Li, Daxiong; Zhang, Chunsheng; Ding, Wei; Huang, Siming; Yu, Le; Lu, Nan; Pan, Wenkai; Li, Yiming; De Clercq, Erik; Pannecouque, Christophe; Zhang, Hongbing; Wang, Yueping; He, Yanping; Chen, Fener published their research in Chinese Chemical Letters in 2021. The article was titled 《Structure-based linker optimization of 6-(2-cyclohexyl-1-alkyl)-2-(2-oxo-2-phenylethylsulfanyl)pyrimidin-4(3H)-ones as potent non-nucleoside HIV-1 reverse transcriptase inhibitors》.Name: Diethyl 2-methylmalonate The article contains the following contents:
Most of these new compounds showed moderate to good activities against wild type HIV-1 with IC50 values ranging from 7.55μmol/L to 0.018μmol/L. Most of these new compounds I showed moderate to good activities against wild type HIV-1 with IC50 values ranging from 7.55μmol/L to 0.018μmol/L. Among them, compound I [R1 = Me; R2 = Et; R3 = H] [II] was identified as the most promising inhibitor against HIV-1 replication with an IC50 = 0.018μmol/L, CC50 = 194μmol/L, and SI = 12791, which was much more potent than the reference drugs NVP and DLV and comparable to AZT and EFV. In addition, compound [II] also exhibited improved activity against double mutant HIV-1 strain RES056 compared to that of the reference drugs NVP/DLV and DB02. The preliminary structure-activity relationship (SAR) and mol. modeling studies were also discussed, which provides some useful indications for guiding the further rational design of new S-DACO analogs. In addition to this study using Diethyl 2-methylmalonate, there are many other studies that have used Diethyl 2-methylmalonate(cas: 609-08-5Name: Diethyl 2-methylmalonate) was used in this study.
Diethyl 2-methylmalonate(cas: 609-08-5) belongs to aliphatic hydrocarbons. Aliphatic hydrocarbons belong to the most abundant fraction in crude oil. Aliphatics molecules are linear or branched open-chain structures such as n-alkanes, isoalkanes, cycloalkanes (naphthenes), terpenes and steranes.Name: Diethyl 2-methylmalonate
Referemce:
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Ester – an overview | ScienceDirect Topics