Building Blocks

Versatile small molecule scaffold

4-Aminobenzene-1,2-diol hydrochloride (4ABAH) is a cox-2 inhibitor that has been shown to inhibit the activity of human cell factor and x-ray diffraction data. It has also been shown to possess anti-inflammatory properties by inhibiting the production of prostaglandins. The prodrug ester hydrochloride is converted to 4ABAH in vivo and undergoes hydrolysis by esterases to release 4ABAH. This conversion may be limited by the rate constant, which may decrease with time due to enzyme inactivation or competition with other substrates. 4ABAH inhibits cell proliferation in carcinoma cell lines, but not in normal cells. The drug is water soluble and therefore can be administered orally or intravenously.

9-Azabicyclo[6.2.0]decan-10-one is a lactam that can be synthesized by reacting diisopropyl with β-amino acid. 9-Azabicyclo[6.2.0]decan-10-one has been shown to have high enantioselectivity and enantiopurity, which is due to the use of a chiral catalyst in the synthesis process. This compound is also an intermediate for the synthesis of β-lactams such as penicillin, cephalosporin, and carbapenem antibiotics, which are used to treat bacterial infections. The enzymes in these β-lactams are inhibited by binding to their active site, preventing them from breaking down peptidoglycan during cell wall synthesis.

2-Bromobenzaldehyde (2BA) is a reactive chemical that can be used as a building block for the synthesis of many other chemicals. It is also an efficient catalyst for reactions such as the reduction of amines to amides, and the conversion of nitroarenes to amines. 2BA has been shown to be cytotoxic in vitro and in vivo against human cancer cell lines when attached to magnetic nanoparticles and immobilized on different surfaces. The cytotoxic activity of 2BA was analyzed by using intramolecular cycloaddition reactions with electron-deficient olefins, which led to valuable insights into the mechanism of this reaction.

5-Methyl-1H-pyrrolo[3,2-b]pyridine is a versatile compound that has various applications in different industries. It is commonly used in the production of polyvinyl and interferon, as well as in the synthesis of glycine and glutamate. This compound also finds its use in biomass production, where it acts as a catalyst for the growth of nanofibers. Additionally, 5-Methyl-1H-pyrrolo[3,2-b]pyridine has been studied for its potential therapeutic properties, including its ability to inhibit cytochalasin activity and the synthesis of oligosaccharides. Its unique chemical structure also makes it suitable for the development of copolymers and styrenic electrode materials.

Sildenafil is a drug that is used for the treatment of erectile dysfunction. It belongs to the class of phosphodiesterase inhibitors and inhibits the enzyme phosphodiesterase type 5 (PDE-5). This enzyme functions to breakdown cyclic guanosine monophosphate (cGMP), which causes blood vessels in the penis to relax, leading to an erection. Sildenafil has been shown to be well tolerated with oral bioavailability of more than 70%. Sildenafil can be taken orally, but has also been studied for pulmonary administration. The pharmacokinetic properties of sildenafil have been optimized for oral administration in humans and it has been shown that sildenafil does not inhibit human liver cytochrome P450 enzymes. Sildenafil also shows inhibitory potency against other phosphodiesterases such as PDE-2, PDE-3, and PDE-6.

Versatile small molecule scaffold

Versatile small molecule scaffold

Versatile small molecule scaffold

N2,N2-Dimethylpyridine-2,5-diamine is a gadolinium complex that is used as a contrast agent in magnetic resonance imaging. N2,N2-Dimethylpyridine-2,5-diamine has been shown to be effective in the treatment of cancers and can be used for both diagnostic and therapeutic purposes. The drug can be conjugated with monoclonal antibodies or other drugs to target specific cancer cells. It can also be used to monitor the effectiveness of chemotherapy treatments. The salt form of this drug is soluble in water and stable at acid pH levels. When administered intravenously, it has a high degree of biodistribution and is excreted through the kidneys.

Versatile small molecule scaffold

2-Chloro-3-nitroimidazo[1,2-a]pyridine is a chlorinated derivative of imidazo[1,2-a]pyridine. The nitro group gives the molecule two sites for functionalization and enables it to undergo Suzuki coupling reactions with anilines. The chloro substituent provides the molecule with a high degree of chemical diversity. This compound can be used in cross-coupling reactions with anilines and other heterocycles, such as thiophenes and furans. In addition, this compound has been shown to react with nucleophiles in a nucleophilic substitution reaction to form 2-chloro-5-(substituted)imidazo[1,2-a]pyridinium ions.

Versatile small molecule scaffold

Versatile small molecule scaffold

Versatile small molecule scaffold

Versatile small molecule scaffold

1-Methoxy-4-nitronaphthalene is a yellow crystalline solid that belongs to the group of naphthalenes. It reacts with deionized water to give nitronaphthalene, which can be detected by ultrafast spectroscopy at constant temperature or by second-order rate constants. The nitro group can be reduced to an amine on treatment with phosphite or diphosphorylated. Nitro groups are also susceptible to nucleophilic attack by acetonitrile and ammonium nitrate, and can be photoreduced to the corresponding amino compound.

2-Bibenzylcarboxylic acid is a synthetic retinoid that has been shown to have potent antagonistic effects against the activity of various pro-inflammatory enzymes. It blocks the integrin receptor, which prevents leukocyte adhesion and migration. 2-Bibenzylcarboxylic acid also inhibits protease activity by binding to the active site of the enzyme and preventing substrate binding, as well as dextran sulfate-induced inflammation. 2-Bibenzylcarboxylic acid has been shown to be effective in reducing disease activity in animal models of inflammatory diseases such as rheumatoid arthritis.

Versatile small molecule scaffold