88940-56-1

Upstream product

• 4595-59-9 5-bromopyrimidine 
• 927-74-2 3-Butyn-1-ol 

Downstream Products

• 88940-78-7 4-(5-pyrimidinyl)butyl chloride 
• 260441-11-0 4-(5-pyrimidyl)butyraldehyde 

Relevant academic research and scientific papers

Discovery of Potent Human Glutaminyl Cyclase Inhibitors as Anti-Alzheimer’s Agents Based on Rational Design

Glutaminyl cyclase (QC) has been implicated in the formation of toxic amyloid plaques by generating the N-terminal pyroglutamate of β-amyloid peptides (pGlu-Aβ) and thus may participate in the pathogenesis of Alzheimer’s disease (AD). We designed a library of glutamyl cyclase (QC) inhibitors based on the proposed binding mode of the preferred substrate, Aβ3E?42. An in vitro structure-activity relationship study identified several excellent QC inhibitors demonstrating 5- to 40-fold increases in potency compared to a known QC inhibitor. When tested in mouse models of AD, compound 212 significantly reduced the brain concentrations of pyroform Aβ and total Aβ and restored cognitive functions. This potent Aβ-lowering effect was achieved by incorporating an additional binding region into our previously established pharmacophoric model, resulting in strong interactions with the carboxylate group of Glu327 in the QC binding site. Our study offers useful insights in designing novel QC inhibitors as a potential treatment option for AD.

Synthesis and preliminary pharmacological evaluation of 4′-arylalkyl analogues of clozapine. IV. the effects of aromaticity and isosteric replacement

We report the synthesis and preliminary pharmacological activity of a new series of tricyclic analogues of clozapine as potential antipsychotic agents for the treatment of schizophrenia. These compounds were designed based on a revised structural model, a

Sonogashira cross-coupling reactions with heteroaryl halides in the presence of a tetraphosphine-palladium catalyst

Heteroaryl halides undergoes cross-couplings with alkynes in good yields in the presence of [PdCl(C3H5)]2/cis,cis,cis-1,2, 3,4-tetrakis(diphenylphosphinomethyl)cyclopentane as catalyst. A variety of heteroaryl halides such as pyridines, quinolines, a pyrimidine, an indole, a thiophene, or a thiazole have been used successfully. The reaction also tolerates several alkynes such as phenylacetylene and a range of alk-1-ynols. Furthermore, this catalyst can be used at low loading with some substrates.

Heterocyclic derivatives of 2-(3,5-dimethylphenyl)tryptamine as GnRH receptor antagonists

A series of heterocyclic 2-(3,5-dimethylphenyl)tryptamine derivatives was prepared and evaluated on a rat gonadotropin releasing hormone receptor assay. The carbon tether length and heterocyclic ring attached to the amino group of 2-(3,5-dimethylphenyl)tr

Lactol PAF antagonists

The invention encompasses compounds of general formula I: STR1 wherein W represents an imidazo[4,5-c]pyridyl group, optionally substituted with one or more substituents selected from C1 -C6 alkyl, C1 -C6 alkoxy, halo, CF, and CN; and Z, R1, R2, R3, R4, R5, R6 are variables. These compounds are useful as antagonists of platelet activating factor.

N-(Heterocyclic alkyl)pyridoquinazoline-8-carboxamides as Orally Active Antiallergy Agents

A series of N-(heterocyclic alkyl)pyridoquinazoline-8-carboxamides were evaluated for their ability to antagonize slow-reacting substance of anaphylaxis (SRS-A) induced contractions of guinea pig ilea and to inhibit thromboxane synthase in vitro.The results indicated that those pyridoquinazoline-8-carboxamides bearing a branched-chain alkyl moiety in the 2-position and a four to six atom linear chain between a 3- or 4-substituted pyridine or a 1-substituted imidazole ring and the carboxamide nitrogen atom showed the best combination of potencies in the two assays.Several of these compounds were found to be orally active inhibitors of LTE4-induced bronchoconstriction in the guinea pig and LTE4-induced skin wheal formation in the rat.One of the most potent analogues, 2-(1-methylethyl)-N-(1H-imidazol-1-ylbutyl)-11-oxo-11H-pyridoquinazoline-8-carboxamide (36), was selected for extensive pharmacological investigation.It was found that this compound was not a specific inhibitor of LTE4-induced symptomatology, but exhibited more general activity by inhibiting bronchospasm in guinea pigs induced by LTC4, LTD4, PAF, and histamine and skin wheal formation in rats and guinea pigs induced by LTC4, LTD4, and PAF.In addition, 36 was orally active in the passive cutaneous anaphylaxis assay, suggesting that it also exhibits mediator release inhibitory activity.On the basis of the overall pharmacological profile of 36 and its closely related analogues, it was concluded that these compounds may be useful for the treatment of asthma.