[NMR paper] Synthesis of new thiazolo-celecoxib analogues as dual cyclooxygenase-2/15-lipoxygenase inhibitors: Determination of regio-specific different pyrazole cyclization by 2D NMR.
Synthesis of new thiazolo-celecoxib analogues as dual cyclooxygenase-2/15-lipoxygenase inhibitors: Determination of regio-specific different pyrazole cyclization by 2D NMR.
Related ArticlesSynthesis of new thiazolo-celecoxib analogues as dual cyclooxygenase-2/15-lipoxygenase inhibitors: Determination of regio-specific different pyrazole cyclization by 2D NMR.
Eur J Med Chem. 2016 Aug 08;118:250-8
Authors: Abdelall EK, Kamel GM
Abstract
Two new series of 1,5-diaryl pyrazoles (5a, 5b, 7a, 7b and 10) and 1,5-diaryl pyrazoline (12a and 12b) were prepared as both Cyclooxygenase-2 and 15-lipoxygenase inhibitors. Carrageenan-induced rat paw edema, ulcer index and anti-COX-1/COX-2 and 15-LOX inhibition assays were also included. Cyclization of different pyrazoles was discussed using 2D NMR such as HSQC, HMBC and NOSEY determinations. Compound 5a is more effective with ED50*=*0.98 and 3.98*?M against COX-2 and 15-lipoxygenase respectively, than the references celecoxib (1.54*?M) and meclofenamate sodium (5.64*?M).
[NMR paper] Design, synthesis, biological evaluation, NMR and DFT studies of structurally-simplified trimethoxy benzamides as P-glycoprotein selective inhibitors: the role of molecular flatness.
Design, synthesis, biological evaluation, NMR and DFT studies of structurally-simplified trimethoxy benzamides as P-glycoprotein selective inhibitors: the role of molecular flatness.
Design, synthesis, biological evaluation, NMR and DFT studies of structurally-simplified trimethoxy benzamides as P-glycoprotein selective inhibitors: the role of molecular flatness.
Chem Biol Drug Des. 2016 Jun 22;
Authors: Stefanachi A, Mangiatordi GF, Tardia P, Alberga D, Leonetti F, Niso M, Colabufo NA, Adamo C, Nicolotti O, Cellamare S
Abstract
...
nmrlearner
Journal club
0
06-23-2016 10:34 AM
[NMR paper] Synthesis, biological activity and NMR-based structural studies of deltorphin I analogues modified in message domain with a new ?,?-disubstituted glycines.
Synthesis, biological activity and NMR-based structural studies of deltorphin I analogues modified in message domain with a new ?,?-disubstituted glycines.
Related Articles Synthesis, biological activity and NMR-based structural studies of deltorphin I analogues modified in message domain with a new ?,?-disubstituted glycines.
Chem Biol Drug Des. 2016 Jan 25;
Authors: Lasota A, Fr?czak O, Muchowska A, Nowakowski M, Maciejczyk M, Ejchart A, Olma A
Abstract
This paper describes new deltorphin I analogues in which phenylalanine...
nmrlearner
Journal club
0
01-26-2016 03:40 PM
Phenotypic Screening Identifies Protein Synthesis Inhibitors as H-Ras-Nanocluster-Increasing Tumor Growth Inducers
Phenotypic Screening Identifies Protein Synthesis Inhibitors as H-Ras-Nanocluster-Increasing Tumor Growth Inducers
http://pubs.acs.org/appl/literatum/publisher/achs/journals/content/bichaw/0/bichaw.ahead-of-print/acs.biochem.5b00724/20151130/images/medium/bi-2015-00724w_0004.gif
Biochemistry
DOI: 10.1021/acs.biochem.5b00724
http://feeds.feedburner.com/~ff/acs/bichaw?d=yIl2AUoC8zA
http://feeds.feedburner.com/~r/acs/bichaw/~4/J39aNiUlZbQ
More...
[NMR paper] Synthesis, 2D-NMR and molecular modelling studies of pentacycloundecane lactam-peptides and peptoids as potential HIV-1 wild type C-SA protease inhibitors.
Synthesis, 2D-NMR and molecular modelling studies of pentacycloundecane lactam-peptides and peptoids as potential HIV-1 wild type C-SA protease inhibitors.
http://www.bionmr.com//www.ncbi.nlm.nih.gov/corehtml/query/egifs/http:--informahealthcare.com-userimages-ContentEditor-1258375244362-ihc-linkout.gif Related Articles Synthesis, 2D-NMR and molecular modelling studies of pentacycloundecane lactam-peptides and peptoids as potential HIV-1 wild type C-SA protease inhibitors.
J Enzyme Inhib Med Chem. 2013 Feb;28(1):78-88
Authors: Makatini MM, Petzold K, Alves...
nmrlearner
Journal club
0
09-21-2013 06:50 PM
[NMR paper] Exploring surfaces and cavities in lipoxygenase and other proteins by hyperpolarized
Exploring surfaces and cavities in lipoxygenase and other proteins by hyperpolarized xenon-129 NMR.
Related Articles Exploring surfaces and cavities in lipoxygenase and other proteins by hyperpolarized xenon-129 NMR.
J Am Chem Soc. 1999 Oct 13;121(40):9370-7
Authors: Bowers CR, Storhaug V, Webster CE, Bharatam J, Cottone A, Gianna R, Betsey K, Gaffney BJ
This paper presents an exploratory study of the binding interactions of xenon with the surface of several different proteins in the solution and solid states using both conventional and...
nmrlearner
Journal club
0
11-18-2010 08:31 PM
[NMR paper] Novel inhibitors of Erm methyltransferases from NMR and parallel synthesis.
Novel inhibitors of Erm methyltransferases from NMR and parallel synthesis.
Related Articles Novel inhibitors of Erm methyltransferases from NMR and parallel synthesis.
J Med Chem. 1999 Sep 23;42(19):3852-9
Authors: Hajduk PJ, Dinges J, Schkeryantz JM, Janowick D, Kaminski M, Tufano M, Augeri DJ, Petros A, Nienaber V, Zhong P, Hammond R, Coen M, Beutel B, Katz L, Fesik SW
The Erm family of methyltransferases confers resistance to the macrolide-lincosamide-streptogramin type B (MLS) antibiotics through the methylation of 23S ribosomal RNA. Upon...
nmrlearner
Journal club
0
11-18-2010 08:31 PM
[NMR paper] Two-dimensional NMR studies of squash family inhibitors. Sequence-specific proton ass
Two-dimensional NMR studies of squash family inhibitors. Sequence-specific proton assignments and secondary structure of reactive-site hydrolyzed Cucurbita maxima trypsin inhibitor III.
Related Articles Two-dimensional NMR studies of squash family inhibitors. Sequence-specific proton assignments and secondary structure of reactive-site hydrolyzed Cucurbita maxima trypsin inhibitor III.
Biochemistry. 1992 Jan 28;31(3):898-904
Authors: Krishnamoorthi R, Gong YX, Lin CL, VanderVelde D
The solution structure of reactive-site hydrolyzed Cucurbita...
Synthesis of new thiazolo-celecoxib analogues as dual cyclooxygenase-2/15-lipoxygenase inhibitors: Determination of regio-specific different pyrazole cyclization by 2D NMR.
Linear Mode
