2017
DOI: 10.1002/jhet.3024
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Design, Synthesis and In Vitro Anti‐mycobacterial Activities of 8‐OMe Ciprofloxacin‐1H‐1,2,3‐triazole‐isatin‐(thio) Semicarbazide/Oxime Hybrids

Abstract: A series of novel 8-OMe ciprofloxacin (8-OMe CPFX)-1H-1,2,3-triazole-isatin-(thio) semicarbazide/oxime hybrids 6a-l with the capacity to form hydrogen bond were designed, synthesized, and evaluated for their in vitro anti-mycobacterial activities against Mycobacterium tuberculosis (MTB) H 37 Rv and MDR-TB as well as cytotoxicity. All the synthesized hybrids (MIC: 0.39-16 μg/mL) exhibited excellent activities against MTB H 37 Rv and MDR-TB, and the majority of them were more potent than the parent 8-OMe CPFX (M… Show more

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Cited by 13 publications
(10 citation statements)
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“…Isatin and 5-fluoroisatin was alkylated with 1,2-dibromoethane in the presence of potassium carbonate to provide the corresponding N-(2-bromoethyl)isatin and N-(2bromoethyl)-5-fluoroisatin 2 (yield: 49% and 57%) by literature methods [17,18]. Isatin and 5-fluoroisatin was alkylated with 1,2-dibromoethane in the presence of potassium carbonate to provide the corresponding N-(2-bromoethyl)isatin and N-(2bromoethyl)-5-fluoroisatin 2 (yield: 49% and 57%) by literature methods [17,18].…”
Section: Resultsmentioning
confidence: 99%
See 1 more Smart Citation
“…Isatin and 5-fluoroisatin was alkylated with 1,2-dibromoethane in the presence of potassium carbonate to provide the corresponding N-(2-bromoethyl)isatin and N-(2bromoethyl)-5-fluoroisatin 2 (yield: 49% and 57%) by literature methods [17,18]. Isatin and 5-fluoroisatin was alkylated with 1,2-dibromoethane in the presence of potassium carbonate to provide the corresponding N-(2-bromoethyl)isatin and N-(2bromoethyl)-5-fluoroisatin 2 (yield: 49% and 57%) by literature methods [17,18].…”
Section: Resultsmentioning
confidence: 99%
“…N-(3-bromopropyl)isatins 2a,b were obtained according to the literature reported method [17,18]. A mixture of N-(3-bromopropyl)isatins 2a,b (5 mmol), 7-hydroxy-4-methyl-7-2H-chromen-2-one 4 (3 mmol), and K 2 CO 3 (20 mmol) was stirred at room temperature for 2 days.…”
Section: Synthesismentioning
confidence: 99%
“…The desired bis‐isatin derivatives 4a‐j were obtained by the synthetic route depicted in Scheme . Isatin was alkylated with 1,3‐dibromopropane with potassium carbonate as base in DMF at room temperature to provide the N ‐(2‐bromopropyl) isatin 2 (yield: 63%) by literature methods . 5‐Fluoroisatin was reacted with methoxyamine or ethoxyamine hydrochloride in the presence of potassium carbonate yielded 5‐fluoro‐3‐(methoxy/ethoxylimino) isatins 3a,b (yield: 78% and 69%) .…”
Section: Resultsmentioning
confidence: 99%
“…The precursors 4 and 6 were prepared via literature methods . A mixture of isatins 4 (1.0 mmol), coumarin 6 (1.0 mmol), and K 2 CO 3 (3.0 mmol) in DMF (20 mL) was stirred at room temperature overnight.…”
Section: Methodsmentioning
confidence: 99%