75986-77-5

Upstream product

• 917-64-6 methyl magnesium iodide 
• 75986-15-1 4-Pyridin-3-ylmethyl-benzaldehyde 
• 75986-14-0 4-(3-pyridylmethyl)benzaldehyde diethyl acetal 
• 133292-05-4 4-(diethoxymethyl)phenylmagnesium bromide 
• 6959-48-4 3-chloromethylpyridinium chloride 

Downstream Products

• 75986-30-0 1-acetyl-4-(pyridin-3-ylmethyl)benzene 
• 75986-49-1 (E)-3-[4-(pyridin-3-ylmethyl)phenyl]-2-butenoic acid ethyl ester 
• 75987-34-7 (E)-3-<4-(pyridylmethyl)phenyl>-2-butenoic acid 

Relevant academic research and scientific papers

Highly Selective Inhibitors of Thromboxane Synthetase. 2. Pyridine Derivatives

The enzyme thromboxane (TX) synthetase is inhibited by pyridine.The β-substituted pyridine derivatives showed higher inhibitory potency than γ-substituted ones having the side chain.Among the β-substituted derivatives containing the ω-carboxyalkyl group, the compounds with 6-8 carbon atoms in the side chain were especially effective.The derivatives holding the phenylene group in the side chain exhibited much higher inhibitory activity than those of the alkylene type.Among them, (E)-3--2-methylacrylic acid hydrochloride (5a) had the highest potency (IC50 = 3*10-9 M).The β-substituted pyridine derivatives and 1-substituted imidazole derivatives which had the same side chain showed almost the same potency.The β-substituted pyridine derivatives do not inhibit arachidonic acid cyclooxygenase or prostaglandin I2 synthetase, two other enzymes of the arachidonic cascade.

Pyridine derivatives

The pyridine derivatives of the general formula: STR1 [wherein A represents an alkylene group containing from 1 to 5 carbon atoms unsubstituted or substituted by a hydroxy group, B represents a single bond, or an oxygen or sulphur atom, or an alkylene group containing from 1 to 5 carbon atoms, D represents a single bond, or an alkylene group containing from 1 to 5 carbon atoms, R represents a grouping of the formula: STR2 (in which R6 represents a hydrogen atom, or an alkyl group containing from 1 to 4 carbon atoms), Z represents a single bond, or an ethynylene group, or a grouping of the formula: STR3 in which R2 represents a hydrogen atom, or an alkyl group containing from 1 to 4 carbon atoms, R3 represents a hydrogen, bromine or chlorine atom, or an alkyl group containing from 1 to 4 carbom atoms; the symbol represents a single or double bond, the carbon atom attached to R2 binds to B, and the carbon atom attached to R3 binds to D, R1 represents a hydroxy group, or a grouping of the formula: --COOR4 or --COSR4, in which R4 represents a hydrogen atom, or an alkyl group containing from 1 to 12 carbon atoms, or an aralkyl group containing from 7 to 13 carbon atoms, or a cycloalkyl group containing from 4 to 7 carbon atoms unsubstituted or substituted by at least one alkyl group containing from 1 to 4 carbon atoms, or a phenyl unsubstituted or substituted by at least one halogen atom, trifluoromethyl group, alkyl or alkoxy or alkylthio group containing from 1 to 4 carbon atoms, nitro or phenyl group, R5 represents a hydrogen atom, or an alkyl group containing from 1 to 4 carbon atoms, with the proviso that, when B represents an oxygen or sulphur atom, Z represents a single bond and D represents an alkylene group containing from 1 to 5 carbon atoms], and non-toxic acid addition salts thereof and, when R1 represents a carboxy or thiocarboxy group, non-toxic salts thereof, possess a strong inhibitory activity on thromboxane synthetase from rabbit platelet microsomes, and are useful as therapeutically active agents in the prevention or treatment of inflammation, hypertension, thrombus, cerebral apoplexy, asthma, myocardial infarction, cardiostenosis, cerebral infarction and acute cardiac death.