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result sql = Synthesis, in vitro and in vivo antimycobacterial activities of diclofenac acid hydrazones and amides.
Synthesis, in vitro and in vivo antimycobacterial activities of diclofenac acid hydrazones and amides.
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char = <;code = 60
char = b;code = 98
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char = <;code = 60
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char = <;code = 60
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char = <;code = 60
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char = <;code = 60
char = b;code = 98
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char = C;code = 67
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char = ;code = 32
char = <;code = 60
char = /;code = 47
char = b;code = 98
char = >;code = 62
char = ;code = 32
char = <;code = 60
char = /;code = 47
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char = >;code = 62
char = ;code = 32
char = 0;code = 48
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char = 2;code = 50
char = 2;code = 50
char = ;code = 32
char = m;code = 109
char = i;code = 105
char = c;code = 99
char = r;code = 114
char = o;code = 111
char = M;code = 77
char = );code = 41
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char = ;code = 32
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char = ;code = 32
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char = ;code = 32
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char = ;code = 32
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char = e;code = 101
char = c;code = 99
char = t;code = 116
char = i;code = 105
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char = n;code = 110
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char = ;code = 32
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char = d;code = 100
char = y;code = 121
char = ;code = 32
char = w;code = 119
char = e;code = 101
char = i;code = 105
char = g;code = 103
char = h;code = 104
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result sql = Various diclofenac acid hydrazones and amides were synthesized and evaluated for in vitro and in vivo antimycobacterial activities against Mycobacterium tuberculosis. Preliminary results indicated that most of the compounds demonstrated better in vitro antimycobacterial activity (





MIC:
0.0383-7.53 microM) than diclofenac (





MIC:
21.10 microM) and ciprofloxacin (





MIC:
9.41 microM). Among the synthesized compounds, 1-cyclopropyl-6-fluoro-8-methoxy-7-[[N4-(2-(2-(2,6-dichlorophenylamino)phenyl)acetyl)-3-methyl]-N1-piperazinyl]-4-oxo-1,4-dihydro-3-quinoline carboxylic acid (5d) was found to be the most active compound in vitro with MIC of 0.0383 microM and was more potent than first line antitubercular drug isoniazid (





MIC:
0.1822 microM). In the in vivo animal model 5d decreased the bacterial load in lung and spleen tissues with 2.42- and 3.66-log10 protections, respectively, at 25 mg/kg body weight.

Publication: Bioorg. Med. Chem. 2006 May 1 ;14(9)::3113-8.
Publication Date: 2006 May 1
Study Author(s): Sriram, Dharmarajan;Yogeeswari, Perumal;Devakaram, Ruth Vandana;
Institution: Medicinal Chemistry Research Laboratory, Pharmacy group, Birla Institute of Technology and Science, Pilani 333031, India. [email protected]
Shortcut link to this study:
Various diclofenac acid hydrazones and amides were synthesized and evaluated for in vitro and in vivo antimycobacterial activities against Mycobacterium tuberculosis. Preliminary results indicated that most of the compounds demonstrated better in vitro antimycobacterial activity (





MIC:
0.0383-7.53 microM) than diclofenac (





MIC:
21.10 microM) and ciprofloxacin (





MIC:
9.41 microM). Among the synthesized compounds, 1-cyclopropyl-6-fluoro-8-methoxy-7-[[N4-(2-(2-(2,6-dichlorophenylamino)phenyl)acetyl)-3-methyl]-N1-piperazinyl]-4-oxo-1,4-dihydro-3-quinoline carboxylic acid (5d) was found to be the most active compound in vitro with MIC of 0.0383 microM and was more potent than first line antitubercular drug isoniazid (





MIC:
0.1822 microM). In the in vivo animal model 5d decreased the bacterial load in lung and spleen tissues with 2.42- and 3.66-log10 protections, respectively, at 25 mg/kg body weight.
PMID: 16412646

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