Samuel Desta
Shandong University
5 Papers
Samuel Desta is an academic researcher from Shandong University. The author has contributed to research in topics: Chemistry & Neuraminidase. The author has an hindex of 5, co-authored 5 publications.
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Papers
Optimization of N-Substituted Oseltamivir Derivatives as Potent Inhibitors of Group-1 and -2 Influenza A Neuraminidases, Including a Drug-Resistant Variant
Jian Zhang,Vasanthanathan Poongavanam,Dongwei Kang,Chiara Bertagnin,Huamei Lu,Xiujie Kong,Han Ju,Xueyi Lu,Ping Gao,Ye Tian,Haiyong Jia,Samuel Desta,Xiao Ding,Lin Sun,Zengjun Fang,Boshi Huang,Xuewu Liang,Ruifang Jia,Xiuli Ma,Wenfang Xu,Natarajan Arul Murugan,Arianna Loregian,Bing Huang,Peng Zhan,Xinyong Liu +24 more
TL;DR: The successful exploitation of the 150-cavity of NAs represents an important breakthrough in the development of more potent anti-influenza agents and Computational modeling and molecular dynamics studies provided insights into the role of R group of 15b in improving potency toward group-1 and -2 NAs.
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Exploring the hydrophobic channel of NNIBP leads to the discovery of novel piperidine-substituted thiophene[3,2-d]pyrimidine derivatives as potent HIV-1 NNRTIs
Dongwei Kang,Da Feng,Tiziana Ginex,Jinmi Zou,Fenju Wei,Tong Zhao,Boshi Huang,Yanying Sun,Samuel Desta,Erik De Clercq,Christophe Pannecouque,Peng Zhan,Xinyong Liu +12 more
TL;DR: A series of novel piperidine-substituted thiophene[3,2-d]pyrimidine derivatives designed to explore the hydrophobic channel of the non-nucleoside reverse transcriptase inhibitors binding pocket by incorporating an aromatic moiety to the left wing of the lead K-5a2 hold great promise as a potential drug candidate for the treatment of HIV-1 infection.
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Discovery of Novel Diarylpyrimidine Derivatives as Potent HIV-1 NNRTIs Targeting the "NNRTI Adjacent" Binding Site.
Zhipeng Huo,Heng Zhang,Dongwei Kang,Zhongxia Zhou,Gaochan Wu,Samuel Desta,Xiaofang Zuo,Zhao Wang,Lanlan Jing,Xiao Ding,Dirk Daelemans,Erik De Clercq,Christophe Pannecouque,Peng Zhan,Xinyong Liu +14 more
TL;DR: A novel series of diarylpyrimidine derivatives, which could simultaneously occupy the classical NNRTIs binding pocket (NNIBP) and the newly reported "NNRTI Adjacent" binding site, were designed, synthesized, and evaluated for their antiviral activities in MT-4 cell cultures and demonstrated excellent activities against wild-type HIV-1 strain.
Design, synthesis and biological evaluation of "Multi-Site"-binding influenza virus neuraminidase inhibitors.
Ruifang Jia,Jian Zhang,Wei Ai,Xiao Ding,Samuel Desta,Lin Sun,Zhuosen Sun,Xiuli Ma,Zhong Li,Defeng Wang,Bing Huang,Peng Zhan,Xinyong Liu +12 more
TL;DR: Compound 15e, the most potent N1-selective inhibitor targeting 150-cavity, showed 1.5 and 1.8 times greater activity than oseltamivir carboxylate (OSC) against N1 (H5N1) and N 1 (H 5N1-H274Y), and may lead to further investigation of more potent anti-influenza agents.
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Design, synthesis, and evaluation of novel heteroaryldihydropyrimidine derivatives as non-nucleoside hepatitis B virus inhibitors by exploring the solvent-exposed region.
Yu Ji,Haiyong Jia,Xiaowei Guo,Samuel Desta,Zhang Shuo,Jian Zhang,Xiao Ding,Xiaohong Liang,Xinyong Liu,Peng Zhan +9 more
TL;DR: The solvent‐exposed protein region of heteroaryldihydropyrimidine derivatives is explored and the morpholine ring of GLS4 was replaced with substituted sulfonamides and triazoles to generate novel non‐nucleoside HBV inhibitors with desirable potency.
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