《In situ click chemistry-based rapid discovery of novel HIV-1 NNRTIs by exploiting the hydrophobic channel and tolerant regions of NNIBP》 was published in European Journal of Medicinal Chemistry in 2020. These research results belong to Kang, Dongwei; Feng, Da; Jing, Lanlan; Sun, Yanying; Wei, Fenju; Jiang, Xiangyi; Wu, Gaochan; De Clercq, Erik; Pannecouque, Christophe; Zhan, Peng; Liu, Xinyong. Related Products of 3764-01-0 The article mentions the following:
HIV-1 RT has been considered as one of the most important targets for the development of anti-HIV-1 drugs for their well-solved three-dimensional structure and well-known mechanism of action. In this study, with HIV-1 RT as target, we used miniaturized parallel click chem. synthesis via CuAAC reaction followed by in situ biol. screening to discover novel potent HIV-1 NNRTIs. A 156 triazole-containing inhibitor library was assembled in microtiter plates and in millimolar scale. The enzyme inhibition screening results showed that 22 compounds exhibited improved inhibitory activity. Anti-HIV-1 activity results demonstrated that A3N19 effected the most potent activity against HIV-1 IIIB (EC50 = 3.28 nM) and mutant strain RES056 (EC50 = 481 nM). The mol. simulation anal. suggested that the hydrogen bonding interactions of A3N19 with the main chain of Lys101 and Lys104 was responsible for its potency. Overall, the results indicated the in situ click chem.-based strategy was rational and might be amenable for the future discovery of more potent HIV-1 NNRTIs.2,4,6-Trichloropyrimidine(cas: 3764-01-0Related Products of 3764-01-0) was used in this study.
2,4,6-Trichloropyrimidine(cas: 3764-01-0) is a member of organic chlorides. Almost all organochlorine compounds are synthesized. It is widely used as intermediates, solvents and pesticides of chemical synthetic products.Related Products of 3764-01-0
Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia