125707-22-4Relevant academic research and scientific papers
Structure-Activity Relationships of N-Acyl Pyrroloquinolone PDE-5 Inhibitors
Lanter, James C.,Sui, Zhihua,Macielag, Mark J.,Fiordeliso, James J.,Jiang, Weiqin,Qiu, Yuhong,Bhattacharjee, Sheela,Kraft, Patricia,John, T. Mathew,Haynes-Johnson, Donna,Craig, Elizabeth,Clancy, Joanna
, p. 656 - 662 (2004)
The discovery of the potent and selective PDE-5 inhibitory activity of a pyrroloquinolone scaffold prompted us to explore the SAR of its acyl derivatives. During the course of these studies, three structural series were found with Ki values for
Furoyl and benzofuroyl pyrroloquinolones as potent and selective PDE5 inhibitors for treatment of erectile dysfunction
Jiang, Weiqin,Sui, Zhihua,Macielag, Mark J.,Walsh, Shawn P.,Fiordeliso, James J.,Lanter, James C.,Guan, Jihua,Qiu, Yuhong,Kraft, Patricia,Bhattacharjee, Sheela,Craig, Elizabeth,Haynes-Johnson, Donna,John, T. Matthew,Clancy, Joanna
, p. 441 - 444 (2007/10/03)
Synthesis of furoyl and benzofuroyl pyrroloquinolones as potent and selective PDE5 inhibitors was reported. Their in vitro potencies in inhibiting PDE5 and selectivity in inhibiting other PDE isozymes (PDE1-4 and PDE6) were evaluated. Some of these compounds are more potent than sildenafil with better selectivity toward PDE1 and PDE6. Incorporation of solublizing groups resulted in bioavailable analogues. Selected compounds showed in vivo efficacy in anesthetized dog model for penile erection.
Potassium superoxide as an alternative reagent for Winterfeldt oxidation of beta-carbolines.
Jiang, Weiqin,Zhang, Xuqing,Sui, Zhihua
, p. 43 - 46 (2007/10/03)
Potassium superoxide was examined as an alternative oxidation reagent for the Winterfeldt reaction. KO(2) was found to be superior to the original Winterfeldt protocol for base-sensitive substrates. [reaction--see text]
SUBSTITUTED PYRROLOPYRIDINONE DERIVATIVES USEFUL AS PHOSPHODIESTERASE INHIBITORS
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, (2008/06/13)
The invention relates to novel pyrrolopyridinone derivatives of the formula (I) or (II): pharmaceutical compositions containing the compounds and their use for the treatment of sexual dysfunction
