Synthesis and QSAR study of novel anti-inflammatory active mesalazine-metronidazole conjugates

Siva S Panda

doi:10.1016/j.bmcl.2015.04.023

Synthesis and QSAR study of novel anti-inflammatory active mesalazine-metronidazole conjugates

Siva S Panda

Chemistry and Biochemistry

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

27 Scopus citations

Abstract

Novel, mesalazine, metronidazole conjugates 6a-e with amino acid linkers were synthesized utilizing benzotriazole chemistry. Biological data acquired for all the novel bis-conjugates showed (a) some bis-conjugates exhibit comparable anti-inflammatory activity with parent drugs and (b) the potent bis-conjugates show no visible stomach lesions. 3D-pharmacophore and 2D-QSAR modeling support the observed bio-properties.

Original language	English (US)
Pages (from-to)	2314-20
Number of pages	7
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	25
Issue number	11
DOIs	https://doi.org/10.1016/j.bmcl.2015.04.023
State	Published - Jun 1 2015

Keywords

Animals
Anti-Inflammatory Agents
Indomethacin
Mesalamine
Metronidazole
Mice
Molecular Structure
Quantitative Structure-Activity Relationship
Stomach Ulcer
Journal Article
Research Support, Non-U.S. Gov't

Access to Document

10.1016/j.bmcl.2015.04.023

Cite this

@article{90842f38d91f4c03aab644d3f93e9936,

title = "Synthesis and QSAR study of novel anti-inflammatory active mesalazine-metronidazole conjugates",

abstract = "Novel, mesalazine, metronidazole conjugates 6a-e with amino acid linkers were synthesized utilizing benzotriazole chemistry. Biological data acquired for all the novel bis-conjugates showed (a) some bis-conjugates exhibit comparable anti-inflammatory activity with parent drugs and (b) the potent bis-conjugates show no visible stomach lesions. 3D-pharmacophore and 2D-QSAR modeling support the observed bio-properties.",

keywords = "Animals, Anti-Inflammatory Agents, Indomethacin, Mesalamine, Metronidazole, Mice, Molecular Structure, Quantitative Structure-Activity Relationship, Stomach Ulcer, Journal Article, Research Support, Non-U.S. Gov't",

author = "Panda, {Siva S}",

year = "2015",

month = jun,

day = "1",

doi = "10.1016/j.bmcl.2015.04.023",

language = "English (US)",

volume = "25",

pages = "2314--20",

journal = "Bioorganic and Medicinal Chemistry Letters",

issn = "0960-894X",

publisher = "Elsevier Limited",

number = "11",

}

TY - JOUR

T1 - Synthesis and QSAR study of novel anti-inflammatory active mesalazine-metronidazole conjugates

AU - Panda, Siva S

PY - 2015/6/1

Y1 - 2015/6/1

N2 - Novel, mesalazine, metronidazole conjugates 6a-e with amino acid linkers were synthesized utilizing benzotriazole chemistry. Biological data acquired for all the novel bis-conjugates showed (a) some bis-conjugates exhibit comparable anti-inflammatory activity with parent drugs and (b) the potent bis-conjugates show no visible stomach lesions. 3D-pharmacophore and 2D-QSAR modeling support the observed bio-properties.

AB - Novel, mesalazine, metronidazole conjugates 6a-e with amino acid linkers were synthesized utilizing benzotriazole chemistry. Biological data acquired for all the novel bis-conjugates showed (a) some bis-conjugates exhibit comparable anti-inflammatory activity with parent drugs and (b) the potent bis-conjugates show no visible stomach lesions. 3D-pharmacophore and 2D-QSAR modeling support the observed bio-properties.

KW - Animals

KW - Anti-Inflammatory Agents

KW - Indomethacin

KW - Mesalamine

KW - Metronidazole

KW - Mice

KW - Molecular Structure

KW - Quantitative Structure-Activity Relationship

KW - Stomach Ulcer

KW - Journal Article

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

U2 - 10.1016/j.bmcl.2015.04.023

DO - 10.1016/j.bmcl.2015.04.023

M3 - Article

C2 - 25937011

SN - 0960-894X

VL - 25

SP - 2314

EP - 2320

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 11

ER -

Synthesis and QSAR study of novel anti-inflammatory active mesalazine-metronidazole conjugates

Abstract

Keywords

Access to Document

Fingerprint

Cite this