5-Aminopyrazole-4-carboxamide analogues are selective inhibitors of Plasmodium falciparum microgametocyte exflagellation and potential malaria transmission blocking agents

Wenlin Huang; Matthew A. Hulverson; Zhongsheng Zhang; Ryan Choi; Kevin J. Hart; Mark Kennedy; Rama Subba Rao Vidadala; Dustin J. Maly; Wesley C. Van Voorhis; Scott E. Lindner; Erkang Fan; Kayode K. Ojo

doi:10.1016/j.bmcl.2016.10.014

5-Aminopyrazole-4-carboxamide analogues are selective inhibitors of Plasmodium falciparum microgametocyte exflagellation and potential malaria transmission blocking agents

Wenlin Huang
, Matthew A. Hulverson
, Zhongsheng Zhang
, Ryan Choi
, Kevin J. Hart
, Mark Kennedy
, Rama Subba Rao Vidadala
, Dustin J. Maly
, Wesley C. Van Voorhis
, Scott E. Lindner
, Erkang Fan
, Kayode K. Ojo

Research output: Contribution to journal › Article › peer-review

18 Scopus citations

Abstract

Plasmodium falciparum calcium-dependent protein kinase 4 (PfCDPK4) is essential for the exflagellation of male gametocytes. Inhibition of PfCDPK4 is an effective way of blocking the transmission of malaria by mosquitoes. A series of 5-aminopyrazole-4-carboxamide analogues are demonstrated to be potent inhibitors of PfCDPK4. The compounds are also able to block exflagellation of Plasmodium falciparum male gametocytes without observable toxicity to mammalian cells.

Original language	English (US)
Pages (from-to)	5487-5491
Number of pages	5
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	26
Issue number	22
DOIs	https://doi.org/10.1016/j.bmcl.2016.10.014
State	Published - 2016

All Science Journal Classification (ASJC) codes

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

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10.1016/j.bmcl.2016.10.014

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Huang, W., Hulverson, M. A., Zhang, Z., Choi, R., Hart, K. J., Kennedy, M., Vidadala, R. S. R., Maly, D. J., Van Voorhis, W. C., Lindner, S. E., Fan, E., & Ojo, K. K. (2016). 5-Aminopyrazole-4-carboxamide analogues are selective inhibitors of Plasmodium falciparum microgametocyte exflagellation and potential malaria transmission blocking agents. Bioorganic and Medicinal Chemistry Letters, 26(22), 5487-5491. https://doi.org/10.1016/j.bmcl.2016.10.014

@article{d36be3e806cb41cdb3980b48fd9c0c9e,

title = "5-Aminopyrazole-4-carboxamide analogues are selective inhibitors of Plasmodium falciparum microgametocyte exflagellation and potential malaria transmission blocking agents",

abstract = "Plasmodium falciparum calcium-dependent protein kinase 4 (PfCDPK4) is essential for the exflagellation of male gametocytes. Inhibition of PfCDPK4 is an effective way of blocking the transmission of malaria by mosquitoes. A series of 5-aminopyrazole-4-carboxamide analogues are demonstrated to be potent inhibitors of PfCDPK4. The compounds are also able to block exflagellation of Plasmodium falciparum male gametocytes without observable toxicity to mammalian cells.",

author = "Wenlin Huang and Hulverson, \{Matthew A.\} and Zhongsheng Zhang and Ryan Choi and Hart, \{Kevin J.\} and Mark Kennedy and Vidadala, \{Rama Subba Rao\} and Maly, \{Dustin J.\} and \{Van Voorhis\}, \{Wesley C.\} and Lindner, \{Scott E.\} and Erkang Fan and Ojo, \{Kayode K.\}",

note = "Publisher Copyright: {\textcopyright} 2016 Elsevier Ltd",

year = "2016",

doi = "10.1016/j.bmcl.2016.10.014",

language = "English (US)",

volume = "26",

pages = "5487--5491",

journal = "Bioorganic and Medicinal Chemistry Letters",

issn = "0960-894X",

publisher = "Elsevier Ltd",

number = "22",

}

Huang, W, Hulverson, MA, Zhang, Z, Choi, R, Hart, KJ, Kennedy, M, Vidadala, RSR, Maly, DJ, Van Voorhis, WC, Lindner, SE, Fan, E & Ojo, KK 2016, '5-Aminopyrazole-4-carboxamide analogues are selective inhibitors of Plasmodium falciparum microgametocyte exflagellation and potential malaria transmission blocking agents', Bioorganic and Medicinal Chemistry Letters, vol. 26, no. 22, pp. 5487-5491. https://doi.org/10.1016/j.bmcl.2016.10.014

5-Aminopyrazole-4-carboxamide analogues are selective inhibitors of Plasmodium falciparum microgametocyte exflagellation and potential malaria transmission blocking agents. / Huang, Wenlin; Hulverson, Matthew A.; Zhang, Zhongsheng et al.
In: Bioorganic and Medicinal Chemistry Letters, Vol. 26, No. 22, 2016, p. 5487-5491.

Research output: Contribution to journal › Article › peer-review

TY - JOUR

T1 - 5-Aminopyrazole-4-carboxamide analogues are selective inhibitors of Plasmodium falciparum microgametocyte exflagellation and potential malaria transmission blocking agents

AU - Huang, Wenlin

AU - Hulverson, Matthew A.

AU - Zhang, Zhongsheng

AU - Choi, Ryan

AU - Hart, Kevin J.

AU - Kennedy, Mark

AU - Vidadala, Rama Subba Rao

AU - Maly, Dustin J.

AU - Van Voorhis, Wesley C.

AU - Lindner, Scott E.

AU - Fan, Erkang

AU - Ojo, Kayode K.

PY - 2016

Y1 - 2016

N2 - Plasmodium falciparum calcium-dependent protein kinase 4 (PfCDPK4) is essential for the exflagellation of male gametocytes. Inhibition of PfCDPK4 is an effective way of blocking the transmission of malaria by mosquitoes. A series of 5-aminopyrazole-4-carboxamide analogues are demonstrated to be potent inhibitors of PfCDPK4. The compounds are also able to block exflagellation of Plasmodium falciparum male gametocytes without observable toxicity to mammalian cells.

AB - Plasmodium falciparum calcium-dependent protein kinase 4 (PfCDPK4) is essential for the exflagellation of male gametocytes. Inhibition of PfCDPK4 is an effective way of blocking the transmission of malaria by mosquitoes. A series of 5-aminopyrazole-4-carboxamide analogues are demonstrated to be potent inhibitors of PfCDPK4. The compounds are also able to block exflagellation of Plasmodium falciparum male gametocytes without observable toxicity to mammalian cells.

UR - https://www.scopus.com/pages/publications/84993967685

UR - https://www.scopus.com/pages/publications/84993967685#tab=citedBy

U2 - 10.1016/j.bmcl.2016.10.014

DO - 10.1016/j.bmcl.2016.10.014

M3 - Article

C2 - 27780638

AN - SCOPUS:84993967685

SN - 0960-894X

VL - 26

SP - 5487

EP - 5491

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 22

ER -

5-Aminopyrazole-4-carboxamide analogues are selective inhibitors of Plasmodium falciparum microgametocyte exflagellation and potential malaria transmission blocking agents

Abstract

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