Literature DB >> 21109332

1,2,5-Oxadiazole analogues of leflunomide and related compounds.

Marta Giorgis1, Marco Lucio Lolli, Barbara Rolando, Angela Rao, Paolo Tosco, Shilpi Chaurasia, Domenica Marabello, Roberta Fruttero, Alberto Gasco.   

Abstract

A new series of compounds, structurally related to leflunomide, based on the 1,2,5-oxadiazole ring system (furazan) has been synthesised, and their ability to undergo ring scission at physiological pH to afford the corresponding cyano-oximes has been analyzed. The latter, together with the respective nitro derivatives obtained by oxidation, have been characterised as weak inhibitors of rat dihydroorotate dehydrogenase (DHODH).
Copyright © 2010 Elsevier Masson SAS. All rights reserved.

Entities:  

Mesh：

Substances：

Year:  2010        PMID： 21109332     DOI： 10.1016/j.ejmech.2010.10.029

Source DB:  PubMed          Journal:  Eur J Med Chem        ISSN： 0223-5234            Impact factor:   6.514


  7 in total

1.  Use of the 4-Hydroxytriazole Moiety as a Bioisosteric Tool in the Development of Ionotropic Glutamate Receptor Ligands.

Authors:  Stefano Sainas; Piero Temperini; Jill C Farnsworth; Feng Yi; Stine Møllerud; Anders A Jensen; Birgitte Nielsen; Alice Passoni; Jette S Kastrup; Kasper B Hansen; Donatella Boschi; Darryl S Pickering; Rasmus P Clausen; Marco L Lolli
Journal:  J Med Chem       Date:  2019-04-18       Impact factor: 7.446

2.  The role of fluorine in stabilizing the bioactive conformation of dihydroorotate dehydrogenase inhibitors.

Authors:  Silvia Bonomo; Paolo Tosco; Marta Giorgis; Marco Lolli; Roberta Fruttero
Journal:  J Mol Model       Date:  2012-11-10       Impact factor: 1.810

3.  Identification of Human Dihydroorotate Dehydrogenase Inhibitor by a Pharmacophore-Based Virtual Screening Study.

Authors:  Salvatore Galati; Stefano Sainas; Marta Giorgis; Donatella Boschi; Marco L Lolli; Gabriella Ortore; Giulio Poli; Tiziano Tuccinardi
Journal:  Molecules       Date:  2022-06-07       Impact factor: 4.927

4.  On the interactions of leflunomide and teriflunomide within receptor cavity--NMR studies and energy calculations.

Authors:  Jacek Kujawski; Marek K Bernard; Elżbieta Jodłowska; Kornelia Czaja; Beata Drabińska
Journal:  J Mol Model       Date:  2015-04-08       Impact factor: 1.810

5.  Isolation and characterization of a degradation product in leflunomide and a validated selective stability-indicating HPLC-UV method for their quantification.

Authors:  Balraj Saini; Gulshan Bansal
Journal:  J Pharm Anal       Date:  2014-10-22

6.  Targeting Acute Myelogenous Leukemia Using Potent Human Dihydroorotate Dehydrogenase Inhibitors Based on the 2-Hydroxypyrazolo[1,5-a]pyridine Scaffold: SAR of the Aryloxyaryl Moiety.

Authors:  Stefano Sainas; Marta Giorgis; Paola Circosta; Giulio Poli; Marta Alberti; Alice Passoni; Valentina Gaidano; Agnese C Pippione; Nicoletta Vitale; Davide Bonanni; Barbara Rolando; Alessandro Cignetti; Cristina Ramondetti; Alessia Lanno; Davide M Ferraris; Barbara Canepa; Barbara Buccinnà; Marco Piccinini; Menico Rizzi; Giuseppe Saglio; Salam Al-Karadaghi; Donatella Boschi; Riccardo Miggiano; Tiziano Tuccinardi; Marco L Lolli
Journal:  J Med Chem       Date:  2022-09-26       Impact factor: 8.039

7.  Crystal structure of poly[(μ3-4-amino-1,2,5-oxa-diazole-3-hydroxamato)thallium(I)].

Authors:  Inna S Safyanova; Oksana A Bondar; Anna V Pavlishchuk; Iryna V Omelchenko; Turganbay S Iskenderov; Valentina A Kalibabchuk
Journal:  Acta Crystallogr E Crystallogr Commun       Date:  2020-02-11
  7 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.