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Sun LQ Qin B Huang L Qian K Chen CH Lee KH Xie L 《Bioorganic & medicinal chemistry letters》2012,22(7):2376-2379
The current optimization of 2,4-diarylaniline analogs (DAANs) on the central phenyl ring provided a series of new active DAAN derivatives 9a-9e, indicating an accessible modification approach that could improve anti-HIV potency against wild-type and resistant strains, aqueous solubility, and metabolic stability. A new compound 9e not only exhibited extremely high potency against wild-type virus (EC(50) 0.53 nM) and several resistant viral strains (EC(50) 0.36-3.9 nM), but also showed desirable aqueous solubility and metabolic stability, which were comparable or better than those of the anti-HIV-1 drug TMC278 (2). Thus, new compound 9e might be a potential drug candidate for further development of novel next-generation NNRTIs. 相似文献
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Xingtao Tian Bingjie Qin Hong Lu Weihong Lai Shibo Jiang Kuo-Hsiung Lee Chin Ho Chen Lan Xie 《Bioorganic & medicinal chemistry letters》2009,19(18):5482-5485
Two series (4 and 5) of diarylpyridine derivatives were designed, synthesized, and evaluated for anti-HIV-1 activity. The most promising compound, 5e, inhibited HIV-1 IIIB, NL4-3, and RTMDR1 with low nanomolar EC50 values and selectivity indexes of >10,000. The results of this study indicate that diarylpyridine can be used as a novel scaffold to derive a new class of potent NNRTIs, active against both wild-type and drug-resistant HIV-1 strains. 相似文献
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De La Rosa M Kim HW Gunic E Jenket C Boyle U Koh YH Korboukh I Allan M Zhang W Chen H Xu W Nilar S Yao N Hamatake R Lang SA Hong Z Zhang Z Girardet JL 《Bioorganic & medicinal chemistry letters》2006,16(17):4444-4449
A new series of 1,2,4-triazoles was synthesized and tested against several NNRTI-resistant HIV-1 isolates. Several of these compounds exhibited potent antiviral activities against efavirenz- and nevirapine-resistant viruses, containing K103N and/or Y181C mutations or Y188L mutation. Triazoles were first synthesized from commercially available substituted phenylthiosemicarbazides, then from isothiocyanates, and later by condensing the desired substituted anilines with thiosemicarbazones. 相似文献
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