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Center of Excellence for Advanced Materials Research
Document Details
Document Type
:
Article In Journal
Document Title
:
Synthesis and biological evaluation of new 3- trifluoromethylpyrazolesulfonyl-urea and thiourea derivatives as antidiabetic and antimicrobial agents
Synthesis and biological evaluation of new 3- trifluoromethylpyrazolesulfonyl-urea and thiourea derivatives as antidiabetic and antimicrobial agents
Subject
:
Chemistry
Document Language
:
English
Abstract
:
Fluorinated pyrazoles, and benzenesulfonylurea and thiourea derivatives as well as their cyclic sulfonylthioureas 2-18 were prepared as hypoglycemic and antibacterial agents. The chemistry involves the condensation of 4-hydrazino benzenesulfonamide hydrochloride with 1-trifluoromethyl diketones 1 to give pyrazole derivatives 2 which upon bromination gave the bromopyrazole 3. Reaction of 2 or 3 with isocyanates and isothiocyanates gave the corresponding ureas 4 and 5 and thioureas 6 and 7. Cyclization of thiourea derivatives with ethyl bromoacetate, ethyl β-bromopropionate, 1,3-dichloroacetone and α-bromoacetophenone yielded the corresponding 4-oxothiazolidines 8 and 9, 4-oxo-5,6-dihydrothiazine 10, 5-oxo-4,5-dihydrothiazines 11 and 12 and thiazolines 13 and 14. Preliminary biological screening of the prepared compounds revealed significant antidiabetic and antibacterial activities.
ISSN
:
0022-1139
Journal Name
:
Journal of Fluorine Chemistry
Volume
:
132
Issue Number
:
2
Publishing Year
:
1432 AH
2011 AD
Article Type
:
Article
Added Date
:
Friday, February 17, 2012
Researchers
Researcher Name (Arabic)
Researcher Name (English)
Researcher Type
Dr Grade
Email
حسن مصطفى فيض الله
Faidallah, Hassan Mostafa
Researcher
Doctorate
hfaidallahm@hotmail.com
خالد خان
Khan, Khalid A
Researcher
Doctorate
عبدالله محمد عسيري
Asiri, Abdullah Mohamed
Researcher
Doctorate
aasiri2@kau.edu.sa
Files
File Name
Type
Description
32306.pdf
pdf
Abstract
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