共查询到20条相似文献,搜索用时 15 毫秒
1.
2.
3.
4.
5.
6.
Esra Tatar İlkay Küçükgüzel Dirk Daelemans Tanaji T. Talele Neerja Kaushik‐Basu Erik De Clercq Christophe Pannecouque 《Archiv der Pharmazie》2013,346(2):140-153
In accordance with our antiviral drug development attempt, acylhydrazone derivatives bearing amino acid side chains were synthesized for the evaluation of their antiviral activity against various types of viruses. Among these compounds, 8 S , 11 S , and 12 S showed anti‐HIV‐1 activity with a 50% inhibitory concentration (IC50) = 123.8 µM (selectivity index, SI > 3), IC50 = 12.1 µM (SI > 29), IC50 = 17.4 µM (SI > 19), respectively. Enantiomers 8 R , 11 R , and 12 R were inactive against the HIV‐1 strain IIIB. Hydrazones 8 S , 11 S , and 12 S which were active against HIV‐1 wild type showed no inhibition against a double mutant NNRTI‐resistant strain (K103N;Y181C). Molecular docking calculations of R‐ and S‐enantiomers of 8 , 11 , and 12 were performed using the hydrazone‐bound novel site of HIV‐1 RT. 相似文献
7.
8.
9.
Synthesis,Biological Evaluation and Molecular Modeling Studies of New 2,3‐Diheteroaryl Thiazolidin‐4‐Ones as NNRTIs
下载免费PDF全文
![点击此处可从《Chemical biology & drug design》网站下载免费的PDF全文](/ch/ext_images/free.gif)
Utsab Debnath Saroj Verma Pankaj Singh Kavita Rawat Satish K. Gupta Raj K. Tripathi Hefazat H. Siddiqui Seturam B. Katti Yenamandra S. Prabhakar 《Chemical biology & drug design》2015,86(5):1285-1291
10.
11.
12.
13.
Junwon Kim Doohyun Lee Changmin Park Wonyoung So Mina Jo Taedong Ok Jeongjin Kwon Sunju Kong Suyeon Jo Youngmi Kim Jihyun Choi HyoungCheul Kim Yoonae Ko Inhee Choi Youngsam Park Jaewan Yoon MoonKyeong Ju Junghwan Kim Sung-Jun Han Tae-Hee Kim Jonathan Cechetto Jiyoun Nam Peter Sommer Michel Liuzzi Jinhwa Lee Zaesung No 《ACS medicinal chemistry letters》2012,3(8):678-682
14.
15.
16.
Nasser R. El-Brollosy Omar. A. Al-Deeb Ali A. El-Emam Erik B. Pedersen Paolo La Colla Gabriella Collu Giuseppina Sanna Roberta Loddo 《Archiv der Pharmazie》2009,342(11):663-670
Novel emivirine and TNK-651 analogues 5a – d were synthesized by reaction of chloromethyl ethyl ether and / or benzyl chloromethyl ether, respectively, with uracils having 5-ethyl and 6-(4-methylbenzyl) or 6-(3,4-dimethoxybenzyl) substituents. A series of new uracil non-nucleosides substituted at N-1 with cyclopropylmethyloxymethyl 9a – d , 2-phenylethyloxymethyl 9e – h , and 3-phenylprop-1-yloxymethyl 9i – l were prepared on treatment of the corresponding uracils with the appropriate acetals 8a – c . Some of the tested compounds showed good activity against HIV-1 wild type. Among them, 1-cyclopropylmethyloxymethyl-5-ethyl-6-(3,5-dimethylbenzyl)uracil 9c and 5-ethyl-6-(3,5-dimethylbenzyl)-1-(2-phenylethyloxymethyl)uracil 9g showed inhibitory potency equally to emivirine against HIV-1 wild type. Furthermore, compounds 9c and 9g showed marginal better activity against NNRTI resistant mutants than emivirine. 相似文献
17.
18.
19.