Antihistaminic and other biological activities of 2-methylpropanamide and benzamide derivatives of carboxyterfenadine
In the present study the 2-methylpropanamide and benzamide derivatives of carboxyterfenadine, have been synthesized by nucleophilic substitution at carboxylic acid moiety (C-33) of tertiary carbon C-19 substituted with benzene ring. The proficient and high yielding series was carried out in two step...
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| Format: | Article |
| Language: | English |
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Elsevier
2017-01-01
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| Series: | Arabian Journal of Chemistry |
| Subjects: | |
| Online Access: | http://www.sciencedirect.com/science/article/pii/S1878535215000222 |
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| author | M. Saeed Arayne Najma Sultana Hina Shehnaz Saf-ur-Rehman Mandukhail Anwarul Hassan Gilani Amir Haider |
| author_facet | M. Saeed Arayne Najma Sultana Hina Shehnaz Saf-ur-Rehman Mandukhail Anwarul Hassan Gilani Amir Haider |
| author_sort | M. Saeed Arayne |
| collection | DOAJ |
| description | In the present study the 2-methylpropanamide and benzamide derivatives of carboxyterfenadine, have been synthesized by nucleophilic substitution at carboxylic acid moiety (C-33) of tertiary carbon C-19 substituted with benzene ring. The proficient and high yielding series was carried out in two steps by continuous monitoring with TLC. The carboxylic group was utilized in the formation of 2-methylpropanamide and benzamide derivatives of carboxyterfenadine. The derivatives were characterized by spectroscopic techniques including mass. The starting material (2-[4-[1-hydroxy-4-[4-(hydroxydiphenylmethyl)piperidino]butyl]phenyl]-2-methylpropanoic acid) itself is H1 receptor antagonist. Hence, all these compounds A–E were biologically evaluated for antihistaminic and anticholinergic activity, using isolated guinea pig ileum tissues. |
| first_indexed | 2024-12-23T20:18:52Z |
| format | Article |
| id | doaj.art-be1dd39d066440ef9b5318f853bdc86a |
| institution | Directory Open Access Journal |
| issn | 1878-5352 |
| language | English |
| last_indexed | 2024-12-23T20:18:52Z |
| publishDate | 2017-01-01 |
| publisher | Elsevier |
| record_format | Article |
| series | Arabian Journal of Chemistry |
| spelling | doaj.art-be1dd39d066440ef9b5318f853bdc86a2022-12-21T17:32:37ZengElsevierArabian Journal of Chemistry1878-53522017-01-0110111412010.1016/j.arabjc.2015.01.004Antihistaminic and other biological activities of 2-methylpropanamide and benzamide derivatives of carboxyterfenadineM. Saeed Arayne0Najma Sultana1Hina Shehnaz2Saf-ur-Rehman Mandukhail3Anwarul Hassan Gilani4Amir Haider5Department of Chemistry, University of Karachi, Karachi 75270, PakistanResearch Institute of Pharmaceutical Sciences, Faculty of Pharmacy, University of Karachi, Karachi 75270, PakistanDepartment of Environmental Studies, Sind Madressatul Islam University, Karachi 74000, PakistanNatural Product Research Division, Department of Biological and Biomedical Sciences, Aga Khan University Medical College, Karachi 74800, PakistanNatural Product Research Division, Department of Biological and Biomedical Sciences, Aga Khan University Medical College, Karachi 74800, PakistanDepartment of Chemistry, University of Karachi, Karachi 75270, PakistanIn the present study the 2-methylpropanamide and benzamide derivatives of carboxyterfenadine, have been synthesized by nucleophilic substitution at carboxylic acid moiety (C-33) of tertiary carbon C-19 substituted with benzene ring. The proficient and high yielding series was carried out in two steps by continuous monitoring with TLC. The carboxylic group was utilized in the formation of 2-methylpropanamide and benzamide derivatives of carboxyterfenadine. The derivatives were characterized by spectroscopic techniques including mass. The starting material (2-[4-[1-hydroxy-4-[4-(hydroxydiphenylmethyl)piperidino]butyl]phenyl]-2-methylpropanoic acid) itself is H1 receptor antagonist. Hence, all these compounds A–E were biologically evaluated for antihistaminic and anticholinergic activity, using isolated guinea pig ileum tissues.http://www.sciencedirect.com/science/article/pii/S1878535215000222FexofenadineAnticholinergic activityCarboxyterfenadine |
| spellingShingle | M. Saeed Arayne Najma Sultana Hina Shehnaz Saf-ur-Rehman Mandukhail Anwarul Hassan Gilani Amir Haider Antihistaminic and other biological activities of 2-methylpropanamide and benzamide derivatives of carboxyterfenadine Arabian Journal of Chemistry Fexofenadine Anticholinergic activity Carboxyterfenadine |
| title | Antihistaminic and other biological activities of 2-methylpropanamide and benzamide derivatives of carboxyterfenadine |
| title_full | Antihistaminic and other biological activities of 2-methylpropanamide and benzamide derivatives of carboxyterfenadine |
| title_fullStr | Antihistaminic and other biological activities of 2-methylpropanamide and benzamide derivatives of carboxyterfenadine |
| title_full_unstemmed | Antihistaminic and other biological activities of 2-methylpropanamide and benzamide derivatives of carboxyterfenadine |
| title_short | Antihistaminic and other biological activities of 2-methylpropanamide and benzamide derivatives of carboxyterfenadine |
| title_sort | antihistaminic and other biological activities of 2 methylpropanamide and benzamide derivatives of carboxyterfenadine |
| topic | Fexofenadine Anticholinergic activity Carboxyterfenadine |
| url | http://www.sciencedirect.com/science/article/pii/S1878535215000222 |
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