Building Blocks

<p>Versatile small molecule scaffold</p>

<p>6-Amino-[1,2,4]triazolo[1,5-a]pyridine is a drug that binds to the acetylcholine receptor and blocks the action of acetylcholine. It is used in psychiatry to treat dysfunction. 6-Amino-[1,2,4]triazolo[1,5-a]pyridine may also be used as an adjunct treatment for psychiatric disorders such as schizophrenia or depression. The drug has been shown to have allosteric properties in the muscarinic acetylcholine receptor and has been demonstrated to be a modulator at this site. 6-Amino-[1,2,4]triazolo[1,5-a]pyridine may also act on the muscarinic acetylcholine receptors in the central nervous system by blocking acetylcholine binding.</p>

<p>Versatile small molecule scaffold</p>

<p>Versatile small molecule scaffold</p>

<p>Versatile small molecule scaffold</p>

<p>Versatile small molecule scaffold</p>

<p>Versatile small molecule scaffold</p>

<p>Versatile small molecule scaffold</p>

<p>2,4-Dimethoxyphenyl isothiocyanate (DMITC) is a molecule that has been shown to have pro-apoptotic activity against human colorectal carcinoma cells. It also inhibits the growth of the colon cancer cells by inducing apoptosis. DMITC has been shown to inhibit the synthesis of DNA and RNA in a dose-dependent manner. This molecule is efficiently synthesized by reacting an imine with an isothiocyanate. DMITC has cytometric analysis for mechanistic studies and can be used as a chemotherapeutic agent for cancer treatment.</p>

<p>Dicyclohexylmethanol is a trifunctional compound that contains a hydroxyl group, and can be used as a hydrogen bond donor or acceptor. The chemical structure of dicyclohexylmethanol can be seen in the figure below. Dicyclohexylmethanol has been used for sample preparation for hydrogen chloride gas. It has also been used to determine the concentration of blood ethanol levels and to measure blood pH in humans. Dicyclohexylmethanol is an important reactant in asymmetric synthesis reactions due to its ability to form hydrogen bonds with both reactants.</p>

<p>Versatile small molecule scaffold</p>

<p>3-(Hydroxymethyl)cyclobutan-1-one is a synthetic piperazine derivative that has been shown to have antitumor and antimycobacterial activities. It is a selective inhibitor of the enzyme purine nucleoside phosphorylase (PNP), which catalyzes the conversion of inosine monophosphate (IMP) to xanthosine monophosphate (XMP). This inhibition results in an accumulation of IMP and deoxyinosine monophosphate (dIMP) in tumor cells. 3-(Hydroxymethyl)cyclobutan-1-one also inhibits Mycobacterium tuberculosis, but not other bacteria such as Escherichia coli or Staphylococcus aureus. The product is synthetically produced by reacting cyclobutanone with hydroxylamine.</p>

<p>Versatile small molecule scaffold</p>

<p>Versatile small molecule scaffold</p>

<p>Versatile small molecule scaffold</p>

<p>Versatile small molecule scaffold</p>

<p>2-Cyano-5-fluorophenol is an organic compound that is used as a precursor to medicines and other chemicals. It reacts with calcium hydroxide in water to form 2-cyano-5-hydroxyfluorobenzene, which can be hydrolyzed to form 2-cyano-5-chlorofluorobenzene. This compound can also react with sodium hydroxide to produce sodium cyanate, which can be hydrolyzed to form sodium chloride and hydrogen cyanide gas. The alkali metal ions are needed for this reaction, which is why the product should not be exposed to water or moisture. 2-Cyano-5-fluorophenol has been shown to have liquid crystal properties and is used in the production of certain types of polymers. 2Cyano-5Fluorophenol crystals are also used in some medicines such as acetaminophen (paracetamol).</p>

<p>2-Bromo-3,3,3-trifluoro-1-propene is a chemical compound that has been synthesized in an asymmetric reaction. The reactant is bromopropane and the product is 2,2,2-trifluoropropene. The methylene group on the propene molecule is activated by the nucleophilic attack of a fluoride ion from hydrogen fluoride to form a cavity with a highly strained bond. The kinetic study of this reaction revealed that the activation energy for the reaction is 42 kJ/mol. Palladium-catalyzed coupling reactions are catalyzed by palladium and require nonpolar solvents such as toluene or dichloromethane. This type of reaction has been shown to be exothermic with an isolated yield of 1%.</p>

<p>Versatile small molecule scaffold</p>

<p>Tri-GalNAc-NHS ester is a multivalent molecule composed of three GalNAc cluster arms. It is a protein degrader and a ligand of the asialoglycoprotein receptor (ASGPR) used for the development of targeted therapies for liver diseases. The GalNAc arms enable high-affinity binding to the ASGPR on hepatocyte surfaces. The crucial functional group, N-hydroxysuccinimide (NHS) ester, is known for its ease of conjugation with various biomolecules possessing amine (NH2) groups. This biocompatible reaction strategy allows the design and development of targeted conjugates such as drug-GalNAc conjugates, siRNA delivery vehicles, or probes for ASGPR imaging in the liver.</p>