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Synthesis of novel fluorene bisamide derivatives via ugi reaction and evaluation their biological activity against Mycobacterium species
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نویسنده
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rezayan a.h. ,hariri s. ,azerang p. ,ghavami g. ,portugal i. ,sardari s.
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منبع
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iranian journal of pharmaceutical research - 2017 - دوره : 16 - شماره : 2 - صفحه:724 -752
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چکیده
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A series of new fluorene bisamide derivatives were synthesized through multi-component ugi reaction and tested for their in-vitro anti-mycobacterial activity. the structures of the products 5a-w were deduced from their ir,1h nmr,and 13c nmr spectra. elemental analyses (chn) for novel compounds (5a,5d,5f,5h,5k,5l,5p,5s,5t,5v,5w) was done. these compounds were evaluated as anti-bacterial agents against mycobacterium bovis and m. tuberculosis,while their activity expressed as the minimum inhibitory concentration (mic) in μg/ml. among the twenty-three synthesized compounds,5a was found to be the most active compound in vitro with mic of 1.95 μg/ml against mycobactrium bovis and compound 5k showed greatest potency against sensitive and resistant strains of m. tuberculosis (h37rv,ihmt149/09,hpv115/08,and hpv65/08). © 2017 by school of pharmacy.
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کلیدواژه
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Brine shrimp toxicity study; Fluorene bisamide derivatives; Multi-component reaction; Mycobacterium bovis; Ugi reaction
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آدرس
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department of life science engineering,faculty of new sciences and technologies,university of tehran,tehran, ایران, drug design and bioinformatics unit,department of medical biotechnology,biotechnology research center,pasteur institute of iran,tehran, ایران, drug design and bioinformatics unit,department of medical biotechnology,biotechnology research center,pasteur institute of iran,tehran, ایران, drug design and bioinformatics unit,department of medical biotechnology,biotechnology research center,pasteur institute of iran,tehran, ایران, imed.ulisboa,instituto de investigação do medicamento,faculdade de farmácia da universidade de lisboa,av. das forcas armadas,lisboa, Portugal, drug design and bioinformatics unit,department of medical biotechnology,biotechnology research center,pasteur institute of iran,tehran, ایران
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Authors
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