Antitussive effects of azepino[2,1-b]quinazolones

Kunal Nepali; Mukunda S. Bande; Sameer Sapra; Atul Garg; Sunil Kumar; Punita Sharma; Rohit Goyal; Naresh Kumar Satti; Om Parkash Suri; Kanaya Lal Dhar

doi:10.1007/s00044-011-9641-1

Antitussive effects of azepino[2,1-b]quinazolones

Kunal Nepali, Mukunda S. Bande, Sameer Sapra, Atul Garg, Sunil Kumar, Punita Sharma, Rohit Goyal, Naresh Kumar Satti, Om Parkash Suri, Kanaya Lal Dhar

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

10 Citations (Scopus)

Abstract

A series of azepino[2,1-b]quinazolones (C-1-C-16) have been synthesized and evaluated for their antitussive activity using citric acid-induced cough model in Guinea pigs. The compounds C-1-C-16 caused notable decrease in cough frequency and increase in cough latency induced by citric acid. C-3 [2,4-dibromo-7,8,9,10-tetrahydroazepino[2,1-b]quinazolin-12(6H)-one] showed notable antitussive effect as compared with codeine (10 mg/kg). Various substitutions were made at Rings A and B, and all substituents like methoxy, hydroxyl, nitro, amino (Ring A) and alkyl, acetyl, benzoyl (Ring B) other than bromine were found to reduce the potential of the unsubstituted 7,8,9,10-tetrahydroazepino[2,1-b]quinazolin-12(6H)-one as antitussive.

Original language	English
Pages (from-to)	1271-1277
Number of pages	7
Journal	Medicinal Chemistry Research
Volume	21
Issue number	7
DOIs	https://doi.org/10.1007/s00044-011-9641-1
Publication status	Published - Jul 1 2012
Externally published	Yes

Keywords

Antitussive
Azepinoquinazolone
Codeine
Cough

ASJC Scopus subject areas

Pharmacology, Toxicology and Pharmaceutics(all)
Organic Chemistry

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10.1007/s00044-011-9641-1

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title = "Antitussive effects of azepino[2,1-b]quinazolones",

abstract = "A series of azepino[2,1-b]quinazolones (C-1-C-16) have been synthesized and evaluated for their antitussive activity using citric acid-induced cough model in Guinea pigs. The compounds C-1-C-16 caused notable decrease in cough frequency and increase in cough latency induced by citric acid. C-3 [2,4-dibromo-7,8,9,10-tetrahydroazepino[2,1-b]quinazolin-12(6H)-one] showed notable antitussive effect as compared with codeine (10 mg/kg). Various substitutions were made at Rings A and B, and all substituents like methoxy, hydroxyl, nitro, amino (Ring A) and alkyl, acetyl, benzoyl (Ring B) other than bromine were found to reduce the potential of the unsubstituted 7,8,9,10-tetrahydroazepino[2,1-b]quinazolin-12(6H)-one as antitussive.",

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author = "Kunal Nepali and Bande, {Mukunda S.} and Sameer Sapra and Atul Garg and Sunil Kumar and Punita Sharma and Rohit Goyal and Satti, {Naresh Kumar} and Suri, {Om Parkash} and Dhar, {Kanaya Lal}",

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AU - Nepali, Kunal

AU - Bande, Mukunda S.

AU - Sapra, Sameer

AU - Garg, Atul

AU - Kumar, Sunil

AU - Sharma, Punita

AU - Goyal, Rohit

AU - Satti, Naresh Kumar

AU - Suri, Om Parkash

AU - Dhar, Kanaya Lal

PY - 2012/7/1

Y1 - 2012/7/1

N2 - A series of azepino[2,1-b]quinazolones (C-1-C-16) have been synthesized and evaluated for their antitussive activity using citric acid-induced cough model in Guinea pigs. The compounds C-1-C-16 caused notable decrease in cough frequency and increase in cough latency induced by citric acid. C-3 [2,4-dibromo-7,8,9,10-tetrahydroazepino[2,1-b]quinazolin-12(6H)-one] showed notable antitussive effect as compared with codeine (10 mg/kg). Various substitutions were made at Rings A and B, and all substituents like methoxy, hydroxyl, nitro, amino (Ring A) and alkyl, acetyl, benzoyl (Ring B) other than bromine were found to reduce the potential of the unsubstituted 7,8,9,10-tetrahydroazepino[2,1-b]quinazolin-12(6H)-one as antitussive.

AB - A series of azepino[2,1-b]quinazolones (C-1-C-16) have been synthesized and evaluated for their antitussive activity using citric acid-induced cough model in Guinea pigs. The compounds C-1-C-16 caused notable decrease in cough frequency and increase in cough latency induced by citric acid. C-3 [2,4-dibromo-7,8,9,10-tetrahydroazepino[2,1-b]quinazolin-12(6H)-one] showed notable antitussive effect as compared with codeine (10 mg/kg). Various substitutions were made at Rings A and B, and all substituents like methoxy, hydroxyl, nitro, amino (Ring A) and alkyl, acetyl, benzoyl (Ring B) other than bromine were found to reduce the potential of the unsubstituted 7,8,9,10-tetrahydroazepino[2,1-b]quinazolin-12(6H)-one as antitussive.

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Antitussive effects of azepino[2,1-b]quinazolones

Abstract

Keywords

ASJC Scopus subject areas

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