synthesis of novel derivatives of 4-amino-3-(2-furyl)-5-mercapto-1,2,4-triazole as potential hiv-1 nnrtis(合成新颖的衍生品4-amino-3)- 2-furyl 5-mercapto-1,2,4-triazole作为潜在的hiv - 1 nnrtis.pdfVIP

synthesis of novel derivatives of 4-amino-3-(2-furyl)-5-mercapto-1,2,4-triazole as potential hiv-1 nnrtis(合成新颖的衍生品4-amino-3)- 2-furyl 5-mercapto-1,2,4-triazole作为潜在的hiv - 1 nnrtis.pdf

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synthesis of novel derivatives of 4-amino-3-(2-furyl)-5-mercapto-1,2,4-triazole as potential hiv-1 nnrtis(合成新颖的衍生品4-amino-3)- 2-furyl 5-mercapto-1,2,4-triazole作为潜在的hiv - 1 nnrtis

Molecules 2007, 12, 2003-2016 molecules ISSN 1420-3049 © 2007 by MDPI /molecules Full Paper Synthesis of Novel Derivatives of 4-Amino-3-(2-Furyl)-5-Mercapto-1,2,4-Triazole as Potential HIV-1 NNRTIs Jingde Wu 1, Xinyong Liu 1,*, Xianchao Cheng 1, Yuan Cao 1, Defeng Wang 1, Zhong Li 1, 1 2 2 2 Wenfang Xu , Christophe Pannecouque , Myriam Witvrouw and Erik De Clercq 1 Institute of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University, No.44, Wenhuaxi Road, Jinan, 250012, P.R. China 2 Rega Institute for Medical Research, Katholieke Universiteit Leuven, B-3000 Leuven, Belgium; E- mail: erik.declercq@rega.kuleuven.be (Erik De Clercq) * Author to whom correspondence should be addressed; E-mail: xinyongl@; Tel: (+86)-531 Fax: (+86)-531 Received: 21 July 2007; in revised form: 17 August 2007 / Accepted: 20 August 2007 / Published: 21 August 2007 Abstract: A series of 5-alkylthio (2a-d), 4-arylideneamino (3a-d) and 4-arylideneamino- 5-alkylthio derivatives (4a-f) of 4-amino-3-(2-furyl)-5-mercapto-1,2,4-triazole (1) were synthesized by alkylation of the parent compound with alkyl halides and condensation with aldehydes, respectively. Sulfanyl dimers 5a-d and 4-iminomethyl dimer 6 were correspondingly prepared by reaction with alkane dibromides and 1,4-diformylbenzene. Mannich base 7 was also synthesized by aminomethylation of the 3-sulfanyltriazole 1 at the N

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