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

Research output: Contribution to journalArticle

16 Citations (Scopus)

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 languageEnglish (US)
Pages (from-to)2314-20
Number of pages7
JournalBioorganic and Medicinal Chemistry Letters
Volume25
Issue number11
DOIs
StatePublished - Jun 1 2015

Fingerprint

Mesalamine
Quantitative Structure-Activity Relationship
Metronidazole
Stomach
Anti-Inflammatory Agents
Amino Acids
Pharmaceutical Preparations
benzotriazole

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

Cite this

Synthesis and QSAR study of novel anti-inflammatory active mesalazine-metronidazole conjugates. / Panda, Siva S.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 25, No. 11, 01.06.2015, p. 2314-20.

Research output: Contribution to journalArticle

@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}",
note = "Copyright {\circledC} 2015 Elsevier Ltd. All rights reserved.",
year = "2015",
month = "6",
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

N1 - Copyright © 2015 Elsevier Ltd. All rights reserved.

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

VL - 25

SP - 2314

EP - 2320

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

SN - 0960-894X

IS - 11

ER -