Literature DB >> 25977593

Evaluation of pyrrolidine and pyrazolone derivatives as inhibitors of trypanosomal phosphodiesterase B1 (TbrPDEB1).

Emanuele Amata1, Nicholas D Bland2, Robert K Campbell2, Michael P Pollastri1.   

Abstract

Human African trypanosomiasis (HAT) is a parasitic disease, caused by the protozoan pathogen Trypanosoma brucei, which affects thousands every year and which is in need of new therapeutics. Herein we report the synthesis and assessment of a series of pyrrolidine and pyrazolone derivatives of human phosphodiesterase 4 (hPDE4) inhibitors for the assessment of their activity against the trypanosomal phosphodiesterase TbrPDEB1. The synthesized compounds showed weak potency against TbrPDEB1.

Entities:  

Keywords:  TbrPDEB1; Trypanosoma brucei; neglected tropical disease; phosphodiesterases

Year:  2015        PMID： 25977593      PMCID： PMC4426996          DOI： 10.1016/j.tetlet.2015.04.061

Source DB:  PubMed          Journal:  Tetrahedron Lett        ISSN： 0040-4039            Impact factor:   2.415


  14 in total

1.  Pharmacological validation of Trypanosoma brucei phosphodiesterases B1 and B2 as druggable targets for African sleeping sickness.

Authors:  Nicholas D Bland; Cuihua Wang; Craig Tallman; Alden E Gustafson; Zhouxi Wang; Trent D Ashton; Stefan O Ochiana; Gregory McAllister; Kristina Cotter; Anna P Fang; Lara Gechijian; Norman Garceau; Rajiv Gangurde; Ron Ortenberg; Mary Jo Ondrechen; Robert K Campbell; Michael P Pollastri
Journal:  J Med Chem       Date:  2011-11-08       Impact factor: 7.446

2.  Novel potent and selective σ ligands: evaluation of their agonist and antagonist properties.

Authors:  Agostino Marrazzo; Enrique J Cobos; Carmela Parenti; Giuseppina Aricò; Giuseppina Marrazzo; Simone Ronsisvalle; Lorella Pasquinucci; Orazio Prezzavento; Nicola A Colabufo; Marialessandra Contino; Luis G González; Giovanna M Scoto; Giuseppe Ronsisvalle
Journal:  J Med Chem       Date:  2011-04-21       Impact factor: 7.446

3.  Repurposing human PDE4 inhibitors for neglected tropical diseases: design, synthesis and evaluation of cilomilast analogues as Trypanosoma brucei PDEB1 inhibitors.

Authors:  Emanuele Amata; Nicholas D Bland; Charles T Hoyt; Luca Settimo; Robert K Campbell; Michael P Pollastri
Journal:  Bioorg Med Chem Lett       Date:  2014-07-30       Impact factor: 2.823

4.  Target repurposing for neglected diseases.

Authors:  Michael P Pollastri; Robert K Campbell
Journal:  Future Med Chem       Date:  2011-08       Impact factor: 3.808

5.  The Trypanosoma brucei cAMP phosphodiesterases TbrPDEB1 and TbrPDEB2: flagellar enzymes that are essential for parasite virulence.

Authors:  Michael Oberholzer; Gabriela Marti; Mario Baresic; Stefan Kunz; Andrew Hemphill; Thomas Seebeck
Journal:  FASEB J       Date:  2006-12-13       Impact factor: 5.191

6.  Synthesis and assessment of catechol diether compounds as inhibitors of trypanosomal phosphodiesterase B1 (TbrPDEB1).

Authors:  Jennifer L Woodring; Nicholas D Bland; Stefan O Ochiana; Robert K Campbell; Michael P Pollastri
Journal:  Bioorg Med Chem Lett       Date:  2013-08-21       Impact factor: 2.823

7.  Pharmacokinetic optimization of class-selective histone deacetylase inhibitors and identification of associated candidate predictive biomarkers of hepatocellular carcinoma tumor response.

Authors:  Jason C Wong; Guozhi Tang; Xihan Wu; Chungen Liang; Zhenshan Zhang; Lei Guo; Zhenghong Peng; Weixing Zhang; Xianfeng Lin; Zhanguo Wang; Jianghua Mei; Junli Chen; Song Pan; Nan Zhang; Yongfu Liu; Mingwei Zhou; Lichun Feng; Weili Zhao; Shijie Li; Chao Zhang; Meifang Zhang; Yiping Rong; Tai-Guang Jin; Xiongwen Zhang; Shuang Ren; Ying Ji; Rong Zhao; Jin She; Yi Ren; Chunping Xu; Dawei Chen; Jie Cai; Song Shan; Desi Pan; Zhiqiang Ning; Xianping Lu; Taiping Chen; Yun He; Li Chen
Journal:  J Med Chem       Date:  2012-10-12       Impact factor: 7.446

8.  TbPDE1, a novel class I phosphodiesterase of Trypanosoma brucei.

Authors:  Stefan Kunz; Thomas Kloeckner; Lars-Oliver Essen; Thomas Seebeck; Michael Boshart
Journal:  Eur J Biochem       Date:  2004-02

Review 9.  A current analysis of chemotherapy strategies for the treatment of human African trypanosomiasis.

Authors:  Peter Babokhov; Adekunle O Sanyaolu; Wellington A Oyibo; Adetayo F Fagbenro-Beyioku; Nnaemeka C Iriemenam
Journal:  Pathog Glob Health       Date:  2013-07       Impact factor: 2.894

10.  Nifurtimox-eflornithine combination therapy for second-stage African Trypanosoma brucei gambiense trypanosomiasis: a multicentre, randomised, phase III, non-inferiority trial.

Authors:  Gerardo Priotto; Serena Kasparian; Wilfried Mutombo; Daniel Ngouama; Sara Ghorashian; Ute Arnold; Salah Ghabri; Elisabeth Baudin; Vincent Buard; Serge Kazadi-Kyanza; Médard Ilunga; Willy Mutangala; Gabriele Pohlig; Caecilia Schmid; Unni Karunakara; Els Torreele; Victor Kande
Journal:  Lancet       Date:  2009-06-24       Impact factor: 79.321
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  3 in total

1.  Synthesis of new Spiropyrazole derivatives under microwaves irradiation and docking study for inhibition the microbes and COVID-19.

Authors:  Ghada S Masaret
Journal:  J Mol Struct       Date:  2022-06-25       Impact factor: 3.841

Review 2.  Pyrazolone structural motif in medicinal chemistry: Retrospect and prospect.

Authors:  Zefeng Zhao; Xufen Dai; Chenyang Li; Xiao Wang; Jiale Tian; Ying Feng; Jing Xie; Cong Ma; Zhuang Nie; Peinan Fan; Mingcheng Qian; Xirui He; Shaoping Wu; Yongmin Zhang; Xiaohui Zheng
Journal:  Eur J Med Chem       Date:  2019-11-16       Impact factor: 6.514

Review 3.  The ever unfolding story of cAMP signaling in trypanosomatids: vive la difference!

Authors:  Daniel N A Tagoe; Titilola D Kalejaiye; Harry P de Koning
Journal:  Front Pharmacol       Date:  2015-09-07       Impact factor: 5.810
  3 in total

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