Building Blocks

Benzo[d][1,2,3]thiadiazole is a benzothiadiazole with a redox potential of -0.25 V that is stable in the absence of oxygen and light. It can be used to synthesize chemical pesticides by reacting with hydrochloric acid. The reaction mechanism of benzo[d][1,2,3]thiadiazole has been determined using nuclear magnetic resonance spectroscopy and quantum chemical calculations. This compound reacts with hydrogen bond acceptors on the enzyme active site to form covalent bonds. It also interacts with the enzyme's steric environment by forming hydrogen bonds and van der Waals forces. Benzo[d][1,2,3]thiadiazole also emits light when it reacts with nitric oxide in solution.

Imidazo[4,5-b]pyrazine is a chemical compound that binds to calcium ions and has been used in the treatment of metabolic disorders. The symptoms of imidazopyrazine include fatigue, weight loss, fever, chills, and muscle aches. Imidazopyrazine is also used for the treatment of autoimmune diseases such as rheumatoid arthritis. In vitro assays have shown that it activates macrophages and lymphocytes and may be useful in the treatment of skin lesions caused by an infection. Imidazopyrazine has been found to have pharmacokinetic properties with a half-life of 3 hours when administered orally. This drug has also been shown to have biological activity against rat liver microsomes.

3-Oxa-7-azabicyclo[3.3.1]nonane is a linker that contains a hydroxyl group, heterocycle, intramolecular hydrogen, and fluorine. It has been shown to be an effective inhibitor of the HIV protease enzyme in vitro, although it is not active against other enzymes such as the human serum albumin or cytochrome P450. 3-Oxa-7-azabicyclo[3.3.1]nonane binds to the active site of the HIV protease by forming hydrogen bonds with amino acids near the active site and by stabilizing the conformation of its piperidine ring. This drug also has an axial orientation with respect to its fluoroquinolone plane and benzyl group that makes it stereoisomeric with 2 possible configurations: cis or trans.

Versatile small molecule scaffold

Versatile small molecule scaffold

2-(4-Fluorophenyl)acetamide (FFAA) is a broad-spectrum antiviral drug that has been evaluated against picornavirus, enterovirus, and rhinovirus. FFAA has been shown to be effective in the treatment of acute enterovirus infections in mice. This compound was also found to have a cytopathic effect on cells infected with enteroviruses in culture. It binds to the virus's RNA-dependent RNA polymerase and prevents viral replication. FFAA is not active against influenza A or B viruses, but it is active against influenza C virus. This compound has also been found to have medicinal properties, as it can inhibit the growth of human lung cancer cells in culture and may be useful for treating cancers such as leukemia.

Versatile small molecule scaffold

Versatile small molecule scaffold

Versatile small molecule scaffold

Versatile small molecule scaffold

Versatile small molecule scaffold

2H-1,2,4-Benzothiadiazine-1,1-dione is a pharmaceutical agent that belongs to the group of benzothiadiazine compounds. It is used as an intermediate in the synthesis of other drugs and has antihypertensive activity. 2H-1,2,4-Benzothiadiazine-1,1-dione inhibits blood pressure by acting on alpha receptors in vascular smooth muscle cells to inhibit the release of nitric oxide. This drug also blocks the binding of angiotensin II to its receptors and thus reduces the production of aldosterone and other hormones that promote sodium retention. Benzothiadiazine compounds are also known for their ability to form tautomers and isomers with each other. One such example is 2H-1,2,4-benzothiadiazine-1,1-dione (TBDT).

Versatile small molecule scaffold

Versatile small molecule scaffold

3,3,3-Trifluoro-2-methylpropanoic acid is a racemic mixture of 3,3,3-trifluoro-2-methylpropanoic acid and its enantiomer. It is an organic compound that is used as a reagent in organic synthesis. It has the property of being hydrolyzed by lipase mediated by hydrolytic enzymes to form 3,3,3-trifluoroethanol and propanoic acid. The enantiomers are racemic mixtures of 3,3,3-trifluoropropionic acid and (R)-(+)-3,3,3-trifluoropropionic acid. Both enantiomers have the same chemical properties but their kinetic behavior differs because one is a substrate for lipase while the other is not.

Versatile small molecule scaffold

3-Fluoronaphthalene-2-carboxylic acid is a nitrile that is derivatized with carboxylic acid, amide, and benzimidazole. It has been shown to be reactive toward radical, carbonyl, halide, and imidoester. 3-Fluoronaphthalene-2-carboxylic acid can also be used in the synthesis of 3-(3'-fluoro)benzoxazinones and related compounds.

Versatile small molecule scaffold

Versatile small molecule scaffold

2,2,2-Trichloroethyl chlorosulfate is an organic compound that has a hydroxyl group and a chlorine in its structure. It is cytotoxic to cells and causes health effects in humans. This compound binds to the p-coumaric acid in the cell and inhibits the enzyme activity of the demethylase, which is responsible for the oxidation of p-coumaric acid to ferulic acid. This prevents p-coumaric acid from being converted into other metabolites such as dihydroferulic acid and dihydrocaffeic acid. 2,2,2-Trichloroethyl chlorosulfate also inhibits enzymes involved in the synthesis of cholesterol by competitively inhibiting HMG CoA reductase.