微波辅助一锅法合成高效新型异烟肼类似物。
Microwave assisted one-pot synthesis of highly potent novel isoniazid analogues.
机构信息
Medicinal Chemistry and Antimycobacterial Research Laboratory, Department of Pharmacy, Birla Institute of Technology and Science, Pilani, Hyderabad Campus, Jawahar Nagar, Hyderabad 500 078, India.
出版信息
Bioorg Med Chem Lett. 2011 Apr 1;21(7):2125-8. doi: 10.1016/j.bmcl.2011.01.122. Epub 2011 Feb 2.
A series of novel isoniazid (INH) analogues were synthesized by microwave assisted one pot reaction of INH, various benzaldehydes and dimedone in water with catalytic amount of DBSA. The synthesized compounds were evaluated for their anti-TB activity against Mycobacterium tuberculosis H37Rv (MTB) and multi-drug resistant Mycobacterium tuberculosis (MDR-TB). Among the 29 compounds, compound N-[9-[2-(benzyloxy)phenyl]-3,3,6,6-tetramethyl-1,8-dioxo-2,3,4,5,6,7,8,9-octahydro-10(1H)-acridinyl]isonicotinamide (12) inhibited MTB with MIC of <0.17 μM and MDR-TB with MIC of 0.69 μM.
一系列新型异烟肼（INH）类似物通过 INH、各种苯甲醛和二甲基乙内酰脲在水中与催化量的 DBSA 的微波辅助一锅反应合成。合成的化合物被评估了它们对结核分枝杆菌 H37Rv（MTB）和耐多药结核分枝杆菌（MDR-TB）的抗结核活性。在 29 种化合物中，化合物 N-[9-[2-（苯氧基）苯基]-3,3,6,6-四甲基-1,8-二氧代-2,3,4,5,6,7,8,9-八氢-10(1H)-吖啶基]异烟酰胺（12）对 MTB 的 MIC 值<0.17 μM，对 MDR-TB 的 MIC 值为 0.69 μM。
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