Building Blocks

7-Methoxy-2H-benzo[b][1,4]oxazin-3(4H)-one (7MB) is a hydroxamic acid that has been shown to be an effective inhibitor of β-glucosidase. 7MB leaves the glucosides intact and only affects the substrate by attacking the carbonyl group. The enzyme β-glucosidase is responsible for hydrolyzing these glycosides into glucose, which can then be absorbed by the body. 7MB has been shown to inhibit glucosidase activity in insect and bacterial cells. It also inhibits esculin, which is a drug used as a skin test for allergies, and has been shown to have antiinflammatory properties.

2-Amino-N,N-dimethylbenzamide is an organic compound with the chemical formula CH3CONH2. It is a white solid with a pungent odor. 2-Amino-N,N-dimethylbenzamide is used as an industrial chemical in the synthesis of selenium oxide and carbon monoxide. It also acts as a catalyst for various reactions such as the synthesis of acetaldehyde from ethanol and oxygen gas or the conversion of ammonia to nitric acid.

Versatile small molecule scaffold

Versatile small molecule scaffold

3,5,6-Trichloro-2-pyridinol (3,5,6-TCP) is an intermediate in the production of chlorpyrifos. It is also a metabolite of chlorpyrifos and has been detected in urine samples. 3,5,6-TCP can be determined by titrimetric analysis using sodium carbonate as a reagent. 3,5,6-TCP is toxic to both humans and animals at high doses. The process optimization for the synthesis of 3,5,6-TCP was investigated in order to reduce the amount of wastewater produced during production. In this study it was found that reaction solution pH was significantly lower when anhydrous sodium carbonate was used instead of water saturated sodium carbonate. This discovery would allow for more efficient wastewater treatment because less wastewater would need to be treated per unit product.

Versatile small molecule scaffold

Versatile small molecule scaffold

L-152,804 is a potent inhibitor of the dopamine receptor. It has been shown to have an inhibitory effect on wild-type mice and functional assays in vitro. L-152,804 inhibits locomotor activity in wild type mice and increases energy metabolism in adipose tissue. L-152,804 binds to the dopamine receptor by competitive inhibition and inhibits the binding of glutamate and dopamine to the receptor. This drug has also been shown to have anti-inflammatory effects in a rat model of arthritis.

Versatile small molecule scaffold

Versatile small molecule scaffold

Versatile small molecule scaffold

N-(2-Aminopropyl)aniline is a voltage-gated sodium channel blocker that inhibits the voltage-gated sodium channels. It has been shown to be effective in treating chronic pain, especially in animal models. N-(2-Aminopropyl)aniline is not used for the treatment of cough because it does not have any effect on the vagal nerve. The drug also shows some inhibitory activity against voltage-gated sodium channels, which are found in neurons and play an important role in pain signaling.

N-Aminomorpholine-4-carbothioamide is a ligand that binds to the carboxylates of chloroform. It is produced by the enzyme subtilisin from the amino acid L-alanine and the compound 2-acetylpyridine. This ligand has been found in microorganisms such as Escherichia coli, Staphylococcus aureus, and Saccharomyces cerevisiae. N-Aminomorpholine-4-carbothioamide has been shown to be an effective inhibitor of yeast growth but not bacterial growth. The molecular weight of this ligand is 226.2 g mol−1 and it is a dimer at room temperature with two molecules linked together by hydrogen bonds.

1-Ethyl-1,2,3,4-tetrahydropyrimidine-2,4-dione (ETP) is a potent inhibitor of pyrimidine biosynthesis. It has been shown to inhibit the growth of cancer cells in vitro and in vivo. ETP binds to the enzyme dihydroorotate dehydrogenase and prevents the formation of orotic acid from l-tartaric acid. This inhibition leads to an accumulation of orotic acid and l-tartaric acid in the cell which inhibits cellular respiration. ETP also inhibits other enzymes involved in DNA replication, such as ribonucleotide reductase and thymidylate synthase. This inhibition leads to decreased synthesis of DNA and RNA molecules that are necessary for cell division. ETP has also been shown to be effective against hepatitis B virus by inhibiting viral DNA synthesis and causing viral DNA degradation.

Versatile small molecule scaffold

Versatile small molecule scaffold

Versatile small molecule scaffold

Versatile small molecule scaffold

2-Methylquinazoline-4-thiol is a heterocyclic compound with a thione group. Its amide groups are similar to those found in peptides, which play an important role in the coordination chemistry of the molecule. The 2-methylquinazoline-4-thiol skeleton is tetracyclic and can be used for synthetic purposes. This compound has been shown to have hepatoprotective properties, but also has cytotoxic effects on cells.

Versatile small molecule scaffold

Versatile small molecule scaffold

3-Phenylumbelliferone is a coumarin derivative that is used as an antidiabetic drug. It is a competitive inhibitor of the enzyme phosphatase, which inactivates tyrosine kinase, and inhibits the formation of DOPA from L-tyrosine, resulting in inhibition of glucose uptake by cells. 3-Phenylumbelliferone also fluoresces at wavelengths of 340 nm when excited with ultraviolet light. This property has been shown to be helpful in the detection of phenylurea herbicides, polycyclic aromatic hydrocarbons, and other compounds.