Literature DB >> 20727748

Design of a series of bicyclic HIV-1 integrase inhibitors. Part 1: selection of the scaffold.

Eric D Jones1, Nick Vandegraaff, Giang Le, Neil Choi, William Issa, Katherine Macfarlane, Neeranat Thienthong, Lisa J Winfield, Jonathan A V Coates, Long Lu, Xinming Li, Xiao Feng, Changjiang Yu, David I Rhodes, John J Deadman.   

Abstract

HIV integrase inhibitors based on a novel bicyclic pyrimidinone core is presented. Nine variations of the core scaffold are evaluated leading to optimization of the 6:6 core giving compound 48 with an EC(50) of 3 nM against wild type HIV infected T-cells.
Copyright © 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID: 20727748     DOI: 10.1016/j.bmcl.2010.07.079

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  4 in total

Review 1.  Targeting Metalloenzymes for Therapeutic Intervention.

Authors:  Allie Y Chen; Rebecca N Adamek; Benjamin L Dick; Cy V Credille; Christine N Morrison; Seth M Cohen
Journal:  Chem Rev       Date:  2018-09-07       Impact factor: 60.622

2.  Synergism of fused bicyclic 2-aminothiazolyl compounds with polymyxin B against Klebsiella pneumoniae.

Authors:  Rong Wang; Shuang Hou; Xiaojing Dong; Daijie Chen; Lei Shao; Liujia Qian; Zhong Li; Xiaoyong Xu
Journal:  Medchemcomm       Date:  2017-09-14       Impact factor: 3.597

Review 3.  KYNA Derivatives with Modified Skeleton; Hydroxyquinolines with Potential Neuroprotective Effect.

Authors:  Bálint Lőrinczi; István Szatmári
Journal:  Int J Mol Sci       Date:  2021-11-03       Impact factor: 5.923

4.  Catalyst-Free One-Pot Synthesis of Densely Substituted Pyrazole-Pyrazines as Anti-Colorectal Cancer Agents.

Authors:  Jia Xu; Hong-Bo Tan; Ya-Jun Zhang; Dian-Yong Tang; Fenghuang Zhan; Hong-Yu Li; Zhong-Zhu Chen; Zhi-Gang Xu
Journal:  Sci Rep       Date:  2020-06-09       Impact factor: 4.379

  4 in total

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