SrasV1, Main, Exploration, bibRecord, 001D63

Antimycobacterial Activities of Novel 5-(1H-1,2,3-Triazolyl)Methyl Oxazolidinones

Identifieur interne : 001D63 ( Main/Exploration ); précédent : 001D62; suivant : 001D64

Antimycobacterial Activities of Novel 5-(1H-1,2,3-Triazolyl)Methyl Oxazolidinones

Auteurs : Oludotun Adebayo Phillips [Koweït] ; Edet Ekpenyong Udo [Koweït] ; Reny Varghese [Koweït]

Source :

Tuberculosis Research and Treatment [ 2090-150X ] ; 2012.

RBID : PMC:3345221

Abstract

The antibacterial activities of a series of triazolyl oxazolidinones against Mycobacterium tuberculosis strain in vitro and in vivo in a mice model are presented. Most active compounds were noncytotoxic against VERO cells with acceptable selectivity indexes (SI) as measures of compound tolerability. Structure activity relationships (SARs) revealed that analogs with alkylcarbonyl (IC₉₀: < 0.2 to 0.422 μg/mL) and arylcarbonyl (IC₉₀: < 0.2 to 2.103 μg/mL) groups at the piperazine 4N-position-displayed potent antimycobacterium activities, comparable to the methanesulfonyl (IC₉₀: < 0.2 μg/mL) analog, linezolid (IC₉₀: < 0.2 μg/mL), and isoniazid (IC₉₀: < 0.034 μg/mL). The furanylcarbonyl derivative also displayed potent activity, while the arylsulfonyl analogs were inactive. Of the triazolyl oxazolidinones, the morpholino (PH-27) derivative with medium bioavailability in plasma was most active in vivo, but relatively less efficacious than isoniazid.

Url:

http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3345221

DOI: 10.1155/2012/289136
PubMed: 22577542
PubMed Central: 3345221

Affiliations:

Koweït

Le document en format XML

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 and <italic>in vivo</italic>
 in a mice model are presented. Most active compounds were noncytotoxic against VERO cells with acceptable selectivity indexes (SI) as measures of compound tolerability. Structure activity relationships (SARs) revealed that analogs with alkylcarbonyl (IC<sub>90</sub>
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g/mL) and arylcarbonyl (IC<sub>90</sub>
: < 0.2 to 2.103 <italic><italic>μ</italic>
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g/mL) groups at the piperazine 4N-position-displayed potent antimycobacterium activities, comparable to the methanesulfonyl (IC<sub>90</sub>
: < 0.2 <italic><italic>μ</italic>
</italic>
g/mL) analog, linezolid (IC<sub>90</sub>
: < 0.2 <italic><italic>μ</italic>
</italic>
g/mL), and isoniazid (IC<sub>90</sub>
: < 0.034 <italic><italic>μ</italic>
</italic>
g/mL). The furanylcarbonyl derivative also displayed potent activity, while the arylsulfonyl analogs were inactive. Of the triazolyl oxazolidinones, the morpholino (PH-27) derivative with medium bioavailability in plasma was most active <italic>in vivo</italic>
, but relatively less efficacious than isoniazid.</p>
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Antimycobacterial Activities of Novel 5-(1H-1,2,3-Triazolyl)Methyl Oxazolidinones

Antimycobacterial Activities of Novel 5-(1H-1,2,3-Triazolyl)Methyl Oxazolidinones

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Abstract

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