Results 41 to 50 of about 148 (100)

Synthesis and anti-HIV Activity of aryl-2-[(4-cyanophenyl)amino]-4-pyrimidinone hydrazones as potent non-nucleoside reverse transcriptase inhibitors

, 2011
A series of novel diarylpyrimidines (DAPYs) with a ketone hydrazone substituent on the methylene linker between the pyrimidine nucleus and the aryl moiety at the C-4 position were synthesized, and their antiviral activity against human immunodeficiency ...
Ma, Xiao-Dong, De Clercq, Erik, Pannecouque, Christophe, Chen, Fen-Er, Gu, Shuang-Xi, Balzarini, Jan, Yang, Shi-Qiong, Xiao-Dong Ma, Christophe Pannecouque, Jan Balzarini, Shi-Qiong Yang, Erik De Clercq, Qiu-Qin He, Fen-Er Chen, Shuang-Xi Gu   +14 more
core   +1 more source

Discovery of nitropyridine derivatives as potent HIV-1 non-nucleoside reverse transcriptase inhibitors via a structure-based core refining approach

, 2014
As a continuation of our efforts to discover and develop back-up analogs of DAPYs, novel substituted nitropyridine derivatives were designed via a structure-based core refining approach, synthesized and evaluated for their in vitro HIV-1 activity in MT-4 
Zhan, Peng, De Clercq, Erik, Pannecouque, Christophe, Li, Zhenyu, Liu, Huiqing, Liu, Xinyong, Wang, J.   +6 more
core   +1 more source

Synthesis and biological evaluation of DAPY-DPEs hybrids as non-nucleoside inhibitors of HIV-1 reverse transcriptase

, 2015
A series of new DAPY-DPEs hybrids, combined the important pharmacophores of DAPYs and DPEs, has been synthesized and biologically evaluated for their anti-HIV activities against wild-type HIV-1 strain IIIB, double RT mutant (K103N+Y181C) strain RES056 ...
Pannecouque, Christophe, De Clercq, Erik, He, Qiu-Qin, Chen, Fen-Er, Daelemans, Dirk, Wu, Hai-Qiu, Chen, Wen-Xue, Yao, Jin   +7 more
core   +1 more source

Conformational restriction design of thiophene-biphenyl-DAPY HIV-1 non-nucleoside reverse transcriptase inhibitors

, 2019
Conformational restriction is a promising strategy in the development of DAPY-type non-nucleoside reverse transcriptase inhibitors (NNRTIs). Herein, eighteen thiophene-biphenyl-DAPY derivatives were designed and synthesized as potent HIV-1 NNRTIs in ...
Sang, Yali, Pannecouque, Christophe, De Clercq, Erik, Chen, Fener, Han, Sheng, Zhuang, Chunlin   +5 more
core   +1 more source

In vitro evaluation of nonnucleoside reverse transcriptase inhibitors UC-781 and TMC120-R147681 as human immunodeficiency virus microbicides

, 2004
An in vitro model of monocyte-derived dendritic cells (MO-DC) and CD4(+) T cells, representing the primary targets of sexual human immunodeficiency virus (HIV) transmission, was used to evaluate the antiviral and immune suppressive activity of new ...
Vanham, G., Janssen, P., Kestens, L., Lewi, P., Balzarini, J., Michiels, J., Van Herrewege, Y., Van Roey, J., Fransen, K.   +8 more
core   +1 more source

Structural optimization of pyridine-type DAPY derivatives to exploit the tolerant regions of the NNRTI binding pocket

, 2016
Based on the crystallographic studies of diarylpyrimidines (DAPYs), we embarked on incorporating the hydrophilic piperidyl or morpholinyl group into the known DAPY derivatives bearing the pyridine moiety as a core structure, with the double aim to ...
Zhan, Peng, Huang, Boshi, De Clercq, Erik, Pannecouque, Christophe, Daelemans, Dirk, Liu, Xinyong, Chen, Wenmin, Yang, Jiapei   +7 more
core   +1 more source

Reflections on the Rega Institute for Medical Research, at the fiftieth anniversary of the Rega Stichting vzw (Rega Instituut vzw, Rega Foundation). [PDF]

Antivir Chem Chemother, 2022
Clercq E.
europepmc   +1 more source

Evolving understanding of HIV-1 reverse transcriptase structure, function, inhibition, and resistance. [PDF]

Curr Opin Struct Biol, 2020
Xavier Ruiz F, Arnold E.
europepmc   +1 more source

Recovery of the soil fungal microbiome after steam disinfection to manage the plant pathogen Fusarium solani. [PDF]

Front Plant Sci, 2023
Larson ER, Crandall SG.
europepmc   +1 more source

Improving the positional adaptability: structure-based design of biphenyl-substituted diaryltriazines as novel non-nucleoside HIV-1 reverse transcriptase inhibitors. [PDF]

Acta Pharm Sin B, 2020
Jin K, Liu M, Zhuang C, De Clercq E, Pannecouque C, Meng G, Chen F.   +6 more
europepmc   +1 more source