Literature DB >> 16563760

The search for novel TRPV1-antagonists: from carboxamides to benzimidazoles and indazolones.

Stephen Robert Fletcher1, Edward McIver, Stephen Lewis, Frank Burkamp, Clare Leech, Glenn Mason, Susan Boyce, Denise Morrison, Gillian Richards, Kathy Sutton, Anthony Brian Jones.   

Abstract

Based on a series of diaryl amides the corresponding inverse amides have been found to be potent TRPV1 receptor antagonists. Benzimidazole and indazolone derivatives prepared retained good potency in vitro and indazolone 4a was identified as a novel TRPV1 receptor antagonist suitable for evaluating orally in animal models of analgesia.

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Year:  2006        PMID: 16563760     DOI: 10.1016/j.bmcl.2006.03.004

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


  10 in total

1.  High-throughput screening for inhibitors of Mycobacterium tuberculosis H37Rv.

Authors:  Subramaniam Ananthan; Ellen R Faaleolea; Robert C Goldman; Judith V Hobrath; Cecil D Kwong; Barbara E Laughon; Joseph A Maddry; Alka Mehta; Lynn Rasmussen; Robert C Reynolds; John A Secrist; Nice Shindo; Dustin N Showe; Melinda I Sosa; William J Suling; E Lucile White
Journal:  Tuberculosis (Edinb)       Date:  2009-09-15       Impact factor: 3.131

2.  Nucleophilic substitution of oxazino-/oxazolino-/benzoxazin [3,2-b]indazoles: an effective route to 1H-indazolones.

Authors:  Michael B Donald; Wayne E Conrad; James S Oakdale; Jeffrey D Butler; Makhluf J Haddadin; Mark J Kurth
Journal:  Org Lett       Date:  2010-06-04       Impact factor: 6.005

3.  The Davis-Beirut reaction: N1,N2-disubstituted-1H-indazolones via 1,6-electrophilic addition to 3-alkoxy-2H-indazoles.

Authors:  Wayne E Conrad; Ryo Fukazawa; Makhluf J Haddadin; Mark J Kurth
Journal:  Org Lett       Date:  2011-05-25       Impact factor: 6.005

4.  Efficient synthesis of highly substituted tetrahydroindazolone derivatives.

Authors:  Angela Scala; Anna Piperno; Francesco Risitano; Santa Cirmi; Michele Navarra; Giovanni Grassi
Journal:  Mol Divers       Date:  2015-03-18       Impact factor: 2.943

5.  A one-pot-three-step route to triazolotriazepinoindazolones from oxazolino-2H-indazoles.

Authors:  Wayne E Conrad; Kevin X Rodriguez; Huy H Nguyen; James C Fettinger; Makhluf J Haddadin; Mark J Kurth
Journal:  Org Lett       Date:  2012-07-23       Impact factor: 6.005

6.  Davis-Beirut Reaction: A Photochemical Brønsted Acid Catalyzed Route to N-Aryl 2H-Indazoles.

Authors:  Niklas Kraemer; Clarabella J Li; Jie S Zhu; Julio M Larach; Ka Yi Tsui; Dean J Tantillo; Makhluf J Haddadin; Mark J Kurth
Journal:  Org Lett       Date:  2019-07-24       Impact factor: 6.005

7.  Electrochemical synthesis of N,N'-disubstituted indazolin-3-ones via an intramolecular anodic dehydrogenative N-N coupling reaction.

Authors:  Jessica C Bieniek; Michele Grünewald; Johannes Winter; Dieter Schollmeyer; Siegfried R Waldvogel
Journal:  Chem Sci       Date:  2022-06-13       Impact factor: 9.969

8.  PIII/PV═O-Catalyzed Intermolecular N-N Bond Formation: Cross-Selective Reductive Coupling of Nitroarenes and Anilines.

Authors:  Gen Li; Steven P Miller; Alexander T Radosevich
Journal:  J Am Chem Soc       Date:  2021-09-02       Impact factor: 16.383

9.  Rapid and halide compatible synthesis of 2-N-substituted indazolone derivatives via photochemical cyclization in aqueous media.

Authors:  Hui-Jun Nie; An-Di Guo; Hai-Xia Lin; Xiao-Hua Chen
Journal:  RSC Adv       Date:  2019-04-30       Impact factor: 4.036

10.  Synthesis of Succinimide-Linked Indazol-3-ols Derived from Maleimides under Rh(III) Catalysis.

Authors:  Ju Young Kang; Suho Kim; Junghyea Moon; Eunjae Chung; Jaeyoung Kim; So Young Kyung; Hyung Sik Kim; Neeraj Kumar Mishra; In Su Kim
Journal:  ACS Omega       Date:  2022-04-21
  10 in total

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