Synthesis, characterisation & useful therapeutic activity of novel 2-quinolone derivatives

B. S. Jayashree, N. Sharma, S. Nigam

Research output: Contribution to journalArticle

Abstract

A series of novel 2-oxo-1,2,3,4-Tetrahydroquinolin-7-yl benzoate derivatives were synthesised and obtained in moderate yields (55-85%) by the reaction of parent 7-hydroxy-1,2,3,4-Tetrahydroquinolin- 2-one (7-hydroxy-3,4-dihydroquinolin-2(1H)-one) with substituted benzoyl chlorides. The synthesised test compounds were characterised by spectral analysis. Partition coefficient was determined for all test compounds and was found to be in the range of 1.2-2.9. Further, the compounds were screened for their antibacterial and antioxidant activities. They were also randomly screened for their antidiabetic potential by non-enzymatic glycosylation of haemoglobin assay. However, the results revealed that test compounds did not possess antioxidant and antidiabetic potential comparable to that of their respective standards. The results also revealed that most of the compounds exhibited antibacterial action against four bacterial strains namely Bacillus subtilis, Staphylococcus aureus, Pseudomonas aeruginosa and Escherichia coli. Further, the test compound VIIl (at 500 μg mL-1), showed zone of inhibition comparable to that of the standard ciprofloxacin (at 500 μg mL-1).

Original languageEnglish
Pages (from-to)41-46
Number of pages6
JournalIndian Drugs
Volume50
Issue number12
Publication statusPublished - 01-12-2013

Fingerprint

Hypoglycemic Agents
Antioxidants
Benzoates
Ciprofloxacin
Bacillus subtilis
Glycosylation
Pseudomonas aeruginosa
Staphylococcus aureus
Hemoglobins
Escherichia coli
Therapeutics
1,2,3,4-tetrahydroquinoline
carbostyril
dihydroquinolin-2(1H)-one
benzoyl chloride

All Science Journal Classification (ASJC) codes

  • Pharmacology
  • Pharmaceutical Science
  • Drug Discovery

Cite this

@article{94ec856479bd464cb8a05b69862dec50,
title = "Synthesis, characterisation & useful therapeutic activity of novel 2-quinolone derivatives",
abstract = "A series of novel 2-oxo-1,2,3,4-Tetrahydroquinolin-7-yl benzoate derivatives were synthesised and obtained in moderate yields (55-85{\%}) by the reaction of parent 7-hydroxy-1,2,3,4-Tetrahydroquinolin- 2-one (7-hydroxy-3,4-dihydroquinolin-2(1H)-one) with substituted benzoyl chlorides. The synthesised test compounds were characterised by spectral analysis. Partition coefficient was determined for all test compounds and was found to be in the range of 1.2-2.9. Further, the compounds were screened for their antibacterial and antioxidant activities. They were also randomly screened for their antidiabetic potential by non-enzymatic glycosylation of haemoglobin assay. However, the results revealed that test compounds did not possess antioxidant and antidiabetic potential comparable to that of their respective standards. The results also revealed that most of the compounds exhibited antibacterial action against four bacterial strains namely Bacillus subtilis, Staphylococcus aureus, Pseudomonas aeruginosa and Escherichia coli. Further, the test compound VIIl (at 500 μg mL-1), showed zone of inhibition comparable to that of the standard ciprofloxacin (at 500 μg mL-1).",
author = "Jayashree, {B. S.} and N. Sharma and S. Nigam",
note = "cited By 0",
year = "2013",
month = "12",
day = "1",
language = "English",
volume = "50",
pages = "41--46",
journal = "Indian Drugs",
issn = "0019-462X",
publisher = "Indian Drug Manufacturers' Association",
number = "12",

}

Synthesis, characterisation & useful therapeutic activity of novel 2-quinolone derivatives. / Jayashree, B. S.; Sharma, N.; Nigam, S.

In: Indian Drugs, Vol. 50, No. 12, 01.12.2013, p. 41-46.

Research output: Contribution to journalArticle

TY - JOUR

T1 - Synthesis, characterisation & useful therapeutic activity of novel 2-quinolone derivatives

AU - Jayashree, B. S.

AU - Sharma, N.

AU - Nigam, S.

N1 - cited By 0

PY - 2013/12/1

Y1 - 2013/12/1

N2 - A series of novel 2-oxo-1,2,3,4-Tetrahydroquinolin-7-yl benzoate derivatives were synthesised and obtained in moderate yields (55-85%) by the reaction of parent 7-hydroxy-1,2,3,4-Tetrahydroquinolin- 2-one (7-hydroxy-3,4-dihydroquinolin-2(1H)-one) with substituted benzoyl chlorides. The synthesised test compounds were characterised by spectral analysis. Partition coefficient was determined for all test compounds and was found to be in the range of 1.2-2.9. Further, the compounds were screened for their antibacterial and antioxidant activities. They were also randomly screened for their antidiabetic potential by non-enzymatic glycosylation of haemoglobin assay. However, the results revealed that test compounds did not possess antioxidant and antidiabetic potential comparable to that of their respective standards. The results also revealed that most of the compounds exhibited antibacterial action against four bacterial strains namely Bacillus subtilis, Staphylococcus aureus, Pseudomonas aeruginosa and Escherichia coli. Further, the test compound VIIl (at 500 μg mL-1), showed zone of inhibition comparable to that of the standard ciprofloxacin (at 500 μg mL-1).

AB - A series of novel 2-oxo-1,2,3,4-Tetrahydroquinolin-7-yl benzoate derivatives were synthesised and obtained in moderate yields (55-85%) by the reaction of parent 7-hydroxy-1,2,3,4-Tetrahydroquinolin- 2-one (7-hydroxy-3,4-dihydroquinolin-2(1H)-one) with substituted benzoyl chlorides. The synthesised test compounds were characterised by spectral analysis. Partition coefficient was determined for all test compounds and was found to be in the range of 1.2-2.9. Further, the compounds were screened for their antibacterial and antioxidant activities. They were also randomly screened for their antidiabetic potential by non-enzymatic glycosylation of haemoglobin assay. However, the results revealed that test compounds did not possess antioxidant and antidiabetic potential comparable to that of their respective standards. The results also revealed that most of the compounds exhibited antibacterial action against four bacterial strains namely Bacillus subtilis, Staphylococcus aureus, Pseudomonas aeruginosa and Escherichia coli. Further, the test compound VIIl (at 500 μg mL-1), showed zone of inhibition comparable to that of the standard ciprofloxacin (at 500 μg mL-1).

UR - http://www.scopus.com/inward/record.url?scp=85012188455&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=85012188455&partnerID=8YFLogxK

M3 - Article

VL - 50

SP - 41

EP - 46

JO - Indian Drugs

JF - Indian Drugs

SN - 0019-462X

IS - 12

ER -