98294-48-5Relevant academic research and scientific papers
Synthesis and structure-affinity relationships at the central benzodiazepine receptor of pyridazino[4,3-b]indoles and Indeno[1,2-c]pyridazines
Campagna,Palluotto,Carotti,Casini,Genchi
, p. 1533 - 1538 (2007/10/03)
A series of 2-aryl-3-chloro-2H-pyridazino[4,3-b]indoles, 2-aryl-3-methoxy-2H-pyridazino[4,3-b]indoles, and 2-aryl-2,5-dihydroindeno[1,2-c]pyridazino-3(3H)-ones has been prepared and tested for their ability to inhibit the [3H]flunitrazepam binding to the central benzodiazepine receptor. SAR are presented and discussed in comparison with existing pharmacophore models. Copyright (C) 1999 Elsevier Science Ltd.
Structure-activity relationships of 2-Aryl-2,5-dihydropyridazino [4,3-b]indol-3(3H)-ones at the benzodiazepine receptor
Palluotto,Carotti,Casini,Campagna,Genchi,Rizzo,De Sarro
, p. 2091 - 2104 (2007/10/03)
A large series of 2-aryl-2,5-dihydropyridazino[4,3-b]indol-3(3H)ones (PIs) carrying properly selected substituents at the indole and N2-phenyl rings was prepared and tested as central benzodiazepine receptor (BZR) ligands and potential (anti)convulsant agents. Stereoelectronic requirements for high receptor affinity were detected by means of 2-D and 3-D QSAR analyses. BZR affinities and pharmacological profiles of the compounds were examined in comparison with some other pyridazinoindolones recently described by us and with pyrazoloquinoline (PQ) analogues. An anticonvulsant activity greater than PQs was generally observed for PIs. Notably, in the test of audiogenically induced seizures, one compound showed a potency comparable to that of diazepam.
A STUDY OF THE INTRAMOLECULAR CYCLIZATION OF ESTERS OF 3-ARYLAZOINDOL-2-YLACETIC ACIDS
Trofimov, F. A.,Garnova, V. I.,Tsyshkova, N. G.
, p. 538 - 541 (2007/10/02)
A method is proposed for the synthesis of the new heterocyclic system pyridazinoindole which is based on the intramolecular condensation of ethyl 3-arylazoindol-2-ylacetates in the presence of bases.
