Synthesis and BZR affinity of pyrazolo[1,5-a]pyrimidine derivatives. part 1: study of the structural features for BZR recognition

Selleri, Silvia; Bruni, F.; Costagli, Chiara; Costanzo, A.; Guerrini, Gabriella; Ciciani, Giovanna; Costa, Barbara; Martini, Claudia

doi:10.1016/s0968-0896(99)00232-1

Cited by 29 publications

(26 citation statements)

References 16 publications

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“…1-7 In addition, these compounds tend to form fairly stable complexes with metal ions. [8][9][10][11][12] Incorporation of an oligooxyethylene fragment into azolopyrimidines and preparation of the open chain ana logs of crown ethers (podands) can be of certain interest for medicinal chemistry, since it is known that podands can mimic behavior of natural ionophores (for example, nihericine), performing transportation function in liv ing cells. 13 One of the most convenient methods for functional ization of podands with azolopyrimidine moieties consists in cyclocondensation of α,β unsaturated carbonyl com pounds (chalcones) with aminoazoles, in particular, with 3 amino 1,2,4 triazole.…”

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confidence: 99%

Unusual heterocyclization of chalcone podands with 3-amino-1,2,4-triazole

et al. 2011

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A new type of intramolecular cyclization of 1,5 bis[2 (E 3 oxo 3 phenylprop 1 enyl) phenoxy] 3 oxapentane with 3 aminotriazole promoted by potassium ions was discovered. A cascade mechanism for the formation of crownophane with 4,7 dihydro[1,2,4]triazolo[1,5 a] pyrimidine fragment was suggested. Effects of oligooxyethylene fragment of the chalcone podand and acid base catalysis on the selectivity of the cyclocondensation processes and degree of oxidation of triazolopyrimidine fragments were studied. The product structures were confirmed by IR, 1 H and 13 C NMR spectroscopy and X ray diffraction study.

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confidence: 99%

Unusual heterocyclization of chalcone podands with 3-amino-1,2,4-triazole

et al. 2011

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“…One compound of this class (Ar: 3 -thienyl, R 1 : 2 -pyridyl) showed a promising selectivity for α1 containing receptors [129]. These structures can be obtained in a one-step reaction as displayed in general Scheme 30, which allows a rapid synthesis of a variety of derivatives [131]. Among the pyrazolopyrimidines investigated as sedative-hypnotic agents, Indiplon [128] received an initial approval letter from the United States Food and Drug Administration (FDA).…”

Section: Triazolobenzodiazepinesmentioning

confidence: 99%

“…One compound of this class (Ar: 3′-thienyl, R 1 : 2′-pyridyl) showed a promising selectivity for α1 containing receptors [129]. These structures can be obtained in a one-step reaction as displayed in general Scheme 30, which allows a rapid synthesis of a variety of derivatives [131].…”

Section: Triazolobenzodiazepinesmentioning

confidence: 99%

Allosteric GABAA Receptor Modulators—A Review on the Most Recent Heterocyclic Chemotypes and Their Synthetic Accessibility

et al. 2020

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GABAA receptor modulators are structurally almost as diverse as their target protein. A plethora of heterocyclic scaffolds has been described as modulating this extremely important receptor family. Some made it into clinical trials and, even on the market, some were dismissed. This review focuses on the synthetic accessibility and potential for library synthesis of GABAA receptor modulators containing at least one heterocyclic scaffold, which were disclosed within the last 10 years.

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“…Several compounds of this class display interesting antitrypanosomal [4] and antischistosomal activities [6]. They are used as HMG-CoA reductaseinhibitors [7], COX-2 selective inhibitors [8], 30,50-cyclic-AMP phosphodiesteraseinhibitors [9], CRF1 antagonists [10][11], selective peripheral benzodiazepine receptor ligands [12][13][14][15][16], potassium channel [17] and histamine-3 receptor ligands [18], CDK9 inhibitor [19]and antianxiety agents [20].…”

Section: Introductionmentioning

confidence: 99%

Synthesis, Characterization and Biological Evaluation of some Novel Pyrazolo[1,5-a]Pyrimidine Derivatives

Thumar¹,

Kaneria²,

Vadodaria³

et al. 2016

ILCPA

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A convenient synthesis of substituted Pyrazolo[1,5-a]pyrimidine was carried out by the reaction of different ketene dithioacetals with different aromatic amine in isopropanol in the presence of potassium carbonate. The newly synthesized compound were characterized by 1 H NMR, IR, Mass and screened for their antimicrobial activity against various strains of bacteria and fungi. From the synthesized different NCEs, compounds 8a, 8d and 8e are broad spectrum drug which can inhibit the growth of gram positive, gram negative bacteria and fungi.

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Synthesis and BZR affinity of pyrazolo[1,5-a]pyrimidine derivatives. part 1: study of the structural features for BZR recognition

Cited by 29 publications

References 16 publications

Unusual heterocyclization of chalcone podands with 3-amino-1,2,4-triazole

Unusual heterocyclization of chalcone podands with 3-amino-1,2,4-triazole

Allosteric GABAA Receptor Modulators—A Review on the Most Recent Heterocyclic Chemotypes and Their Synthetic Accessibility

Synthesis, Characterization and Biological Evaluation of some Novel Pyrazolo[1,5-a]Pyrimidine Derivatives

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