Literature DB >> 17950601

Discovery of novel non-cytotoxic salicylhydrazide containing HIV-1 integrase inhibitors.

Laith Q Al-Mawsawi1, Raveendra Dayam, Laleh Taheri, Myriam Witvrouw, Zeger Debyser, Nouri Neamati.   

Abstract

The previously discovered salicylhydrazide class of compounds displayed potent HIV-1 integrase (IN) inhibitory activity. The development of this class of compounds as antiretroviral agents was halted due to cytotoxicity in the nanomolar to sub-micromolar range. We identified a novel class of non-cytotoxic hydrazide IN inhibitors utilizing the minimally required salicylhydrazide substructure as a template in a small-molecule database search. The novel hydrazides displayed low micromolar IN inhibitory activity and are several hundred-fold less cytotoxic than previously disclosed salicylhydrazide IN inhibitors.

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Year:  2007        PMID： 17950601     DOI： 10.1016/j.bmcl.2007.09.102

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


  11 in total

1.  4-Substituted 2-Hydroxyisoquinoline-1,3(2H,4H)-diones as a Novel Class of HIV-1 Integrase Inhibitors.

Authors:  Muriel Billamboz; Virginie Suchaud; Fabrice Bailly; Cedric Lion; Jonas Demeulemeester; Christina Calmels; Marie-Line Andréola; Frauke Christ; Zeger Debyser; Philippe Cotelle
Journal:  ACS Med Chem Lett       Date:  2013-05-17       Impact factor: 4.345

2.  Design of HIV-1 integrase inhibitors targeting the catalytic domain as well as its interaction with LEDGF/p75: a scaffold hopping approach using salicylate and catechol groups.

Authors:  Xing Fan; Feng-Hua Zhang; Rasha I Al-Safi; Li-Fan Zeng; Yumna Shabaik; Bikash Debnath; Tino W Sanchez; Srinivas Odde; Nouri Neamati; Ya-Qiu Long
Journal:  Bioorg Med Chem       Date:  2011-06-26       Impact factor: 3.641

Review 3.  HIV-1 IN inhibitors: 2010 update and perspectives.

Authors:  Christophe Marchand; Kasthuraiah Maddali; Mathieu Métifiot; Yves Pommier
Journal:  Curr Top Med Chem       Date:  2009       Impact factor: 3.295

Review 4.  Progress in HIV-1 Integrase Inhibitors: A Review of their Chemical Structure Diversity.

Authors:  Zahra Hajimahdi; Afshin Zarghi
Journal:  Iran J Pharm Res       Date:  2016       Impact factor: 1.696

5.  Synthesis of novel (E)-1-(2-(2-(4(dimethylamino) benzylidene) hydrazinyl)-4-methylthiazol-5-yl)ethanone derivatives as ecto-5'-nucleotidase inhibitors.

Authors:  Sidra Hassan; Pervaiz Ali Channar; Fayaz Ali Larik; Aamer Saeed; Hamid Saeed Shah; Joanna Lecka; Jean Sévigny; Jamshed Iqbal
Journal:  R Soc Open Sci       Date:  2018-09-12       Impact factor: 2.963

6.  Benzylidene/2-chlorobenzylidene hydrazides: synthesis, antimicrobial activity, QSAR studies and antiviral evaluation.

Authors:  Davinder Kumar; Vikramjeet Judge; Rakesh Narang; Sonia Sangwan; Erik De Clercq; Jan Balzarini; Balasubramanian Narasimhan
Journal:  Eur J Med Chem       Date:  2010-03-07       Impact factor: 6.514

7.  1-{(E)-[5-(2-Nitro-phen-yl)furan-2-yl]methyl-idene}-2,2-diphenyl-hydrazine.

Authors:  Marcos Flores-Alamo; Blanca M Cabrera-Vivas; Ruth Meléndrez-Luevano; Julio M Hernández P; Lena Ruiz-Azuara
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2012-12-15

8.  2-Hy-droxy-N'-methyl-5-nitro-benzohydrazide.

Authors:  Ming Yang; Chengzhi Jin; Xiaodong Zhou; Longfei Jin
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2013-07-24

9.  Syntheses, spectral characterization, and antimicrobial studies on the coordination compounds of metal ions with schiff base containing both aliphatic and aromatic hydrazide moieties.

Authors:  Dinesh Kumar; Silky Chadda; Jyoti Sharma; Parveen Surain
Journal:  Bioinorg Chem Appl       Date:  2013-10-03       Impact factor: 7.778

10.  Crystal structure of (E)-1-(2-nitro-benzyl-idene)-2,2-di-phenyl-hydrazine.

Authors:  Marcos Flores-Alamo; Ruth Meléndrez-Luévano; José A Ortiz Márquez; Estibaliz Sansinenea Royano; Blanca M Cabrera-Vivas
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2014-08-01
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