1,720,991 research outputs found
A novel approach to quinazolin-4(3H)-one via quinazoline oxidation: an improved synthesis of 4-anilinoquinazolines
No full textA novel strategy to prepare 4-anilinoquinazoline derivatives based on the oxidation of the quinazoline ring is described. Quinazoline oxidation has been investigated and improved, thus leading to an efficient and high yielding method to quinazolin-4(3H)-ones. Efficiency of this approach has been evaluated
synthesizing four well known tyrosine kinase inhibitors and comparing the obtained yields with those achievable through conventional synthetic methods
A novel convenient synthesis of benzoquinazolines
No full textA novel synthetic pathway to benzoquinazolines from naphthylamines is reported. Benzoquinazoline nucleus was cyclized in good yield from N-protected naphthylamines using hexamethylenetetramine in TFA and potassium ferricyanide in aqueous ethanolic KOH. This method is efficient and convenient with respect to previously reported synthetic pathways
Synthesis of methyl derivatives of linear and angular thienocoumarins and thiopyranocoumarins
No full textNew linear and angular thienocoumarins and thiopyranocoumarins were synthesized. The key intermediates were appropriate methyl derivatives of 7-mercaptocoumarin, which were condensed with chloroketones or propargyl chloride. Thioethers were cyclized under various conditions in order to determine which methods produced the best yields of the desired thienocoumarins and thiopyranocoumarins
Synthesis of coumarin compounds as CK2 inhibitors.
No full textProtein kinase CK2 is ubiquitous, essential and highly pleiotropic kinase whose abnormally high constitutive activity is suspected to underlie its pathogenic potential in neoplasia and possible implication in viral infections. CK2 is a messenger-independent protein serine/threonine kinase with more than 300 protein substrates and is implicated in many cellular functions [1, 2]. Recently some halogen-substitute 4-methylcoumarins has shown a good biological inhibitory activity. In this work is described the synthesis of new substitute coumarins and was made a preliminary structure-activity relationship through comparison with data in literature [3]. 2 goals are persecuted: verify the importance of hydroxy group in 7 position of the 3,8-dibromo-7-hydroxy-4-methylcoumarin (DBC) [3] to maintain biological activities; study how various substituent in 4-position can influence the IC50 of literature compounds.
The structures of novel coumarin compounds as CK2 inhibitors are summarized in figure
METHYLTRIAZOLOCOUMARINS - NEW FUROCOUMARIN ISOSTERS AS POTENTIAL PHOTOCHEMOTHERAPEUTIC AGENTS
No full textA number of new methyltriazolocoumarins were synthesized. The synthesis was performed starting from the appropriate methylated 7-aminocoumarins which were nitrated, reduced and diazotized with concomitant cyclization to form the triazole ring
Synthesis of some benzo[c][2,6]naphthyridin-5-ones and new tetracyclic benzofuro[4,5-c]-2,6-naphthyridin-5(6H)-ones
No full textA series of novel methylbenzofuro[4,5-c]-2,6-naphthyridin-5(6H)-ones were synthesized, first building the pyridine nucleus on the appropriated quinolin-2-ones, and then condensing the furan ring on the preconstituted benzonaphthyridinones. The benzo[c][2,6]naphthyridinic nucleus was also interesting for its known pharmacological properties, as well as intermediate for the synthesis of natural product analogues
Uso di nuovi composti endocannabinoido simili, nonché metodo di preparazione e composizioni farmaceutiche ottenibili con gli stessi.
No full textL'invenzione trova applicazione nel campo della farmacologia e dei composti a struttura N-acilamminoacidica ad uso terapeutico e ha per oggetto l'uso di nuovi composti endocannabinoido-simili o esteri o sali farmaceuticamente accettabili degli stessi, per la preparazione di composizioni farmaceutiche per la prevenzione o il trattamento di stati patologici
Synthesis of furo[3,2-g][1,4]benzoxazin-3-ones, new psoralen isosters
No full textFurobenzoxazin-3-one, a new tricyclic nucleus, was synthesised in two different and straightforward routes: the first route consisted of condensing a furan ring onto a preconstituted 1,4-benzoxazinone nucleus, and the other in condensing a 1,4-oxazine ring onto the appropriate benzofuran system obtained from coumarin by ring contraction
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