Organocatalyzed highly atom economic one pot synthesis of tetrahydropyridines as antimalarials

Mridul Misra; Swaroop Kumar Pandey; Vivek Parashar Pandey; Jyoti Pandey; Renu Tripathi; Rama Pati Tripathi

doi:10.1016/j.bmc.2008.11.062

Organocatalyzed highly atom economic one pot synthesis of tetrahydropyridines as antimalarials

Mridul Misra, Swaroop Kumar Pandey, Vivek Parashar Pandey, Jyoti Pandey, Renu Tripathi, Rama Pati Tripathi

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

214 Scopus citations

Abstract

A highly atom economic one pot synthesis of tetrahydropyridines was achieved by l-proline/TFA catalysed multicomponent reaction of β-keto-esters, aromatic aldehydes and anilines. The synthesized compounds were screened against Plasmodium falciparum in vitro and one of them showed antimalarial activity with MIC as low as 0.09 μg/mL.

Original language	English
Pages (from-to)	625-633
Number of pages	9
Journal	Bioorganic and Medicinal Chemistry
Volume	17
Issue number	2
DOIs	https://doi.org/10.1016/j.bmc.2008.11.062
State	Published - 15 Jan 2009
Externally published	Yes

Keywords

Antimalarial activity
Organocatalysis
Schizont maturation
Tetrahydropyridines
Trifluoroacetic acid
l-Proline

ASJC Scopus subject areas

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

UN SDGs

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

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10.1016/j.bmc.2008.11.062

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title = "Organocatalyzed highly atom economic one pot synthesis of tetrahydropyridines as antimalarials",

abstract = "A highly atom economic one pot synthesis of tetrahydropyridines was achieved by l-proline/TFA catalysed multicomponent reaction of β-keto-esters, aromatic aldehydes and anilines. The synthesized compounds were screened against Plasmodium falciparum in vitro and one of them showed antimalarial activity with MIC as low as 0.09 μg/mL.",

keywords = "Antimalarial activity, Organocatalysis, Schizont maturation, Tetrahydropyridines, Trifluoroacetic acid, l-Proline",

author = "Mridul Misra and Pandey, {Swaroop Kumar} and Pandey, {Vivek Parashar} and Jyoti Pandey and Renu Tripathi and Tripathi, {Rama Pati}",

note = "Funding Information: Authors thank ICMR and DBT New Delhi for financial assistance. V.P. and J.P. thank CSIR New Delhi for JRF and SRF, respectively. It is a CDRI Communication No. 7466. ",

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doi = "10.1016/j.bmc.2008.11.062",

language = "English",

volume = "17",

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journal = "Bioorganic and Medicinal Chemistry",

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T1 - Organocatalyzed highly atom economic one pot synthesis of tetrahydropyridines as antimalarials

AU - Misra, Mridul

AU - Pandey, Swaroop Kumar

AU - Pandey, Vivek Parashar

AU - Pandey, Jyoti

AU - Tripathi, Renu

AU - Tripathi, Rama Pati

N1 - Funding Information: Authors thank ICMR and DBT New Delhi for financial assistance. V.P. and J.P. thank CSIR New Delhi for JRF and SRF, respectively. It is a CDRI Communication No. 7466.

PY - 2009/1/15

Y1 - 2009/1/15

N2 - A highly atom economic one pot synthesis of tetrahydropyridines was achieved by l-proline/TFA catalysed multicomponent reaction of β-keto-esters, aromatic aldehydes and anilines. The synthesized compounds were screened against Plasmodium falciparum in vitro and one of them showed antimalarial activity with MIC as low as 0.09 μg/mL.

AB - A highly atom economic one pot synthesis of tetrahydropyridines was achieved by l-proline/TFA catalysed multicomponent reaction of β-keto-esters, aromatic aldehydes and anilines. The synthesized compounds were screened against Plasmodium falciparum in vitro and one of them showed antimalarial activity with MIC as low as 0.09 μg/mL.

KW - Antimalarial activity

KW - Organocatalysis

KW - Schizont maturation

KW - Tetrahydropyridines

KW - Trifluoroacetic acid

KW - l-Proline

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U2 - 10.1016/j.bmc.2008.11.062

DO - 10.1016/j.bmc.2008.11.062

M3 - Article

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AN - SCOPUS:58549088118

SN - 0968-0896

VL - 17

SP - 625

EP - 633

JO - Bioorganic and Medicinal Chemistry

JF - Bioorganic and Medicinal Chemistry

IS - 2

ER -

Organocatalyzed highly atom economic one pot synthesis of tetrahydropyridines as antimalarials

Abstract

Keywords

ASJC Scopus subject areas

UN SDGs

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