Synthesis and in vitro evaluation of pteridine analogues as monoamine oxidase B and nitric oxide synthase inhibitors

Synthesis and evaluation of fluorescent heterocyclic aminoadamantanes as multifunctional neuroprotective agents

“…The antioxidant activity of the synthesised compounds is related to their electron or hydrogen radical releasing ability to DPPH + so that it becomes a stable diamagnetic molecule. The average percentage DPPH + radical scavenging abilities of all the adamantine heterocyclic derivatives (7)(8)(9)(10)(11)(12) were lower than of Trolox Ò , but it was evident that these derivatives showed high reducing ability (possibly by hydrogen atom transfer) and could serve as free-radical scavengers. Compound 8 showed the most promising activity inhibiting the radical to 91.68%.…”

“…Three positive controls were also included: MK-801, a commercially available potent high affinity NMDAR channel blocker, amantadine (1) and NGP1-01 (3). The results (Table 1) indicated that at a concentration of 100 lM, compounds 9 (17%), 10 (19.25%), 8 (20.29%) and 11 (21.95%) showed statistically significant (p < 0.05) blockage of the NMDAR and attenuated calcium flux into the cells better than the references NGP1-01 (3; 13.37%) and (7,8,9) and amine (10,11,12) conjugates.…”

“…The compounds (7)(8)(9)(10)(11)(12) showed inhibition of 27.41-91.68%. Trolox Ò , used as a standard, has concentration dependant values ranging from 45.80-95.14%.…”

“…The anthranilic indazole and coumarin complexes were obtained through the intermediate complexes with N,N-carbonyldiimidazole (CDI) and yielded the amides (7,8,9) on reaction with the primary amine. The dinitrobenzene and dansyl complexes (10,11) were obtained through amination with the primary amine of amantadine. The fluorescent isoindole (12) was obtained by reaction of between o-phthaldialdehyde (OPD) and amantadine in the presence of sodium cyanide.…”

“…9,10 From the above discussion it is clear that neurodegenerative disorders are complex diseases with multiple pathways which contribute to their etiology and finally cell death of CNS neurons. 11 A drug with a single-target mechanism of action cannot always compensate for, or correct these complex pathways. Polypharmaceutical approaches have been applied as a means of multiple targeting in a clinical setting, wherein several drugs act independently on various biological targets of the disease.…”