کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1361587 | 981467 | 2007 | 7 صفحه PDF | دانلود رایگان |

4-(5-Substituted-1,3,4-oxadiazol-2-yl)pyridine derivatives 1–12 were synthesized and evaluated for their in vitro antimycobacterial activity. Some compounds showed an interesting activity against Mycobacterium tuberculosis H37Rv and five clinical isolates (drug-sensitive and -resistant strains). Compound 4 [4-(5-pentadecyl-1,3,4-oxadiazol-2-yl)pyridine] was 10 times more active than isoniazid, 20 times more active than streptomycin, and 28 times more potent than ethambutol against drug-resistant strain CIBIN 112. Compound 5 [4-(5-heptadecyl-1,3,4-oxadiazol-2-yl)pyridine] showed the same behavior as compound 4. Both of the above structures bear a high lipophilic chain bonded to the 5-position of the oxadiazole moiety. This fact implies that there exists a contribution of lipophilicity, which could facilitate the entrance of these molecules through lipid-enriched bacterial cell membrane.
4-(5-Substituted-1,3,4-oxadiazol-2-yl)pyridine derivatives 1–12 were synthesized and evaluated for their in vitro antimycobacterial activity. Some compounds showed an interesting activity against strain of Mycobacterium tuberculosis H37Rv and five clinical isolates (drug-sensitive and -resistant strains). Compound 4 was 10, 20, and 28 times more active than isoniazid, streptomycin, and ethambutol against multidrug-resistant strain CIBIN 112. Compound 5 showed the same behavior as compound 4. Both structures bear a high lipophilic chain bonded to the 5-position of oxadiazole moiety.Figure optionsDownload as PowerPoint slide
Journal: Bioorganic & Medicinal Chemistry - Volume 15, Issue 16, 15 August 2007, Pages 5502–5508