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

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8 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 languageEnglish
Pages (from-to)1271-1277
Number of pages7
JournalMedicinal Chemistry Research
Volume21
Issue number7
DOIs
Publication statusPublished - Jul 1 2012
Externally publishedYes

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Keywords

  • Antitussive
  • Azepinoquinazolone
  • Codeine
  • Cough

ASJC Scopus subject areas

  • Pharmacology, Toxicology and Pharmaceutics(all)
  • Organic Chemistry

Cite this

Nepali, K., Bande, M. S., Sapra, S., Garg, A., Kumar, S., Sharma, P., Goyal, R., Satti, N. K., Suri, O. P., & Dhar, K. L. (2012). Antitussive effects of azepino[2,1-b]quinazolones. Medicinal Chemistry Research, 21(7), 1271-1277. https://doi.org/10.1007/s00044-011-9641-1