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Design, synthesis and biological evaluation of sulfamethazine derivatives as potent neuraminidase inhibitors.

ABSTRACT: Aim: The purpose of this study is to design and synthesize a new series of sulfamethazine derivatives as potent neuraminidase inhibitors. Materials & methods: A sulfamethazine lead compound, ZINC670537, was first identified by structure-based virtual screening technique, then some novel inhibitors X1-X10 based on ZINC670537 were designed and synthesized. Results: Compound X3 exerts the most good potency in inhibiting the wild-type H5N1 NA (IC50 = 6.74 μM) and the H274Y mutant NA (IC50 = 21.09 μM). 150-cavity occupation is very important in determining activities of these inhibitors. The sulfamethazine moiety also plays an important role. Conclusion: Compound X3 maybe regard as a good anti-influenza candidate to preform further study.

SUBMITTER: Cheng LP 

PROVIDER: S-EPMC11244698 | biostudies-literature | 2024

REPOSITORIES: biostudies-literature

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Design, synthesis and biological evaluation of sulfamethazine derivatives as potent neuraminidase inhibitors.

Cheng Li Ping LP   Zhang Xing Yong XY   Pang Wan W   Xiao Xiu Zhen XZ  

Future medicinal chemistry 20240510 12

<b>Aim:</b> The purpose of this study is to design and synthesize a new series of sulfamethazine derivatives as potent neuraminidase inhibitors. <b>Materials & methods:</b> A sulfamethazine lead compound, <b>ZINC670537</b>, was first identified by structure-based virtual screening technique, then some novel inhibitors <b>X1-X10</b> based on <b>ZINC670537</b> were designed and synthesized. <b>Results:</b> Compound <b>X3</b> exerts the most good potency in inhibiting the wild-type H5N1 NA (IC<sub>  ...[more]

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