Synthesis, biological evaluation and molecular modeling of novel azaspiro dihydrotriazines as influenza virus inhibitors targeting the host factor dihydrofolate reductase (DHFR) was written by Francesconi, Valeria;Giovannini, Luca;Santucci, Matteo;Cichero, Elena;Costi, Maria Paola;Naesens, Lieve;Giordanetto, Fabrizio;Tonelli, Michele. And the article was included in European Journal of Medicinal Chemistry in 2018.Quality Control of 1-Benzylpiperidin-3-one hydrochloride This article mentions the following:
Recently, cycloguanil-like dihydrotriazine derivatives were identified, which provided host-factor directed antiviral activity against influenza viruses and respiratory syncytial virus (RSV), by targeting the human dihydrofolate reductase (hDHFR) enzyme. In this context, it was deemed interesting to further investigate the structure activity relationship (SAR) of our first series of cycloguanil-like dihydrotriazines, designing two novel azaspiro dihydrotriazine scaffolds. The present study allowed the exploration of the potential chem. space around these new scaffolds that are well tolerated for maintaining the antiviral effect by means of interaction with the hDHFR enzyme. The new derivatives confirmed their inhibitory profile against influenza viruses, especially type B. In particular, the two best compounds shared potent antiviral activity, (I: EC50 = 0.29 渭M; II: EC50 = 0.19 渭M), which was comparable to that of zanamivir (EC50 = 0.14 渭M), and better than that of ribavirin (EC50 = 3.2 渭M). In addition, these two compounds proved to be also effective against RSV (I: EC50 = 0.40 渭M, SI 鈮?250; II: EC50 = 1.8 渭M, SI 鈮?56), surpassing the potency and selectivity index (SI) of ribavirin (EC50 = 5.8 渭M, SI > 43). In perspective, the above adequately substituted azaspiro dihydrotriazines may represent valuable hit compounds worthy of further structural optimization to develop improved host DHFR-directed antiviral agents. In the experiment, the researchers used many compounds, for example, 1-Benzylpiperidin-3-one hydrochloride (cas: 50606-58-1Quality Control of 1-Benzylpiperidin-3-one hydrochloride).
1-Benzylpiperidin-3-one hydrochloride (cas: 50606-58-1) belongs to piperidine derivatives. Piperidine is a saturated organic heteromonocyclic parent, an azacycloalkane, a secondary amine and a member of piperidines. Some chemotherapeutic agents have piperidine moiety within their structure, foremost among them, vinblastine and raloxifene.Quality Control of 1-Benzylpiperidin-3-one hydrochloride
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem