Literature DB >> 7238851

[N1-substituted 1H-indazole-3-ethyl carboxylates and 1H-indazole-3-hydroxamic acids].

G A Bistocchi, G De Meo, M Pedini, A Ricci, H Brouilhet, S Boucherie, M Rabaud, P Jacquignon.   

Abstract

Sixty five new derivatives of ethyl-1H-indazole-3-carboxylate are described; they contain in N1 various aliphatic or aromatic acyl radicals. Moreover halogens or methyl groups are present as substituents at the 5 position or methyl groups at 5,6. The synthesis of seven 1H-indazole-3-hydroxamic acids, substituted at 6 and/or 5 as above, is also described. Some of the synthesized derivatives have preliminarily been tested on rats to investigate acute toxicity, possible antiarthritic effects on primary or secondary arthritis, and their action on weight gain. Some of these indazole derivatives had an antiarthritic effect at doses much lower than the toxic ones; among the compounds tested up to now, the ethyl-5-methyl-N1-p-chlorobenzoyl-1H-indazole-3-carboxylate gave the best results. Weight gain as not affected by any of the examined compounds.

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Year:  1981        PMID: 7238851

Source DB:  PubMed          Journal:  Farmaco Sci        ISSN: 0430-0920


  5 in total

1.  Design, synthesis and evaluation of N-benzoylindazole derivatives and analogues as inhibitors of human neutrophil elastase.

Authors:  Letizia Crocetti; Maria Paola Giovannoni; Igor A Schepetkin; Mark T Quinn; Andrei I Khlebnikov; Agostino Cilibrizzi; Vittorio Dal Piaz; Alessia Graziano; Claudia Vergelli
Journal:  Bioorg Med Chem       Date:  2011-07-07       Impact factor: 3.641

2.  Optimization of N-benzoylindazole derivatives as inhibitors of human neutrophil elastase.

Authors:  Letizia Crocetti; Igor A Schepetkin; Agostino Cilibrizzi; Alessia Graziano; Claudia Vergelli; Donatella Giomi; Andrei I Khlebnikov; Mark T Quinn; Maria Paola Giovannoni
Journal:  J Med Chem       Date:  2013-07-25       Impact factor: 7.446

3.  3-(4-Pyrid-yl)-4,5-dihydro-1H-benzo[g]indazole.

Authors:  Xin Xiao; Yun-Qiang Zhang; Sai-Feng Xue; Qian-Jiang Zhu; Zhu Tao
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2008-11-26

4.  2-(4-Methyl-phen-yl)-2H-indazole.

Authors:  Xingqin Zhou; Xiaofen Qin; Jiankang Zhang
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2010-10-09

5.  4-(4,5-Dihydro-1H-benzo[g]indazol-3-yl)pyridinium chloride dihydrate.

Authors:  Luan-Fang Yang; Hong-Bo Hou; Yi-Ming Liu
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2012-07-07
  5 in total

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