148748-01-0

Upstream product

• 874-90-8 4-methoxybenzonitrile 
• 118872-16-5 4-Methoxy-benzimidoyl chloride; hydrochloride 
• 22483-09-6 2,2-dimethoxyethylamine 

Downstream Products

• 1027046-01-0 1-(2,2-Dimethoxy-ethyl)-2-(4-methoxy-phenyl)-6-oxo-1,6-dihydro-pyrimidine-5-carboxylic acid methyl ester 
• 148748-25-8 [1-(2,2-Dimethoxy-ethyl)-2-(4-methoxy-phenyl)-6-oxo-1,6-dihydro-pyrimidin-5-yl]-carbamic acid benzyl ester 
• 148748-41-8 [5-benzyloxycarbonylamino-2-(4-methoxyphenyl)-6-oxo-1,6-dihydro-1-pyrimidinyl]acetic acid 
• 148748-33-8 [5-Benzyloxycarbonylamino-2-(4-methoxyphenyl)-6-oxo-1,6-dihydro-1-pyrimidinyl]acetaldehyde 
• 148748-17-8 1-(2,2-Dimethoxy-ethyl)-2-(4-methoxy-phenyl)-6-oxo-1,6-dihydro-pyrimidine-5-carboxylic acid 

Relevant academic research and scientific papers

Nonpeptidic inhibitors of human leukocyte elastase. 5. Design, synthesis, and X-ray crystallography of a series of orally active 5-aminopyrimidin-6- one-containing trifluoromethyl ketones

The effects of changes in substitution in a series of 5-amino-2- pyrimidin-6-ones on both in vitro activity and oral activity in an acute hemorrhage assay have been explored. These compounds contained either a trifluoromethyl ketone or a boronic acid moiety to bind covalently to the Ser-195 hydroxyl of human leukocyte elastase (HLE). Boronic acid-containing inhibitors were found to be more potent than the corresponding trifluoromethyl ketones in vitro but were less active upon oral administration. Compound 13b was found to offer the best combination of oral potency, duration of action, and enzyme selectivity and, as such, was selected for further biological testing. X-ray crystallography of a cocrystallized complex of compound 19m and porcine pancreatic elastase demonstrated that the inhibitor is bound to the enzyme in a manner similar to that found previously for a closely related series of pyridone-containing inhibitors of HLE.

Synthesis and analgesic-antiinflammatory activity of some 4- and 5-substituted heteroarylsalicylic acids

We have made a series of 4- and 5-aryl- and 4- and 5-heteroarylsalicylic acid derivatives with the objective of reducing gastric irritation and increasing potency. Here we describe a series of 4- and 5-heterocyclic salicylic acids and their antiinflammatory-analgesic potencies measured in comparison to aspirin. An improvement of the therapeutic index over aspirin of 100 was achieved; however, the heterocyclic salicylic acids lacked antipyretic activity. Some physicochemical parameters which may bear on the antiinflammatory activity of these compounds are discussed.