Literature DB >> 16250831

Pharmacological properties of indazole derivatives: recent developments.

Hugo Cerecetto1, Alejandra Gerpe, Mercedes González, Vicente J Arán, Carmen Ochoa de Ocáriz.   

Abstract

The chemistry of indazole and its N-oxide derivatives is very well-known. Indazole derivatives were extensively studied as bioactive compounds, such as anti-aggregatory and vasorelaxant activity by NO release and increase of cGMP levels and anticancer effects, antimicrobial and antiparasitic properties, among others. Recently, the research and development in the medicinal chemistry of these systems have produced compounds with contraceptive activities for men, for the treatment of osteoporosis, inflammatory disorders and neurodegenerative diseases. On the other hand, indazole N-oxide derivatives were poorly studied as bioactive compounds, but recently compounds with antiparasitic properties were produced. In this presentation, recent developments in the chemistry and medicinal chemistry of indazole and its N-oxide derivatives will be reviewed.

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Year:  2005        PMID: 16250831     DOI: 10.2174/138955705774329564

Source DB:  PubMed          Journal:  Mini Rev Med Chem        ISSN: 1389-5575            Impact factor:   3.862


  24 in total

1.  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

2.  3-substituted indazoles as configurationally locked 4EGI-1 mimetics and inhibitors of the eIF4E/eIF4G interaction.

Authors:  Revital Yefidoff-Freedman; Ting Chen; Rupam Sahoo; Limo Chen; Gerhard Wagner; Jose A Halperin; Bertal H Aktas; Michael Chorev
Journal:  Chembiochem       Date:  2014-01-23       Impact factor: 3.164

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.  Synthesis of 2H-indazoles by the [3 + 2] cycloaddition of arynes and sydnones.

Authors:  Chunrui Wu; Yuesi Fang; Richard C Larock; Feng Shi
Journal:  Org Lett       Date:  2010-05-21       Impact factor: 6.005

6.  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

7.  Efficient Pd-catalyzed amination reactions for heterocycle functionalization.

Authors:  Jaclyn L Henderson; Stephen L Buchwald
Journal:  Org Lett       Date:  2010-10-15       Impact factor: 6.005

8.  Suzuki-Miyaura cross-coupling of unprotected, nitrogen-rich heterocycles: substrate scope and mechanistic investigation.

Authors:  M Alexander Düfert; Kelvin L Billingsley; Stephen L Buchwald
Journal:  J Am Chem Soc       Date:  2013-08-16       Impact factor: 15.419

9.  Unprecedented rearrangement of 2-(2-aminoethyl)-1-aryl-3,4-dihydropyrazino[1,2-b]indazole-2-ium 6-oxides to 2,3-dihydro-1H-imidazo[1,2-b]indazoles.

Authors:  Jan Kocí; Allen G Oliver; Viktor Krchnák
Journal:  J Org Chem       Date:  2010-01-15       Impact factor: 4.354

10.  cis-Tetrachlorido-bis(indazole)osmium(iv) and its osmium(iii) analogues: paving the way towards the cis-isomer of the ruthenium anticancer drugs KP1019 and/or NKP1339.

Authors:  Gabriel E Büchel; Susanne Kossatz; Ahmad Sadique; Peter Rapta; Michal Zalibera; Lukas Bucinsky; Stanislav Komorovsky; Joshua Telser; Jörg Eppinger; Thomas Reiner; Vladimir B Arion
Journal:  Dalton Trans       Date:  2017-09-12       Impact factor: 4.390

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