69 research outputs found

    Synthesis of fullerene@gold core-shell nanostructures

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    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

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    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

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    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

    Organoruthenium antagonists of human A3 adenosine receptors

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    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

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    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

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    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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