urease inhibitor with an IC50 of 19.5 μM, effectively impedes the enzyme's activity [1].

Urease-IN-6, a potent Urease inhibitor, exhibits an IC50 value of 14.2 μM and is utilized in the research of peptic and gastric ulcers [1].

Urease-IN-7 (Compound 5k) acts as a competitive inhibitor of the enzyme urease, exhibiting an IC50 value of 3.33 μM and a K_i of 3.62 μM. This compound has potential applications in the study of peptic and gastric ulcers [1].

Urease-IN-8 (Compound 5e) functions as a competitive inhibitor of urease, with an IC50 value of 3.51 μM and a Ki of 3.11 μM. It is applicable for research pertaining to peptic and gastric ulcers [1].

Urease-IN-4 is a potent urease inhibitor, demonstrating an IC50 value of 1.64 µM and exhibiting low cytotoxicity. Additionally, it exhibits inhibitory activity against P. vulgaris, with an IC50 value of 15.27 µg/mL.

Urease-IN-2 is a non-competitive inhibitor of urease (IC50: 0.94 μM, Ki: 1.6 μM) that non-competitively inhibits Jack bean urease (JBU).

Urease -IN-1 is a urease inhibitor (IC50: 2.21±0.45 μM).

Urease-IN-5, an urease inhibitor, exhibits a potent inhibitory effect with an IC50 of 1.473 µM and demonstrates low cytotoxicity alongside inhibitory activity against P. vulgaris, marked by an IC50 of 17.78 µg/mL.

Butylboronicacid is a competitive inhibitor of urease and acts as a monosaccharide complexing reagent.

Benurestat (EU-2826) is a urease inhibitor.

Acetohydroxamic acid (N-Hydroxyacetamide) is an antagonist of the bacterial enzyme urease.

(R)-3-hydroxy Myristic Acid is an antifungal compound from Lactobacillus plantarum MiLAB 14 with antioxidant, anti-elastase, and anti-urease activities and can be used in the study of fungal infections.

Atalantoflavone shows urease inhibitory potential. It displays weak cytotoxic activity against the human Caucasian prostate adenocarcinoma cell line PC-3.

9,11-Dehydro-β-boswellic acid is a compound with urease inhibitory activity and acts as an inhibitor of 5-lipoxygenase (5-LO), a critical enzyme in leukotriene biosynthesis.

MMP inhibitor I is a peptide inhibitor of matrix metalloproteinase-1 (MMP-1), MMP-2, and MMP-3 (IC50s = 1.3, 30, and 150 μM, respectively). It is selective for MMP-1, MMP-2, and MMP-3 over the proteases thermolysin, urease, trypsin, α-chymotrypsin, plasmin, and elastase at concentrations up to 4 mM.

4-Chlorocinnamic acid is a photosensitive compound. 2-Chlorocinnamic acid and 4-chlorocinnamic acid show potent urease inhibitory activities with the respective IC50 values of 0.66 and 1.10 uM.

2-Chlorocinnamic acid is a photosensitive compound, it can inhibit tyrosinase activity. 2-Chlorocinnamic acid and 4-chlorocinnamic acid show potent urease inhibitory activities with the respective IC50 values of 0.66 and 1.10 uM.

3,3'-((2-Chlorophenyl)methylene)bis(4-hydroxy-2H-chromen-2-one) is a non-nucleotide inhibitor of ectonucleotide pyrophosphatase/phosphodiesterase 1 (ENPP1; Ki = 50 μM).1,2 It also inhibits urease (IC50 = 84.53 μM for the Jack bean enzyme).3 |1. Choudhary, M.I., Fatima, N., Khan, K.M., et al. New biscoumarin derivatives-cytotoxicity and enzyme inhibitory activities. Bioorg. Med. Chem. 14(23), 8066-8072 (2006).|2. Onyedibe, K.I., Wang, M., and Sintim, H.O. ENPP1, an old enzyme with new functions, and small molecule inhibitors - A STING in the tale of ENPP1. Molecules 24(22), E4192 (2019).|3. Khan, K.M., Iqbal, S., Lodhi, M.A., et al. Biscoumarin: New class of urease inhibitors; economical synthesis and activity. Bioorg. Med. Chem. 12(8), 1963-1968 (2004).

Enzyme-IN-2 (compound 15) serves as a potent urease inhibitor, exhibiting anti-ureolytic activity with a K i of 2.36 µM and an IC 50 of 0.75 µM [1].

CAY10761 is an inhibitor of ectonucleotide pyrophosphatase/phosphodiesterase 1 (ENPP1; IC50s = 467 and 429 μM for the human and snake venom enzymes, respectively).1,2 It also inhibits mushroom tyrosinase (Ki = 1.9 μM) and urease from jack bean, P. mirabilis, and B. pasteurii (IC50s = 0.093, <0.125, and 0.089 mM, respectively, at pH 8.2).3,4 |1. Khan, K.M., Fatima, N., Rasheed, M., et al. 1,3,4-Oxadiazole-2(3H)-thione and its analogues: A new class of non-competitive nucleotide pyrophosphatases/phosphodiesterases 1 inhibitors. Bioorg. Med. Chem. 17(22), 7816-7822 (2009).|2. Onyedibe, K.I., Wang, M., and Sintim, H.O. ENPP1, an old enzyme with new functions, and small molecule inhibitors - A STING in the tale of ENPP1. Molecules 24(22), E4192 (2019).|3. Ghani, U., and Ullah, N. New potent inhibitors of tyrosinase: Novel clues to binding of 1,3,4-thiadiazole-2(3H)-thiones, 1,3,4-oxadiazole-2(3H)-thiones, 4-amino-1,2,4-triazole-5(4H)-thiones, and substituted hydrazides to the dicopper active site. Bioorg. Med. Chem. 18(11), 4042-4048 (2010).|4. Amtul, Z., Rasheed, M., Choudhary, M.I., et al. Kinetics of novel competitive inhibitors of urease enzymes by a focused library of oxadiazoles/thiadiazoles and triazoles. Biochem. Biophys. Res. Commun. 319(3), 1053-1063 (2004).

1. Guaijaverin (Quercetin-3-Arabinoside) is a urease inhibitor. 2. Guaijaverin has antioxidant activity. 3. Guaijaverin has antibacterial activity against Strep. mutans.

Glutamate dehydrogenase, an enzyme found in prokaryotes and eukaryotic mitochondria, facilitates the enzymatic determination of ammonia, alpha-ketoglutaric acid, L-glutamate, and urease [1].

Flurofamide is an effective bacterial urease inhibitor and has potential in the treatment of infected urinary calculi.