Synthesis, Antimicrobial Evaluation and Hemolytic Activity of 2-[[5-alkyl/aralkyl substituted-1,3,4-oxadiazol-2-yl]thio]-N-[4-(4-morpholinyl)phenyl]acetamide derivatives

2,5-Disubstituted 1,3,4-oxadiazole compounds are one of the most attractive classes for researchers due to their pharmacological activities. In the current research, a new series of 2-[[5-alkyl/aralkyl-1,3,4-oxadiazol-2-yl]thio]-N-[4-(4-morpholinyl)phenyl]acetamides (6a–m) were prepared by convertin...

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Main Authors:	Akhtar, Muhammad Nadeem, Gul, Samreen, Rehman, Aziz-ur, Abbasi, M. Athar, Khan, Khalid Mohammed, Nafeesa, Khadija, Siddiqa, Asia, Shahid, Muhammad, Subhani, Zinayyera
Format:	Article
Language:	English
Published:	Elsevier 2017
Subjects:	QD Chemistry
Online Access:	http://umpir.ump.edu.my/id/eprint/7986/ http://umpir.ump.edu.my/id/eprint/7986/ http://umpir.ump.edu.my/id/eprint/7986/ http://umpir.ump.edu.my/id/eprint/7986/1/fist-2017-nadeem-Synthesis%2C%20antimicrobial%20evaluation%20and%20hemolytic.pdf

