1,2,3-triazolo[1.5-a]quinazolines: synthesis, benzodiazepine receptor binding and theoretical calculations.
This paper reports the synthesis of 3-substituted-1,2,3-triazolo[1,5-a]quinazolin-5-ones prepared by 1,3-dipolar cycloaddition reaction of 2-azidobenzoic acid to methylenic compounds activated by a cyano group. The new derivatives were submitted to benzodiazepine receptor binding assays: the results indicated an interesting receptorial affinity of the 1,2,3-triazolo[1,5-a]quinazoline ring. On the basis of the biological results, theoretical calculations were performed, which suggested useful structural modifications.
Biagi
G
G
Dipartimento di Scienze Farmaceutiche, Facolta di Farmacia, Universita di Pisa, Italy.
Giorgi
I
I
Livi
O
O
Scartoni
V
V
Velo
S
S
Lucacchini
A
A
Senatore
G
G
De Santis
B
B
Martinelli
A
A
D000818:Animals; D002417:Cattle; D005442:Flumazenil / Q000378:metabolism; D011799:Quinazolines / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology; D011963:Receptors, GABA-A / Q000187:drug effects* / Q000378:metabolism; D013329:Structure-Activity Relationship
D011799:Quinazolines; D011963:Receptors, GABA-A; D005442:Flumazenil