Application In Synthesis of 1-Methyl-4-piperidoneIn 2020 ,《Screening and Phenotypical Characterization of Schistosoma mansoni Histone Deacetylase 8 (SmHDAC8) Inhibitors as Multistage Antischistosomal Agents》 was published in ACS Infectious Diseases. The article was written by Saccoccia, Fulvio; Brindisi, Margherita; Gimmelli, Roberto; Relitti, Nicola; Guidi, Alessandra; Saraswati, A. Prasanth; Cavella, Caterina; Brogi, Simone; Chemi, Giulia; Butini, Stefania; Papoff, Giuliana; Senger, Johanna; Herp, Daniel; Jung, Manfred; Campiani, Giuseppe; Gemma, Sandra; Ruberti, Giovina. The article contains the following contents:
Schistosomiasis (also known as bilharzia) is a neglected tropical disease caused by platyhelminths of the genus Schistosoma. The disease is endemic in tropical and subtropical areas of the world where water is infested by the intermediate parasite host, the snail. More than 800 million people live in endemic areas and more than 200 million are infected and require treatment. Praziquantel (PZQ) is the drug of choice for schistosomiasis treatment and transmission control being safe and very effective against adult worms of all the clin. relevant Schistosoma species. Unfortunately, it is ineffective on immature, juvenile worms, therefore it does not prevent reinfection. Moreover, the risk of development and spread of drug resistance strains due to the wide use of a single drug in such a large population represents a serious threat. Therefore, research aimed to identifying novel drugs to be used alone or in combination with PZQ are needed. Histone deacetylase 8 (HDAC8) from the parasite Schistosoma mansoni is a class I zinc-dependent HDAC which is abundantly expressed in all stages of its life cycle, thus representing an interesting target for drug discovery. Through virtual screening and phenotypical characterization of selected hits, the authors discovered two main chem. classes of compounds characterized by the presence of a hydroxamate-based metal binding group coupled to a spiroindoline or a tricyclic thieno[3,2-b]indole core as capping groups. Some of the compounds of both classes were deeply investigated and showed to impair viability of larval, juvenile, and adult schistosomes, to impact egg production in vitro and/or to induce morphol. alterations of the adult schistosome reproductive systems. Noteworthy, all of them inhibit the recombinant form of SmHDAC8 enzyme in vitro. Overall, the authors identified very interesting scaffolds paving the way to the development of effective antischistosomal agents. In the experimental materials used by the author, we found 1-Methyl-4-piperidone(cas: 1445-73-4Application In Synthesis of 1-Methyl-4-piperidone)
1-Methyl-4-piperidone(cas: 1445-73-4) is a member of piperidine. Piperidine is a key saturated heterocyclic scaffold found in several of the top-selling small molecule pharmaceuticals and natural alkaloids, with a diverse range of biological activities. Hence, continuous efforts have been made to develop convenient methods to prepare piperidine derivatives.Application In Synthesis of 1-Methyl-4-piperidone
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem