99187-39-0

Upstream product

• 35191-43-6 1-(4-bromo-butyl)-4-methoxy-benzene 
• 288-32-4 1H-imidazole 
• 86223-05-4 4-(4-hydroxyphenyl)butanol 
• 3673-69-6 4-(3,5-di-tert-butyl-4-hydroxyphenyl)butanol 
• 4521-28-2 4-(4-Methoxyphenyl)butyric acid 
• 52244-70-9 4-(4-methoxyphenyl)butan-1-ol 
• 457606-31-4 4-(4-(benzyloxy)phenyl)but-3-yn-1-ol 
• 19578-68-8 4-(4-benzyloxyphenyl) iodide 
• 457606-32-5 4-(4-benzyloxyphenyl)but-3-ynyl bromide 

Relevant academic research and scientific papers

Interaction of functionally-substituted 4-alkyl-2,6-di-tert-butylphenols with hydrohalic acids

Reactions of 4-alkyl-2,6-di-tert-butylphenols containing OH, SH, COOH, and COOMe groups in their para substituents with hydrogen chloride and hydrohalic acids were studied. One-step transformations of 2,6-di-tert-butyl-4-(ω- hydroxyalkyl)phenols to the corresponding 4-(ω-halogenoalkyl)phenols, as well as of 3-(3,5-di-tert-butyl-4-hydroxyphenyl)propionic acid and its esters to phloretic acid were proposed. 4-(3-Mercaptopropyl)phenol upon heating with conc. HBr undergoes condensation to 3-(4-hydroxyphenyl)propyl 4-(3-mercaptopropyl)phenyl sulfide as the main product.

Synthesis of ketone analogues of prolyl and pipecolyl ester FKBP12 ligands

The recently discovered small-molecule ligands for the peptidyl and prolyl isomerases (PPIase) of FKBP12 have been shown to possess powerful neuroprotective and neuroregenerative effects. Ketone analogues of the prolyl and pipecolyl esters, which mimic on

NOVEL COMPOUNDS USEFUL AS NEURO-PROTECTIVE AGENTS

This invention relates to novel phenyl oxazoles, thiazoles, oxazolines, oxadiazoles and benzoxazoles useful as neuro-protective agents.

Synthesis of N-substituted 4-(4-hydroxyphenyl)piperidines, 4-(4- hydroxybenzyl)piperidines, and (±)-3-(4-hydroxyphenyl)pyrrolidines: Selective antagonists at the 1A/2B NMDA receptor subtype

Antagonists at the 1A/2B subtype of the NMDA receptor (NR1A/2B) are typically small molecules that consist of a 4-benzyl- or a 4-phenylpiperidine with an ω-phenylalkyl substituent on the heterocyclic nitrogen. Many of these antagonists, for example ifenprodil (1), incorporate a 4-hydroxy substituent on the ω-phenyl group. In this study, the position of this 4- hydroxy substituent was transferred from the ω-phenyl group to the benzyl or phenyl group located on the 4-position of the piperidine ring. Analogues incorporating pyrrolidine in lieu of piperidine were also prepared. Electrical recordings using cloned receptors expressed in Xenopus oocytes show that high-potency antagonists at the NR1A/2B subtype are obtained employing N-(ω-phenylalkyl)-substituted 4-(4-hydroxyphenyl)piperidine, 4-(4- hydroxybenzyl)piperidine, and (±)3-(4-hydroxyphenyl)pyrrolidine as exemplified by 21 (IC50 = 0.022 μM), 33 (IC50 = 0.059 μM), and 40 (IC50 = 0.017 μM), respectively. These high-potency antagonists are > 1000 times more potent at the NR1A/2B subtype than at either the NR1A/2A or NR1A/2C subtypes. The binding affinities of 21 at α1-adrenergic receptors ([3H]prazosin, IC50 = 0.54 μM) and dopamine D2 receptors ([3H]raclopride, IC50 = 1.2 μM) are reduced by incorporating a hydroxy group onto the 4-position of the piperidine ring and the β-carbon of the N- alkyl spacer to give (±)-27: IC50 NR1A/2B, 0.026; α1, 14; D2, 105 μM. The high-potency phenolic antagonist 21 and its low-potency O-methylated analogue 18 are both potent anticonvulsants in a mouse maximal electroshock- induced seizure (MES) study (ED50 (iv) = 0.23 and 0.56 mg/kg, respectively). These data indicate that such compounds penetrate the blood- brain barrier but their MES activity may not be related to NMDA receptor antagonism.

Compounds useful as neuro-protective agents

This invention relates to novel phenyl oxazoles, thiazoles, oxazolines, oxadiazoles and benzoxazoles useful as neuro-protective agents.

Structure-activity relationship for a series of 2-substituted 1,2,3,4- tetrahydro-9H-pyrido[3,4-b]indoles: Potent subtype-selective inhibitors of N- methyl-D-aspartate (NMDA) receptors

A series of 2-substituted 1,2,3,4-tetrahydro-9H-pyrido[3,4-b]indoles was synthesized as potential antagonists for the NR1(A)/2B subtype of N-methyl- D-aspartate (NMDA) receptors. Assayed by electrical recording under steady- state conditions, 7-hydroxy-2-(4-phenylbutyl)-1,2,3,4-tetrahydropyrido-[3,4- b]indole (30) was the most potent compound in the series having an IC50 value of 50 nM at the NR1(A)/2B receptors.

Method for treating pain

The present invention provides a method for treating pain using a composition comprising certain phenyl oxazoles or phenyl thiazoles in combination with a Drug Useful in the Treatment of Pain.

Method for treating neuropathic pain

The present invention provides a method for treating neuropathic pain comprising administering an analgesic dosage of a compound of formula I to an animal in need of such treatment certain phenyl oxazoles or phenyl thiazoles.

Use of phenyl oxazole or phenyl thiazole derivatives for treating neuropathic pain

The present invention provides a method for treating neuropathic pain comprising administering an analgesic dosage of a compound of formula I to an animal in need of such treatment certain phenyl oxazoles or phenyl thiazoles.

Use of phenyl oxazole or phenyl thiazole derivatives for treating pain

The present invention provides a method for treating pain comprising administering to an animal in need of such treatment, an analgesic dosage of certain phenyl oxazoles or phenyl thiazoles.