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   Synthesis,characterization and antimicrobial evaluation of some thiazole-derived carbamates,semicarbazones,amides and carboxamide  
   
نویسنده el-sayed n.n.e. ,al-balawi n.a. ,alafeefy a.m. ,al-alshaikh m.a. ,khan k.m.
منبع journal of the chemical society of pakistan - 2016 - دوره : 38 - شماره : 2 - صفحه:358 -368
چکیده    This study comprises the synthesis and characterization of twenty thiazole-derived carbamates (3a-e),n-substituted amides (8a-h) and carboxamide (10) from 2-aminothiazoles (1a,b) via nucleophilic substitution reactions with activated carbonyl compounds including,chloroformates (2a-d),acid chlorides (7a-e) and glutaric anhydride (9),respectively. sequential hydrazinolysis of carbamate (3e) and condensation with a variety of aldehydes and ketones (5a-d) afforded the corresponding semicarbazones (6a-d). some selected synthesized compounds were subjected to in vitro antimicrobial evaluation against common pathogens including,gram+ve bacteria bacillus subtilis (nrrl b-543) and staphylococcus aureus,gram-ve bacteria escherichia coli (nrrlb-21),yeasts-candida albicans (nrrly-477) and saccharomyces cercvisiae (nrrl y-567) and fungs asperigillus niger (nrrl 599). screening results revealed that most of the tested compounds possess good antimicrobial activity compared to standard drugs. the highest inhibitory effects against gram-ve escherichia coli,gram+ve staphylococcus aureus,yeast candida albicans and fungus aspergillus niger was displayed by amide (8g) bearing the thiophene moiety. © 2016,chemical society of pakistan. all rights reserved.
کلیدواژه 2-Aminothiazole; Acylation of 2-aminothiazole; Antimicrobial activity; Drug development; Multidrug resistance
آدرس department of chemistry,college of science,king saud university,girls section,p.o. box 22452,riyadh,saudi arabia,national organization for drug control and research,agouza,giza, Egypt, department of chemistry,college of science,king saud university,girls section,p.o. box 22452,riyadh, Saudi Arabia, department of chemistry,kulliyyah of science international islamic university,p.o. box 141,kuantan, Malaysia, department of chemistry,college of science,king saud university,girls section,p.o. box 22452,riyadh, Saudi Arabia, h. e. j. research institute of chemistry,international center for chemical and biological sciences,university karachi,karachi, Pakistan
 
     
   
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