Pyrido[1,2-a]pyrimidin-4-ones as antiplasmodial falcipain-2 inhibitors

U. R. Mane; H. Li; J. Huang; R. C. Gupta; S. S. Nadkarni; R. Giridhar; P. P. Naik; M. R. Yadav

doi:10.1016/j.bmc.2012.09.008

Pyrido[1,2-a]pyrimidin-4-ones as antiplasmodial falcipain-2 inhibitors

U. R. Mane
, H. Li
, J. Huang
, R. C. Gupta
, S. S. Nadkarni
, R. Giridhar
, P. P. Naik
, M. R. Yadav^*

^*Corresponding author for this work

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

35 Scopus citations

Abstract

Plasmodium falciparum cysteine protease falcipain-2 (FP-2) is a promising target for antimalarial chemotherapy and inhibition of this protease affects the growth of parasite adversely. A series of pyrido[1,2-a]pyrimidin-4-ones were synthesized and evaluated for their in vitro FP-2 inhibitory potential. Compounds (14,17) showed excellent FP-2 inhibition and can serve as lead compounds for further development of potent FP-2 inhibitors as potential antimalarial drugs.

Original language	English
Pages (from-to)	6296-6304
Number of pages	9
Journal	Bioorganic and Medicinal Chemistry
Volume	20
Issue number	21
DOIs	https://doi.org/10.1016/j.bmc.2012.09.008
State	Published - 1 Nov 2012
Externally published	Yes

Keywords

Cysteine protease
Falcipain-2 inhibitor
Malaria
Pyrido[1,2-a]pyrimidin-4-one

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.1016/j.bmc.2012.09.008

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title = "Pyrido[1,2-a]pyrimidin-4-ones as antiplasmodial falcipain-2 inhibitors",

abstract = "Plasmodium falciparum cysteine protease falcipain-2 (FP-2) is a promising target for antimalarial chemotherapy and inhibition of this protease affects the growth of parasite adversely. A series of pyrido[1,2-a]pyrimidin-4-ones were synthesized and evaluated for their in vitro FP-2 inhibitory potential. Compounds (14,17) showed excellent FP-2 inhibition and can serve as lead compounds for further development of potent FP-2 inhibitors as potential antimalarial drugs.",

keywords = "Cysteine protease, Falcipain-2 inhibitor, Malaria, Pyrido[1,2-a]pyrimidin-4-one",

author = "Mane, \{U. R.\} and H. Li and J. Huang and Gupta, \{R. C.\} and Nadkarni, \{S. S.\} and R. Giridhar and Naik, \{P. P.\} and Yadav, \{M. R.\}",

year = "2012",

month = nov,

day = "1",

doi = "10.1016/j.bmc.2012.09.008",

language = "英语",

volume = "20",

pages = "6296--6304",

journal = "Bioorganic and Medicinal Chemistry",

issn = "0968-0896",

publisher = "Elsevier Ltd",

number = "21",

}

TY - JOUR

T1 - Pyrido[1,2-a]pyrimidin-4-ones as antiplasmodial falcipain-2 inhibitors

AU - Mane, U. R.

AU - Li, H.

AU - Huang, J.

AU - Gupta, R. C.

AU - Nadkarni, S. S.

AU - Giridhar, R.

AU - Naik, P. P.

AU - Yadav, M. R.

PY - 2012/11/1

Y1 - 2012/11/1

N2 - Plasmodium falciparum cysteine protease falcipain-2 (FP-2) is a promising target for antimalarial chemotherapy and inhibition of this protease affects the growth of parasite adversely. A series of pyrido[1,2-a]pyrimidin-4-ones were synthesized and evaluated for their in vitro FP-2 inhibitory potential. Compounds (14,17) showed excellent FP-2 inhibition and can serve as lead compounds for further development of potent FP-2 inhibitors as potential antimalarial drugs.

AB - Plasmodium falciparum cysteine protease falcipain-2 (FP-2) is a promising target for antimalarial chemotherapy and inhibition of this protease affects the growth of parasite adversely. A series of pyrido[1,2-a]pyrimidin-4-ones were synthesized and evaluated for their in vitro FP-2 inhibitory potential. Compounds (14,17) showed excellent FP-2 inhibition and can serve as lead compounds for further development of potent FP-2 inhibitors as potential antimalarial drugs.

KW - Cysteine protease

KW - Falcipain-2 inhibitor

KW - Malaria

KW - Pyrido[1,2-a]pyrimidin-4-one

UR - https://www.scopus.com/pages/publications/84867572123

U2 - 10.1016/j.bmc.2012.09.008

DO - 10.1016/j.bmc.2012.09.008

M3 - 文章

C2 - 23040894

AN - SCOPUS:84867572123

SN - 0968-0896

VL - 20

SP - 6296

EP - 6304

JO - Bioorganic and Medicinal Chemistry

JF - Bioorganic and Medicinal Chemistry

IS - 21

ER -

Pyrido[1,2-a]pyrimidin-4-ones as antiplasmodial falcipain-2 inhibitors

Abstract

Keywords

UN SDGs

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