69 research outputs found
Synthesis of fullerene@gold core-shell nanostructures
10.1039/c1cc10599jChemical Communications47277710-7712CHCO
Synthesis of Novel Benzoxazocino Quinoliniums and Quinolones Under PTC Conditions and Their Application in Suzuki Cross Coupling Reaction For the Construction of Polynuclear Heteroaromatics
A general and highly efficient synthetic protocol under phase transfer catalytic condition has been established
for the synthesis of fused tetracyclic oxazocinoquinolone analogues which served as the precursors for novel biaryl quinolones using microwave assisted Suzuki cross coupling reaction
A facile and novel synthesis of N2-, C6-substituted pyrazolo[3,4- d ]pyrimidine-4 carboxylate derivatives as adenosine receptor antagonists
An efficient synthetic procedure was adopted to synthesize a series of new molecules containing the pyrazolo[3,4-d]pyrimidine (PP) scaffold, which have been evaluated as promising human adenosine receptor (AR) antagonists. The effect of substitutions at the N2, C4 and C6 positions of PPs on the affinity and selectivity towards the adenosine receptors were explored. Most of the pyrazolo[3,4-d]pyrimidine-4-carboxylates displayed from moderate to good affinity at the human A3AR (hA3AR), as indicated by the low micromolar range of Ki values (Ki hA3AR \ubc 0.7e34 mM). In particular, compounds 60 and 62 displayed good affinity at the hA3AR (60, Ki hA3AR \ubc 2.2 mM and 62, Ki A3AR \ubc 2.9 mM) and selectivity towards the other AR subtypes (60, >46-fold selective and 62, >34-fold selective, respectively). In view of these results, these novel PP analogues were docked both in the crystallographic structure of the hA2AAR and in a homology model of the hA3AR in order to support the structure activity relationship (SAR) analysis. These preliminary results demonstrated that pyrazolo[3,4-d]pyrimidine can be considered a promising scaffold to obtain new molecules with potent hA3AR antagonist activity
A facile and novel synthesis of N2-, C6-substituted pyrazolo[3,4- d ]pyrimidine-4 carboxylate derivatives as adenosine receptor antagonists
10.1016/j.ejmech.2015.01.046European Journal of Medicinal Chemistry92784-79
Pharmacophore elucidation for a new series of 2-aryl-pyrazolo-triazolo- pyrimidines as potent human A3 adenosine receptor antagonists
10.1016/j.bmcl.2011.03.073Bioorganic and Medicinal Chemistry Letters21102898-2905BMCL
Discovery of simplified N2-substituted pyrazolo[3,4-d]pyrimidine derivatives as novel adenosine receptor antagonists: Efficient synthetic approaches, biological evaluations and molecular docking studies
10.1016/j.bmc.2014.01.018Bioorganic and Medicinal Chemistry2251751-1765BMEC
Organoruthenium antagonists of human A3 adenosine receptors
10.1002/chem.201203291Chemistry - A European Journal19258321-8330CEUJ
Facile Synthesis of Seven to Nine-Membered-Fused Tricyclic Quinolones and Quinolinium Salts under Phase Transfer Catalyzed Conditions
Phase transfer catalyzed one-pot syntheses of fused oxazepino, oxazocino, and oxazonino quinolinium cations and quinolones were achieved from 8-hydroxy quinoline derivatives with 1,u-dihaloalkanes. Structures of all the products were elucidated by spectroscopic analysis. Single
crystal X-ray crystallographic analysis of three compounds and graphical superposition of the structures indicate that products having sevenmembered ring are less planar compared to the product having eight-membered ring
Efficient Synthesis of Novel Tetrahydropyrrolo[30,40:3,4]Pyrrolo[2,1-a] Isoquinoline Derivatives via a Simple and Convenient MCR in Aqueous Micellar System
A simple and efficient one-pot three component synthesis of tetrahydropyrrolo[30,40:3,4]pyrrolo[2,1-
a]isoquinoline-9,11-dione derivatives has been achieved from variously substituted isoquinolines, 2-
bromo acetophenone and N-aryl maleimide derivatives in an aqueous micellar medium. The synthesis
represents an environmentally benign alternative to classical method
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