Computer-Aided Design, Synthesis, and Anti-HIV-1 Activity in Vitro of 2-Alkylamino-6-[1-(2,6-difluorophenyl)alkyl]-3,4-dihydro-5-alkylpyrimidin-4(3H)- ones as Novel Potent Non-Nucleoside Reverse Transcriptase Inhibitors, Also Active Against the Y181C Variant

2004 ◽  
Vol 47 (4) ◽  
pp. 928-934 ◽  
Author(s):  
Rino Ragno ◽  
Antonello Mai ◽  
Gianluca Sbardella ◽  
Marino Artico ◽  
Silvio Massa ◽  
...  
Keyword(s):  
Reverse Transcriptase ◽  
Computer Aided Design ◽  
Reverse Transcriptase Inhibitors ◽  
Nucleoside Reverse Transcriptase Inhibitors ◽  
Design Synthesis ◽  
Computer Aided ◽  
Aided Design ◽  
Anti Hiv ◽  
Hiv 1

Computer-Aided Design, Synthesis and Validation of 2-Phenylquinazolinone Fragments as CDK9 Inhibitors with Anti-HIV-1 Tat-Mediated Transcription Activity

ChemMedChem ◽  
2013 ◽  
Vol 8 (12) ◽  
pp. 1941-1953 ◽  
Author(s):  
Luca Sancineto ◽  
Nunzio Iraci ◽  
Serena Massari ◽  
Vanessa Attanasio ◽  
Gianmarco Corazza ◽  
...  
Keyword(s):  
Computer Aided Design ◽  
Design Synthesis ◽  
Transcription Activity ◽  
Computer Aided ◽  
Aided Design ◽  
Anti Hiv ◽  
Hiv 1

Nitroimidazoles Part 6. Synthesis, Structure and in Vitro anti-HIV Activity of New 5-substituted Piperazinyl-4-nitroimidazole Derivatives

2007 ◽  
Vol 18 (4) ◽  
pp. 191-200 ◽  
Author(s):  
Najim A Al-Masoudi ◽  
Yaseen A Al-Soud ◽  
Erik De Clercq ◽  
Christophe Pannecouque
Keyword(s):  
Reverse Transcriptase ◽  
Reverse Transcriptase Inhibitors ◽  
Nucleoside Reverse Transcriptase Inhibitors ◽  
Phthalimide Derivative ◽  
Anti Hiv ◽  
Hiv 1

2-Amino-1-[4-(1-benzyl-2-ethyl-4-nitro-1 H-imidazol-5-yl)piperazin-1-yl]ethanone [6] was prepared from 1-(1-benzyl-2-ethyl-4-nitro-1 H-imidazol-5-yl) piperazine [3]. A series of new 2-oxoethyl-arylamide [9,10] and 2-oxoethyl-arylsulphonamide [11–14] derivatives were synthesized from [6] with the aim of developing new non-nucleoside reverse transcriptase inhibitors. Alternatively, the amine [17] was synthesized from [3] via the phthalimide derivative [16]. The arylsulphonamide derivatives [18–23] and the arylamide analogues [24–26] were synthesized from [17]. The compounds were evaluated for their anti-HIV-1 and anti-HIV-2 activity in MT-4 cells.

Sign in / Sign up

Export Citation Format

Share Document