51746-87-3

Usage

Uses

Used in Pharmaceutical and Agrochemical Industries:
4-(1H-Imidazol-4-yl)-pyridine is used as a building block for the synthesis of pharmaceuticals and agrochemicals due to its versatile chemical structure and ability to modulate biological targets.
Used in Medicinal Chemistry:
4-(1H-Imidazol-4-yl)-pyridine is utilized as a compound in medicinal chemistry for its potential to interact with various receptors and enzymes, contributing to the development of new therapeutic agents.
Used in Drug Discovery:
I4P is employed in drug discovery processes for its pharmacological properties, which include potential applications in the treatment of various diseases through modulation of biological targets.
Used in Antifungal and Antibacterial Applications:
4-(1H-Imidazol-4-yl)-pyridine is used as an antifungal and antibacterial agent, leveraging its inherent activities against fungi and bacteria, making it a promising candidate for the development of new antimicrobial drugs.

Upstream product

• 71759-89-2 4-iodoimidazole 
• 1692-15-5 4-pyridylboronic acid 
• 167897-36-1 2-(4-pyridyl)-2,2-dimethoxyethylamine dihydrochloride 
• 73286-33-6 4-(α-aminoacetyl)pyridine dihydrochloride 
• 167897-35-0 4-(4-pyridyl)imidazole-2-thione hydrochloride 

Relevant academic research and scientific papers

A convenient synthesis of 4(5)-(hetero)aryl-1H-imidazoles via microwave-assisted Suzuki-Miyaura cross-coupling reaction

A simple and rapid access to a variety of 4(5)-arylated imidazoles via palladium-catalyzed Suzuki-Miyaura cross-coupling reaction is described. Coupling parameters were screened for efficient C-4 arylation of N-unprotected 4-iodoimidazole with a broad range of boronic acids under microwave irradiation. Twenty-one imidazole derivatives were synthesized in modest to excellent yields in short reaction times.

IMIDAZOLE DERIVATIVES AS IDO INHIBITORS

Presently provided are IDO inhibitors of general formulae (VII), (VIII) as shown below and pharmaceutical compositions thereof, useful for modulating an activity of indoleamine 2,3-dioxygenase; treating indoleamine 2,3-dioxygenase (IDO) mediated immunosuppression; treating a medical conditions that benefit from the inhibition of enzymatic activity of indoleamine-2,3-dioxygenase; enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent; treating tumor-specific immunosuppression associated with cancer; and treating immunosupression associated with an infectious disease.

Design of potent non-thiourea H3-receptor histamine antagonists

Starting from thioperamide, the first potent and selective H3-receptor histamine antagonist, analogues have been synthesized and tested in vitro on rat cerebral cortex to explore structure-activity relationships. The aim has been to design potent compounds which do not possess the thiourea group of thioperamide and which may have improved brain penetration. In a short series of open chain thiourea analogues, the optimum chain length for H3- antagonist potency was found to be (CH2)3. Compounds derived from histamine and possessing an aromatic nitrogen-containing heterocycle on the side chain amino group in place of thiourea show H3-antagonist activity. Furthermore, when the heterocycle is 2-pyridyl, electron-withdrawing substituents (e.g. NO2, CF3, CO2Me) in the pyridine 5-position increased potency. The synthesis of 4-[4(5)-imidazolyl]piperidine and its conversion into the (trifluoromethyl)pyridyl analogue 5b of thioperamide is described; however, 5b is not as potent as thioperamide. Replacing imidazole by pyridine or substituting imidazole on the remote N considerably reduced potency. Replacing the side-chain NH by S increased potency still further and the most potent compound is 2-{[2-[4(5)-imidazolyl]ethyl]thio}-5-nitropyridine (UCL 1199) which has K(i) = 4.8 nM.

Process for the preparation of intermediates useful for the synthesis of histamine receptor antagonists

The present invention relates to a novel process for the preparation of highly potent histamine receptor antagonists, in particular histamine H 3 receptor antagonists. Also disclosed is a novel process for the preparation of intermediates useful in the preparation of histamine receptor antagonists, in particular H 3 -receptor antagonists.

Piperidine derivatives, their preparation and their therapeutic application

A compound which is a piperidine derivative of general formula (I) STR1 in which R 1 represents a hydrogen atom, a linear or branched (C 1-6)alkyl group or a cyclo(C 3-8)alkyl group, X represents an oxygen atom, a sulphur atom or a group of general formul