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Recent advances in the development of selective human MAO-B inhibitors: (hetero)arylidene-(4-substituted-thiazol-2-yl)hydrazines.
Secci D, Bolasco A, Carradori S, D'Ascenzio M, Nescatelli R, Yáñez M. Secci D, et al. Among authors: bolasco a. Eur J Med Chem. 2012 Dec;58:405-17. doi: 10.1016/j.ejmech.2012.10.032. Epub 2012 Oct 26. Eur J Med Chem. 2012. PMID: 23153812
Synthesis of a novel series of thiazole-based histone acetyltransferase inhibitors.
Secci D, Carradori S, Bizzarri B, Bolasco A, Ballario P, Patramani Z, Fragapane P, Vernarecci S, Canzonetta C, Filetici P. Secci D, et al. Among authors: bolasco a. Bioorg Med Chem. 2014 Mar 1;22(5):1680-9. doi: 10.1016/j.bmc.2014.01.022. Epub 2014 Jan 26. Bioorg Med Chem. 2014. PMID: 24513187
Investigations on the 2-thiazolylhydrazyne scaffold: synthesis and molecular modeling of selective human monoamine oxidase inhibitors.
Chimenti F, Bolasco A, Secci D, Chimenti P, Granese A, Carradori S, Yáñez M, Orallo F, Ortuso F, Alcaro S. Chimenti F, et al. Bioorg Med Chem. 2010 Aug 1;18(15):5715-23. doi: 10.1016/j.bmc.2010.06.007. Epub 2010 Jun 9. Bioorg Med Chem. 2010. PMID: 20615716
A new series of [4-(3-methoxyphenyl)-thiazol-2-yl]hydrazyne derivatives were synthesized in good yield (71-99%) and characterized by elemental analysis and (1)H NMR studies. ...The most active and selective derivative (20), bearing a pyridine moiety on the CN, displ
A new series of [4-(3-methoxyphenyl)-thiazol-2-yl]hydrazyne derivatives were synthesized in good yield (71-99%) and characterized by
Anti-Candida activity and cytotoxicity of a large library of new N-substituted-1,3-thiazolidin-4-one derivatives.
De Monte C, Carradori S, Bizzarri B, Bolasco A, Caprara F, Mollica A, Rivanera D, Mari E, Zicari A, Akdemir A, Secci D. De Monte C, et al. Among authors: bolasco a. Eur J Med Chem. 2016 Jan 1;107:82-96. doi: 10.1016/j.ejmech.2015.10.048. Epub 2015 Nov 2. Eur J Med Chem. 2016. PMID: 26562544
Design, synthesis and biological characterization of thiazolidin-4-one derivatives as promising inhibitors of Toxoplasma gondii.
D'Ascenzio M, Bizzarri B, De Monte C, Carradori S, Bolasco A, Secci D, Rivanera D, Faulhaber N, Bordón C, Jones-Brando L. D'Ascenzio M, et al. Among authors: bolasco a. Eur J Med Chem. 2014 Oct 30;86:17-30. doi: 10.1016/j.ejmech.2014.08.046. Epub 2014 Aug 15. Eur J Med Chem. 2014. PMID: 25140751
Selective MAO-B inhibitors: a lesson from natural products.
Carradori S, D'Ascenzio M, Chimenti P, Secci D, Bolasco A. Carradori S, et al. Among authors: bolasco a. Mol Divers. 2014 Feb;18(1):219-43. doi: 10.1007/s11030-013-9490-6. Epub 2013 Nov 12. Mol Divers. 2014. PMID: 24218136 Review.
Patent-related survey on new monoamine oxidase inhibitors and their therapeutic potential.
Carradori S, Secci D, Bolasco A, Chimenti P, D'Ascenzio M. Carradori S, et al. Among authors: bolasco a. Expert Opin Ther Pat. 2012 Jul;22(7):759-801. doi: 10.1517/13543776.2012.698613. Epub 2012 Jun 18. Expert Opin Ther Pat. 2012. PMID: 22702491 Review.
Focusing on new monoamine oxidase inhibitors.
Bolasco A, Carradori S, Fioravanti R. Bolasco A, et al. Expert Opin Ther Pat. 2010 Jul;20(7):909-39. doi: 10.1517/13543776.2010.495716. Expert Opin Ther Pat. 2010. PMID: 20553094 Review.
IMPORTANCE OF THE FIELD: Monoamine oxidase (MAO) plays a significant role in the control of intracellular concentration of monoaminergic neurotransmitters or neuromodulators and dietary amines. ...
IMPORTANCE OF THE FIELD: Monoamine oxidase (MAO) plays a significant role in the control of intracellular concentration of monoaminer …
A novel histone acetyltransferase inhibitor modulating Gcn5 network: cyclopentylidene-[4-(4'-chlorophenyl)thiazol-2-yl)hydrazone.
Chimenti F, Bizzarri B, Maccioni E, Secci D, Bolasco A, Chimenti P, Fioravanti R, Granese A, Carradori S, Tosi F, Ballario P, Vernarecci S, Filetici P. Chimenti F, et al. J Med Chem. 2009 Jan 22;52(2):530-6. doi: 10.1021/jm800885d. J Med Chem. 2009. PMID: 19099397
To find modulators of the histone acetyltransferase Gcn5p, we performed a phenotypic screening on a set of newly synthesized molecules derived from thiazole in budding yeast Saccharomyces cerevisiae. ...A novel molecule CPTH2, cyclopentylidene-[4-(4'-chloroph …
To find modulators of the histone acetyltransferase Gcn5p, we performed a phenotypic screening on a set of newly synthesized m …
Synthesis, molecular modeling, and selective inhibitory activity against human monoamine oxidases of 3-carboxamido-7-substituted coumarins.
Chimenti F, Secci D, Bolasco A, Chimenti P, Bizzarri B, Granese A, Carradori S, Yáñez M, Orallo F, Ortuso F, Alcaro S. Chimenti F, et al. J Med Chem. 2009 Apr 9;52(7):1935-42. doi: 10.1021/jm801496u. J Med Chem. 2009. PMID: 19267475
A large series of 3-carboxamido-7-substituted coumarins have been synthesized and tested in vitro for their human monoamine oxidase A and B (hMAO-A and hMAO-B) inhibitory activity. Taking into account all the relevant structural information on MAOs reported i
A large series of 3-carboxamido-7-substituted coumarins have been synthesized and tested in vitro for their human monoamine oxidase
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