id	ump-7986
recordtype	eprints
spelling	ump-79862018-04-18T04:10:58Z http://umpir.ump.edu.my/id/eprint/7986/ Synthesis, Antimicrobial Evaluation and Hemolytic Activity of 2-[[5-alkyl/aralkyl substituted-1,3,4-oxadiazol-2-yl]thio]-N-[4-(4-morpholinyl)phenyl]acetamide derivatives Akhtar, Muhammad Nadeem Gul, Samreen Rehman, Aziz-ur Abbasi, M. Athar Khan, Khalid Mohammed Nafeesa, Khadija Siddiqa, Asia Shahid, Muhammad Subhani, Zinayyera QD Chemistry 2,5-Disubstituted 1,3,4-oxadiazole compounds are one of the most attractive classes for researchers due to their pharmacological activities. In the current research, a new series of 2-[[5-alkyl/aralkyl-1,3,4-oxadiazol-2-yl]thio]-N-[4-(4-morpholinyl)phenyl]acetamides (6a–m) were prepared by converting different aryl/aralkyl organic acids (1a–m) successively into corresponding esters (2a–m), hydrazides (3a–m) and 5-aryl/aralkyl-1,3,4-oxadiazol-2-thiols (4a–m). Finally, the target compounds 6a–m were synthesized by stirring 5-aryl/aralkyl-1,3,4-oxadiazol-2-thiols (4a–m) with 2-bromo-N-[4-(4-morpholinyl)phenyl]acetamide (5) in the presence of N,N-dimethylformamide (DMF) and sodium hydride (NaH). The structures of the synthesized compounds were elucidated through IR, 1H-NMR, 13C-NMR and mass spectral data. The compounds were also screened for antimicrobial and hemolytic activity and most of them were found to be active against the selected microbial species at variable extent relative to reference standards. The compounds, 6d and 6f were active against the selected panel of microbes and the former was the most potent one. This series showed less toxicity and may be considered for further biological screening and application trial except 6h and 6l, possessing higher cytotoxicity. Elsevier 2017 Article PeerReviewed application/pdf en cc_by_nc_nd http://umpir.ump.edu.my/id/eprint/7986/1/fist-2017-nadeem-Synthesis%2C%20antimicrobial%20evaluation%20and%20hemolytic.pdf Akhtar, Muhammad Nadeem and Gul, Samreen and Rehman, Aziz-ur and Abbasi, M. Athar and Khan, Khalid Mohammed and Nafeesa, Khadija and Siddiqa, Asia and Shahid, Muhammad and Subhani, Zinayyera (2017) Synthesis, Antimicrobial Evaluation and Hemolytic Activity of 2-[[5-alkyl/aralkyl substituted-1,3,4-oxadiazol-2-yl]thio]-N-[4-(4-morpholinyl)phenyl]acetamide derivatives. Journal of Saudi Chemical Society, 21 (Suppl. 1). pp. 425-433. ISSN 1319-6103 https://doi.org/10.1016/j.jscs.2014.04.005 DOI: 10.1016/j.jscs.2014.04.005
repository_type	Digital Repository
institution_category	Local University
institution	Universiti Malaysia Pahang
building	UMP Institutional Repository
collection	Online Access
language	English
topic	QD Chemistry
spellingShingle	QD Chemistry Akhtar, Muhammad Nadeem Gul, Samreen Rehman, Aziz-ur Abbasi, M. Athar Khan, Khalid Mohammed Nafeesa, Khadija Siddiqa, Asia Shahid, Muhammad Subhani, Zinayyera Synthesis, Antimicrobial Evaluation and Hemolytic Activity of 2-[[5-alkyl/aralkyl substituted-1,3,4-oxadiazol-2-yl]thio]-N-[4-(4-morpholinyl)phenyl]acetamide derivatives
description	2,5-Disubstituted 1,3,4-oxadiazole compounds are one of the most attractive classes for researchers due to their pharmacological activities. In the current research, a new series of 2-[[5-alkyl/aralkyl-1,3,4-oxadiazol-2-yl]thio]-N-[4-(4-morpholinyl)phenyl]acetamides (6a–m) were prepared by converting different aryl/aralkyl organic acids (1a–m) successively into corresponding esters (2a–m), hydrazides (3a–m) and 5-aryl/aralkyl-1,3,4-oxadiazol-2-thiols (4a–m). Finally, the target compounds 6a–m were synthesized by stirring 5-aryl/aralkyl-1,3,4-oxadiazol-2-thiols (4a–m) with 2-bromo-N-[4-(4-morpholinyl)phenyl]acetamide (5) in the presence of N,N-dimethylformamide (DMF) and sodium hydride (NaH). The structures of the synthesized compounds were elucidated through IR, 1H-NMR, 13C-NMR and mass spectral data. The compounds were also screened for antimicrobial and hemolytic activity and most of them were found to be active against the selected microbial species at variable extent relative to reference standards. The compounds, 6d and 6f were active against the selected panel of microbes and the former was the most potent one. This series showed less toxicity and may be considered for further biological screening and application trial except 6h and 6l, possessing higher cytotoxicity.
format	Article
author	Akhtar, Muhammad Nadeem Gul, Samreen Rehman, Aziz-ur Abbasi, M. Athar Khan, Khalid Mohammed Nafeesa, Khadija Siddiqa, Asia Shahid, Muhammad Subhani, Zinayyera
author_facet	Akhtar, Muhammad Nadeem Gul, Samreen Rehman, Aziz-ur Abbasi, M. Athar Khan, Khalid Mohammed Nafeesa, Khadija Siddiqa, Asia Shahid, Muhammad Subhani, Zinayyera
author_sort	Akhtar, Muhammad Nadeem
title	Synthesis, Antimicrobial Evaluation and Hemolytic Activity of 2-[[5-alkyl/aralkyl substituted-1,3,4-oxadiazol-2-yl]thio]-N-[4-(4-morpholinyl)phenyl]acetamide derivatives
title_short	Synthesis, Antimicrobial Evaluation and Hemolytic Activity of 2-[[5-alkyl/aralkyl substituted-1,3,4-oxadiazol-2-yl]thio]-N-[4-(4-morpholinyl)phenyl]acetamide derivatives
title_full	Synthesis, Antimicrobial Evaluation and Hemolytic Activity of 2-[[5-alkyl/aralkyl substituted-1,3,4-oxadiazol-2-yl]thio]-N-[4-(4-morpholinyl)phenyl]acetamide derivatives
title_fullStr	Synthesis, Antimicrobial Evaluation and Hemolytic Activity of 2-[[5-alkyl/aralkyl substituted-1,3,4-oxadiazol-2-yl]thio]-N-[4-(4-morpholinyl)phenyl]acetamide derivatives
title_full_unstemmed	Synthesis, Antimicrobial Evaluation and Hemolytic Activity of 2-[[5-alkyl/aralkyl substituted-1,3,4-oxadiazol-2-yl]thio]-N-[4-(4-morpholinyl)phenyl]acetamide derivatives
title_sort	synthesis, antimicrobial evaluation and hemolytic activity of 2-[[5-alkyl/aralkyl substituted-1,3,4-oxadiazol-2-yl]thio]-n-[4-(4-morpholinyl)phenyl]acetamide derivatives
publisher	Elsevier
publishDate	2017
url	http://umpir.ump.edu.my/id/eprint/7986/ http://umpir.ump.edu.my/id/eprint/7986/ http://umpir.ump.edu.my/id/eprint/7986/ http://umpir.ump.edu.my/id/eprint/7986/1/fist-2017-nadeem-Synthesis%2C%20antimicrobial%20evaluation%20and%20hemolytic.pdf
first_indexed	2023-09-18T22:05:12Z
last_indexed	2023-09-18T22:05:12Z
_version_	1777414661678825472

Synthesis, Antimicrobial Evaluation and Hemolytic Activity of 2-[[5-alkyl/aralkyl substituted-1,3,4-oxadiazol-2-yl]thio]-N-[4-(4-morpholinyl)phenyl]acetamide derivatives

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