60467-72-3Relevant articles and documents
Potential antidepressants: Pharmacology of 2-(4-methyl piperazin-1-yl)-1,8- naphthyridine-3-carbonitrile in rodent behavioural models
Mahesh,Rajkumar, Ramamoorthy,Minasri,Venkatesha Perumal
, p. 919 - 924 (2007)
Serotonin type 3 (5-HT3) antagonists, which find an unflinching place in the management of nausea and emesis are presently screened for their neuro-pharmacological potential in various animal models. In the present study, 2-(4-methyl piperazin-1-yl)-1,8-naphthyridine-3-carbonitrile (NA-2) with an optimal log P and pA2 value comparable to that of ondansetron was screened in rodent models of depression. The acute and chronic (14 days) treatment of the synthetic compound exhibited antidepressant-like effects at the lower dose levels in mice forced swim test (FST). A typical and similar dose-immobility profile was observed in both mice FST and tail suspension test (TST). Interaction studies in FST revealed the reversal of mCPP induced immobility, attenuation of antidepressant effects of fluoxetine and desipramine. Chronic NA-2 treatment restored the behavioural deficits in olfactory bulbectomized (OBX) rats as indicated by reduction in hyperactivity in novel open field test. This preliminary study points to a serotonergic mechanism behind the antidepressant-like effects of NA-2 and invigorates further investigation of analogous compounds in various other models of depression.
A flexible synthesis of naphthyridine derivatives through diazotization, triflation, and Suzuki reaction
Shireen Mohammed, Maher Khalid
, p. 21 - 25 (2021/06/12)
A facile and suitable method for the synthesis of different 1,8-Naphthyridine derivatives is depicted. The procedure is based on the diazotization and triflation reactions of commercially available 1,8-naphthyridine-2-amines followed by cross-coupling with aromatic and heteroaromatic boronic acids through Suzuki reaction. These processes reserved the required yields in high percentage. All synthesized compounds were identified by spectral data.
Design, synthesis, and preliminary in vitro and in vivo pharmacological evaluation of 2-{4-[4-(2,5-disubstituted thiazol-4-yl)phenylethyl]piperazin-1- yl}-1,8-naphthyridine-3-carbonitriles as atypical antipsychotic agents
Gowri Chandra Sekhar, Kondapalli Venkata,Rao, Vajja Samabasiva,Deuther-Conrad, Winnie,Reddy, Aravalli Satish,Brust, Peter,Krishna Kumar, Mutyala Murali
scheme or table, p. 561 - 568 (2012/06/01)
A series of 2-{4-[4-(2,5-disubstituted thiazolyl)phenylethyl] piperazin-1-yl}-1,8-naphthyridine-3-carbonitriles were synthesized in an effort to prepare novel atypical antipsychotic agents. The compounds were synthesized either by microwave irradiation technique or by conventional synthesis and were characterized by spectral data (IR, 1H NMR, and MS) and the purity was ascertained by microanalysis. The D2 and 5-HT2A affinity of the synthesized compounds was screened in vitro by radioligand displacement assays on membrane homogenates isolated from rat striatum and rat cortex, respectively. Furthermore, all the synthesized compounds were screened for their in vivo pharmacological activity in Swiss albino mice. The D 2 antagonism studies were performed using climbing mouse assay model and 5-HT2A antagonism studies were performed using quipazine-induced head twitches in mice. It was observed that none of the new chemical entities exhibited catalepsy and 10f is the most active among the synthesized compounds with 5-HT2A/D2 ratio of 1.1286 although the standard drug risperidone exhibited 5-HT2A/D2 ratio of 1.0989.
