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Synthesis of acylguanidine zanamivir derivatives as neuraminidase inhibitors and the evaluation of their bio-activities.
Org Biomol Chem. 2013 Jun 28; 11(24):3943-8.OB

Abstract

A series of acylguanidine-modified zanamivir analogs were synthesized and their inhibitory activities against the NAs of avian influenza viruses (H1N1 and H3N2) were evaluated. In particular, zanamivir derivative , with a hydrophobic naphthalene substituent, exhibits the best inhibitory activity against group-1 NA with an IC50 of 20 nM.

Authors+Show Affiliations

Department of Chemistry, National Tsing Hua University, 101, Section 2, Kuang-Fu Road, Hsinchu 30013, Taiwan.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

23695381

Citation

Lin, Chien-Hung, et al. "Synthesis of Acylguanidine Zanamivir Derivatives as Neuraminidase Inhibitors and the Evaluation of Their Bio-activities." Organic & Biomolecular Chemistry, vol. 11, no. 24, 2013, pp. 3943-8.
Lin CH, Chang TC, Das A, et al. Synthesis of acylguanidine zanamivir derivatives as neuraminidase inhibitors and the evaluation of their bio-activities. Org Biomol Chem. 2013;11(24):3943-8.
Lin, C. H., Chang, T. C., Das, A., Fang, M. Y., Hung, H. C., Hsu, K. C., Yang, J. M., von Itzstein, M., Mong, K. K., Hsu, T. A., & Lin, C. C. (2013). Synthesis of acylguanidine zanamivir derivatives as neuraminidase inhibitors and the evaluation of their bio-activities. Organic & Biomolecular Chemistry, 11(24), 3943-8. https://doi.org/10.1039/c3ob40624e
Lin CH, et al. Synthesis of Acylguanidine Zanamivir Derivatives as Neuraminidase Inhibitors and the Evaluation of Their Bio-activities. Org Biomol Chem. 2013 Jun 28;11(24):3943-8. PubMed PMID: 23695381.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Synthesis of acylguanidine zanamivir derivatives as neuraminidase inhibitors and the evaluation of their bio-activities. AU - Lin,Chien-Hung, AU - Chang,Tsung-Che, AU - Das,Anindya, AU - Fang,Ming-Yu, AU - Hung,Hui-Chen, AU - Hsu,Kai-Cheng, AU - Yang,Jinn-Moon, AU - von Itzstein,Mark, AU - Mong,Kwok Kong T, AU - Hsu,Tsu-An, AU - Lin,Chun-Cheng, PY - 2013/5/23/entrez PY - 2013/5/23/pubmed PY - 2014/2/5/medline SP - 3943 EP - 8 JF - Organic & biomolecular chemistry JO - Org. Biomol. Chem. VL - 11 IS - 24 N2 - A series of acylguanidine-modified zanamivir analogs were synthesized and their inhibitory activities against the NAs of avian influenza viruses (H1N1 and H3N2) were evaluated. In particular, zanamivir derivative , with a hydrophobic naphthalene substituent, exhibits the best inhibitory activity against group-1 NA with an IC50 of 20 nM. SN - 1477-0539 UR - https://www.unboundmedicine.com/medline/citation/23695381/Synthesis_of_acylguanidine_zanamivir_derivatives_as_neuraminidase_inhibitors_and_the_evaluation_of_their_bio_activities_ L2 - https://doi.org/10.1039/c3ob40624e DB - PRIME DP - Unbound Medicine ER -