Tetrahydroisoquinolines affect the whole-cell phenotype of Mycobacterium tuberculosis by inhibiting the ATP-dependent MurE ligase [PDF]
Objectives (S)-Leucoxine, isolated from the Colombian Lauraceae tree Rhodostemonodaphne crenaticupula Madriñan, was found to inhibit the growth of Mycobacterium tuberculosis H37Rv. A biomimetic approach for the chemical synthesis of a wide array of 1-
Angell, R+17 more
core +1 more source
A novel chemogenomics analysis of G protein-coupled receptors (GPCRs) and their ligands: a potential strategy for receptor de-orphanization. [PDF]
BACKGROUND: G protein-coupled receptors (GPCRs) represent a family of well-characterized drug targets with significant therapeutic value. Phylogenetic classifications may help to understand the characteristics of individual GPCRs and their subtypes ...
Bender, Andreas+8 more
core +4 more sources
We herein report the identification of UR‐NR435 (25), a SCH‐23390‐based fluorescent ligand bearing a 5‐TAMRA dye, as suitable for fluorescence microscopy at the D1R. Single‐digit nanomolar binding affinity could be determined in radioligand competition binding and molecular brightness studies at D1‐like receptors.
Niklas Rosier+11 more
wiley +1 more source
D1-like receptor activation improves PCP-induced cognitive deficits in animal models: Implications for mechanisms of improved cognitive function in schizophrenia [PDF]
YesPhencyclidine (PCP) produces cognitive deficits of relevance to schizophrenia in animal models. The aim was to investigate the efficacy of the D1-like receptor agonist, SKF-38393, to improve PCPinduced deficits in the novel object recognition (NOR ...
Abdul-Monim+84 more
core +1 more source
Rh(III)‐Catalyzed [5+1] Oxidative Cycloaddition of Arylguanidines with Alkynes: A Novel Access to C4‐Disubstituted 1,4‐ Dihydroquinazolin‐2‐amines [PDF]
NOTICE: This is the peer reviewed version of the following article: Cajaraville, A., Suárez, J., López, S., Varela. J. A., Saá, C. (2015). Rh(III)‐Catalyzed [5+1] Oxidative Cycloaddition of Arylguanidines with Alkynes: A Novel Access to C4‐Disubstituted ...
Cajaraville Leiro, Ana+4 more
core +1 more source
Novas metodologias sintéticas utilizando reator de micro-ondas fundamentadas nos princípios da química verde (azidas alílicas e reações de cicloadição) [PDF]
TCC (graduação) - Universidade Federal de Santa Catarina, Centro de Ciências Físicas e Matemáticas, Curso de Química.Este trabalho objetiva a preparação de compostos nitrogenados multifuncionais e de sistemas alílicos contendo o grupo azido, os quais são
Monteiro, Gustavo Claro
core
A novel, tandem construction of C-N and C-C bonds: facile and one-pot transformation of the Baylis-Hillman adducts into 2-benzazepines [PDF]
A novel reaction involving tandem construction of C-N and C- C bonds via the simultaneous Ritter and Houben-Hoesch reactions on Baylis-Hillman adducts leading to a convenient, one-pot synthesis of 2-benzazepine derivatives is described.
Basavaiah, Deevi+1 more
core +1 more source
Conjugation of Organoruthenium(II) 3-(1H-Benzimidazol-2-yl)pyrazolo[3,4-b]pyridines and Indolo[3,2-d]benzazepines to Recombinant Human Serum Albumin: a Strategy To Enhance Cytotoxicity in Cancer Cells [PDF]
Five organoruthenium complexes [RuCl(η6-arene)(L)]Cl with a modified arene ligand, namely, 4-formylphenoxyacetyl-η6-benzylamide, and L = 3-(1H-benzimidazol-2-yl)-1H-pyrazolo[3,4-b]pyridines or indolo[3,2-d]benzazepines were synthesized and conjugated to ...
Ang W. H.+43 more
core +2 more sources
Seven-membered Rings Through Metal-free Rearrangement Mediated By Hypervalent Iodine. [PDF]
A versatile and metal-free approach for the synthesis of carbocycles and of heterocycles bearing seven- and eight-membered rings is described. The strategy is based on ring expansion of 1-vinylcycloalkanols (or the corresponding silyl or methyl ether ...
de Carvalho, João Ernesto+4 more
core +3 more sources
Q/R site interactions with the M3 helix in GluK2 kainate receptor channels revealed by thermodynamic mutant cycles [PDF]
RNA editing at the Q/R site near the apex of the pore loop of AMPA and kainate receptors controls a diverse array of channel properties, including ion selectivity and unitary conductance and susceptibility to inhibition by polyamines and cis-unsaturated ...
Boland+67 more
core +2 more sources