Abstract:
:The piperazine ring of the potent nootropic drug DM235 has been decorated with H-bond donor and acceptor groups (CH2OH, CH2OMe, CH2OCOMe, COOEt); the aim was to insert new functional groups, suitable for further chemical manipulation. The influence of these modifications on nootropic activity was assessed by means of the mouse passive avoidance test; some of the newly synthesized molecules (alcohol 7b, acetate 8b and ester 10d) showed interesting in vivo potency. This makes it possible to use these functional groups for adding other residues, in order to increase molecular diversity, or for anchoring a biotin group, to obtain compounds useful to capture the biological target. Moreover, the new compounds will improve our knowledge of structure activity relationships of this family of drugs.
journal_name
Bioorg Med Chemjournal_title
Bioorganic & medicinal chemistryauthors
Martino MV,Guandalini L,Di Cesare Mannelli L,Menicatti M,Bartolucci G,Dei S,Manetti D,Teodori E,Ghelardini C,Romanelli MNdoi
10.1016/j.bmc.2017.02.019subject
Has Abstractpub_date
2017-03-15 00:00:00pages
1795-1803issue
6eissn
0968-0896issn
1464-3391pii
S0968-0896(16)31459-6journal_volume
25pub_type
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