68535-53-5Relevant academic research and scientific papers
Synthesis of aryl-substituted or aryl-fused N-hydroxyethyl and N-hydroxymethypyrazole derivatives as potential ligands for the estrogen receptor
Allahyari-Devin, Maryam,Abedi, Behnam,Navidpour, Latifeh,Shafiee, Abbas
, p. 43 - 53 (2013/02/25)
A new series of N-hydroxyethylpyrazole (12a-f) and N-hydroxymethylpyrazole derivatives (15a-f) were designed for their estrogenic activities, having a 11.0 ± 0.5 A distance between their two hydroxyl groups, aliphatic-OH and phenolic-OH similar to 17β-estradiol (E2) as an endogenous hormone. To synthesize the title compounds, the key intermediate 1,3-dicarbonyl derivatives (2 and 8), were treated with hydrazine hydrate to produce the pyrazole ring 5 and 9. Further hydroxyalkylation of the latter produced the title pyrazoles. The position of hydroxyethyl or hydroxymethyl substituents in the products was determined through 2D NOE NMR spectroscopy.
Synthesis and analgesic-antiinflammatory activity of some 4- and 5-substituted heteroarylsalicylic acids
Jones,Fordice,Greenwald,Hannah,Jacobs,Ruyle,Walford,Shen
, p. 1100 - 1104 (2007/10/05)
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.
