Literature DB >> 11128646

Synthesis and biological evaluation of 2,5-dihydropyrazol.

M I Crespo1, J Gràcia, C Puig, A Vega, J Bou, J Beleta, T Doménech, H Ryder, V Segarra, J M Palacios.   

Abstract

A novel series of 2,5-dihydropyrazolo[4,3-c]quinolin-3-ones has been prepared. These compounds showed good PDE 4 inhibitory activity and weak affinity for rolipram's binding site. They also exhibited a good anti-inflammatory profile without emetic side effects.

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Year:  2000        PMID： 11128646     DOI： 10.1016/s0960-894x(00)00548-5

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  3 in total

1.  Discovery and SAR of muscarinic receptor subtype 1 (M1) allosteric activators from a molecular libraries high throughput screen. Part 1: 2,5-dibenzyl-2H-pyrazolo[4,3-c]quinolin-3(5H)-ones as positive allosteric modulators.

Authors:  Changho Han; Arindam Chatterjee; Meredith J Noetzel; Joseph D Panarese; Emery Smith; Peter Chase; Peter Hodder; Colleen Niswender; P Jeffrey Conn; Craig W Lindsley; Shaun R Stauffer
Journal:  Bioorg Med Chem Lett       Date:  2014-11-18       Impact factor: 2.823

2.  Conformational Restriction Leading to a Selective CB2 Cannabinoid Receptor Agonist Orally Active Against Colitis.

Authors:  Jamal El Bakali; Giulio G Muccioli; Mathilde Body-Malapel; Madjid Djouina; Frédérique Klupsch; Alina Ghinet; Amélie Barczyk; Nicolas Renault; Philippe Chavatte; Pierre Desreumaux; Didier M Lambert; Régis Millet
Journal:  ACS Med Chem Lett       Date:  2014-12-04       Impact factor: 4.345

3.  Synthesis and preliminary structure-activity relationship study of 2-aryl-2H-pyrazolo[4,3-c]quinolin-3-ones as potential checkpoint kinase 1 (Chk1) inhibitors.

Authors:  Ivana Malvacio; Alberto Cuzzolin; Mattia Sturlese; D Mariano A Vera; E Laura Moyano; Stefano Moro
Journal:  J Enzyme Inhib Med Chem       Date:  2017-12       Impact factor: 5.051
  3 in total

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