Quinine bis-conjugates with quinolone antibiotics and peptides: synthesis and antimalarial bioassay

Siva S Panda

doi:10.1039/c2ob26439k

Quinine bis-conjugates with quinolone antibiotics and peptides: synthesis and antimalarial bioassay

Siva S Panda

Chemistry and Biochemistry

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

27 Scopus citations

Abstract

Benzotriazole-mediated syntheses led to novel bis-conjugates of quinine with quinolone antibiotics and amino acid linkers which were successfully prepared by two alternative routes with excellent yields and retention of chirality. These bis conjugates retain in vitro antimalarial activity with IC(50) values ranging from 12 to 207 nM, similar to quinine itself.

Original language	English (US)
Pages (from-to)	8985-93
Number of pages	9
Journal	Organic and Biomolecular Chemistry
Volume	10
Issue number	45
DOIs	https://doi.org/10.1039/c2ob26439k
State	Published - Dec 7 2012

Keywords

Anti-Bacterial Agents
Antimalarials
Chemistry Techniques, Synthetic
Inhibitory Concentration 50
Peptide Fragments
Plasmodium falciparum
Quinine
Quinolones
Triazoles
Journal Article
Research Support, Non-U.S. Gov't

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10.1039/c2ob26439k

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abstract = "Benzotriazole-mediated syntheses led to novel bis-conjugates of quinine with quinolone antibiotics and amino acid linkers which were successfully prepared by two alternative routes with excellent yields and retention of chirality. These bis conjugates retain in vitro antimalarial activity with IC(50) values ranging from 12 to 207 nM, similar to quinine itself.",

keywords = "Anti-Bacterial Agents, Antimalarials, Chemistry Techniques, Synthetic, Inhibitory Concentration 50, Peptide Fragments, Plasmodium falciparum, Quinine, Quinolones, Triazoles, Journal Article, Research Support, Non-U.S. Gov't",

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doi = "10.1039/c2ob26439k",

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AU - Panda, Siva S

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AB - Benzotriazole-mediated syntheses led to novel bis-conjugates of quinine with quinolone antibiotics and amino acid linkers which were successfully prepared by two alternative routes with excellent yields and retention of chirality. These bis conjugates retain in vitro antimalarial activity with IC(50) values ranging from 12 to 207 nM, similar to quinine itself.

KW - Anti-Bacterial Agents

KW - Antimalarials

KW - Chemistry Techniques, Synthetic

KW - Inhibitory Concentration 50

KW - Peptide Fragments

KW - Plasmodium falciparum

KW - Quinine

KW - Quinolones

KW - Triazoles

KW - Journal Article

KW - Research Support, Non-U.S. Gov't

U2 - 10.1039/c2ob26439k

DO - 10.1039/c2ob26439k

M3 - Article

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SN - 1477-0520

VL - 10

SP - 8985

EP - 8993

JO - Organic and Biomolecular Chemistry

JF - Organic and Biomolecular Chemistry

IS - 45

ER -

Quinine bis-conjugates with quinolone antibiotics and peptides: synthesis and antimalarial bioassay

Abstract

Keywords

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