Search for new pharmacophores for antimalarial activity. Part II: Synthesis and antimalarial activity of new 6-ureido-4-anilinoquinazolines

S. Madapa; Z. Tusi; A. Mishra; K. Srivastava; S. K. Pandey; R. Tripathi; S. K. Puri; S. Batra

doi:10.1016/j.bmc.2008.11.005

Search for new pharmacophores for antimalarial activity. Part II: Synthesis and antimalarial activity of new 6-ureido-4-anilinoquinazolines

S. Madapa, Z. Tusi, A. Mishra, K. Srivastava, S. K. Pandey, R. Tripathi, S. K. Puri, S. Batra

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

104 Scopus citations

Abstract

Synthesis of new 6-ureido-4-anilinoquinazolines have been accomplished and their in vitro antimalarial activity against chloroquine-sensitive P. falciparum have been examined. Out of 64 compounds evaluated, the IC₅₀ of 16 compounds which have displayed MIC of 0.25 μg/mL were also recorded. One of the compounds (24g) had IC₅₀ value of 2.27 ng/mL which was equipotent to the standard drug chloroquine used in the bioassay. The in vivo evaluation of a few compounds among the series led to discovery of one analog (30g) displaying 40% curative activity (28 days) against mdr P. yoeilli nigeriensis at an oral dose of 100 mg/kg × 4days.

Original language	English
Pages (from-to)	222-234
Number of pages	13
Journal	Bioorganic and Medicinal Chemistry
Volume	17
Issue number	1
DOIs	https://doi.org/10.1016/j.bmc.2008.11.005
State	Published - 1 Jan 2009
Externally published	Yes

Keywords

Antimalarial
In vitro
In vivo
P. falciparum
Quinazoline
Urea

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.2008.11.005

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title = "Search for new pharmacophores for antimalarial activity. Part II: Synthesis and antimalarial activity of new 6-ureido-4-anilinoquinazolines",

abstract = "Synthesis of new 6-ureido-4-anilinoquinazolines have been accomplished and their in vitro antimalarial activity against chloroquine-sensitive P. falciparum have been examined. Out of 64 compounds evaluated, the IC50 of 16 compounds which have displayed MIC of 0.25 μg/mL were also recorded. One of the compounds (24g) had IC50 value of 2.27 ng/mL which was equipotent to the standard drug chloroquine used in the bioassay. The in vivo evaluation of a few compounds among the series led to discovery of one analog (30g) displaying 40% curative activity (28 days) against mdr P. yoeilli nigeriensis at an oral dose of 100 mg/kg × 4days.",

keywords = "Antimalarial, In vitro, In vivo, P. falciparum, Quinazoline, Urea",

author = "S. Madapa and Z. Tusi and A. Mishra and K. Srivastava and Pandey, {S. K.} and R. Tripathi and Puri, {S. K.} and S. Batra",

note = "Funding Information: Three authors (S.M., A.M., S.K.P.) acknowledge the financial support from CSIR, New Delhi and ICMR, New Delhi in the form of fellowships. This work was supported by the DST grant to Z.T. under WOS program.",

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doi = "10.1016/j.bmc.2008.11.005",

language = "English",

volume = "17",

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journal = "Bioorganic and Medicinal Chemistry",

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T2 - Synthesis and antimalarial activity of new 6-ureido-4-anilinoquinazolines

AU - Madapa, S.

AU - Tusi, Z.

AU - Mishra, A.

AU - Srivastava, K.

AU - Pandey, S. K.

AU - Tripathi, R.

AU - Puri, S. K.

AU - Batra, S.

N1 - Funding Information: Three authors (S.M., A.M., S.K.P.) acknowledge the financial support from CSIR, New Delhi and ICMR, New Delhi in the form of fellowships. This work was supported by the DST grant to Z.T. under WOS program.

PY - 2009/1/1

Y1 - 2009/1/1

N2 - Synthesis of new 6-ureido-4-anilinoquinazolines have been accomplished and their in vitro antimalarial activity against chloroquine-sensitive P. falciparum have been examined. Out of 64 compounds evaluated, the IC50 of 16 compounds which have displayed MIC of 0.25 μg/mL were also recorded. One of the compounds (24g) had IC50 value of 2.27 ng/mL which was equipotent to the standard drug chloroquine used in the bioassay. The in vivo evaluation of a few compounds among the series led to discovery of one analog (30g) displaying 40% curative activity (28 days) against mdr P. yoeilli nigeriensis at an oral dose of 100 mg/kg × 4days.

AB - Synthesis of new 6-ureido-4-anilinoquinazolines have been accomplished and their in vitro antimalarial activity against chloroquine-sensitive P. falciparum have been examined. Out of 64 compounds evaluated, the IC50 of 16 compounds which have displayed MIC of 0.25 μg/mL were also recorded. One of the compounds (24g) had IC50 value of 2.27 ng/mL which was equipotent to the standard drug chloroquine used in the bioassay. The in vivo evaluation of a few compounds among the series led to discovery of one analog (30g) displaying 40% curative activity (28 days) against mdr P. yoeilli nigeriensis at an oral dose of 100 mg/kg × 4days.

KW - Antimalarial

KW - In vitro

KW - In vivo

KW - P. falciparum

KW - Quinazoline

KW - Urea

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M3 - Article

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AN - SCOPUS:57649158959

SN - 0968-0896

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SP - 222

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JO - Bioorganic and Medicinal Chemistry

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IS - 1

ER -

Search for new pharmacophores for antimalarial activity. Part II: Synthesis and antimalarial activity of new 6-ureido-4-anilinoquinazolines

Abstract

Keywords

ASJC Scopus subject areas

UN SDGs

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