Pharmaceutical Intermediates

Dexamethasone is a fluorinated steroid and synthetic adrenal glucocorticoid which acts as an immunosuppressive and anti-inflammatory agent in pharmaceuticals. It is a corticosteroid hormone receptor agonist to annexin A and glucocorticoid receptors. In cell signaling activity, it regulates the survival, growth, and differentiation of T-cells.

Dexamethasone inhibits multidrug resistance-associated protein (MRP). As an antineoplastic agent, it negatively modulates inducible nitric oxide synthase (iNOS), a molecule highly expressed in tumors. This substance is capable of interfering with NF-kB activation and apoptosis pathways. Dexamethasone can also increase antiemetic or anti-nausea effects of 5-HT3 receptor antagonists and is given to chemotherapy patients to counteract such symptoms.

Medicinally, this chemical is classified with anti-inflammatories. It’s used to treat rheumatic diseases, autoimmune or immunological responses like allergies, asthma, swelling and allergic anaphylactic shock among others. It’s been incorporated into chemotherapy treatment for multiple myeloma. Endocrine and adrenal disorders are also treated with dexamethasone.

Proline and its derivatives are often used as asymmetric catalysts in organic reactions. The CBS reduction and proline catalysed aldol condensation are prominent examples. L-Proline is an osmoprotectant, and therefore is used in many pharmaceutical, biotechnological applications.

Geniposide is a bioactive monosaccharide-derived molecule with a multitude of chemical identities including indoid glycoside, terpene glycoside and β-D-glucoside. It is also considered an enoate ester and cyclopentapyran. As a plant derivative glycoside, it has displayed medicinal properties in neuroprotective, antioxidant, anti-diabetic and anti-proliferative functions.

Geniposide’s neuroprotective and antioxidant qualities have been attributed to its ability to regulate Nrf2 translocation, affecting PI3K/Akt signaling pathway expression of antioxidant protein HO-1. As an agonist to the GLP-1 receptor, it’s demonstrated inhibition of oxidative damage from PC12 cells.

It’s regulation of glucose-stimulated insulin signaling also links it to diabetes and Alzheimer’s disease studies. Geniposide has been observed to up-regulate β-site APP cleaving enzyme (BACE1) and insulin-degrading enzyme (IDE), adversely reducing Aβ1-42 and ADAM10 levels. Geniposide research in correlation with formaldehyde has proved it to be an inhibitor of misfolding and aggregation of Tau protein and β amyloid protein, both characteristics of Alzheimer’s disease.

Glycocholic acid, sodium salt hydrate is an ionic biologic detergent formed through the conjugation of cholic acid with glycine. It is used to measure total bile acids through fluorometric and enzymatic assays. Additionally, it is used to study its effect on testosterone micelle formation and solubilization.

During cell lysis and the extraction of DNA or RNA, denaturing enzymes such as DNase and RNase are released. To prevent DNA or RNA denaturation, the chaotropic agent, Guanadine thiocyanate is the preferred agent for use during cell lysis, and for DNA or RNA extraction. This is because of its strong ability to irreversibly inhibit the activity of DNase and RNase.

Guanadine thiocyanate has also been effective in deactivating enveloped viruses; however, it demonstrates far less effectiveness in nonenveloped viruses.

Histamine dihydrochloride is a hydrophilic amine compound derived through the decarboxylation of histidine by L-histidine decarboxylase. It is a substrate used to assay histamine-N-methyltransferase ion-pair extraction of histamine using HPLC. Additionally, histamine dihydrochloride activates nitric oxide synthase and inhibits formation of reactive oxygen species.

IBA (Indole-3-butyric acid) is a plant hormone belonging to the auxin family and assists in initiating root formation; the in vitro process is called micropropagation. Aside from accelerating root formation, it is used on various crops to stimulate flower development and the growth of fruits. This ultimately increases crop yields.

Historically, products that contained IBA were used to protect plants during transplantation by stimulating root growth and decreasing shock.

Indole-2-Carboxylic Acid is used in Pd-catalyzed cyclization reactions and for the preparation of spirooxindole-pyrrolidones.

Indole-2-carboxylic acid ethyl ester is a reagent involved in the preparation of: CRTH2 receptor antagonists, acetolactate synthase inhibitors, p38 MAP kinase inhibitors, cannabinoid CB1 receptor antagonists, and an anticancer agent against leukemia K562 cells.

Indole-3-acetyl-L-isoleucine is a conjugate of IAA (indole-3-acetic acid) and can be used as a plant growth regulator.

Indole-3-carbinol is an inhibitor of carcinogenesis at the initiation stage. However, it enhances carcinogenesis at the post-initiation stage. Indole-3-carbinol induces cell cycle arrest and additionally blocks cyclin-dependent kinase 6 expression. It has been shown to suppress cell adhesion and migration in vitro.

Indole-3-Carboxylic acid is used to prepare antitumor agents and amino acid derivatives. Additionally, it can be used to synthesize serotonin 5-HT4 and 5-Ht6 receptor antagonists, Very Late Antigen-4 (VLA-4) antagonists, and potential agents against Alzheimer's disease.

Indole-3-carboxylic acid methyl ester is useful in the preparation of: nitric oxide synthase inhibitors, RNA polymerase II inhibitors, Very Late Antigen-4 (VLA-4) inhibitors, serotonin 5-HT4 inhibitors, and protein kinase C alpha inhibitors.

Indole-3-propionamide or IPAM is an antioxidant used to modify mitochondrial metabolism and to decrease reactive oxygen species production. It is cell-permeable.

Through inhibition of superoxide dismutase, IPA has shown to protect against oxidative damage in primary neurons and neuroblastoma cells. IPA has also shown to protect against death caused by exposure to amyloid β-protein in primary neurons and neuroblastoma cells.

L-Arabinose is an arabinose isomer widely found in nature, while D-arabinose is less common. L-Arabinose is a constituent of many biopolymers that make up plant cell walls.

This monosaccharide is often used in cell culture media, serving as a bacterial carbon source, and can be used to distinguish between bacteria based on their fermentation abilities.

L-Arabinose, in the absence of glucose, induces transcription of the ara operon in E. coli that encodes L-arabinose catabolizing enzymes. It does this by binding to the AraC protein and activating the P_BAD promoter. The P_BAD promoter is used in plasmid vectors as a switch for protein expression that can be turned on by L-arabinose or turned off by addition of glucose.

L-Histidinol dihydrochloride is a histamine precursor. It has been shown to reversibly inhibit protein synthesis.

Homocysteine is a cysteine homolog,and only differs by having an additional methylene bridge. It is often used in vitro as a reference to measure L-homocysteine in plasma in order to diagnose homocystinuria. This genetic disorder causes the body to be unable to process certain amino acids.

Higher levels of homocysteine found in the body is due to having vitamin B6 or B12 deficiencies. Finding higher levels may indicate possible cardiovascular disease; however, reducing the levels of homocysteine in the body does not appear to remedy the situation.