Literature DB >> 11378361

4,1-Benzoxazepinone analogues of efavirenz (Sustiva) as HIV-1 reverse transcriptase inhibitors.

A J Cocuzza1, D R Chidester, B C Cordova, R M Klabe, S Jeffrey, S Diamond, C A Weigelt, S S Ko, L T Bacheler, S K Erickson-Viitanen, J D Rodgers.   

Abstract

A series of 4,1-benzoxazepinone analogues of efavirenz (Sustiva) as potent NNRTIs has been discovered. The cis-3-alkylbenzoxazepinones are more potent then the trans isomers and can be synthesized preferentially by a novel stereoselective cyclization. The best compounds are potent orally bioavailable inhibitors of both wild-type HIV-1 and its clinically relevant K103N mutant virus, but are highly protein-bound in human plasma.

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Year:  2001        PMID： 11378361     DOI： 10.1016/s0960-894x(01)00239-6

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


  7 in total

1.  A highly sensitive ultra performance liquid chromatography-tandem mass spectrometric (UPLC-MS/MS) technique for quantitation of protein free and bound efavirenz (EFV) in human seminal and blood plasma.

Authors:  Lindsay B Avery; Teresa L Parsons; David J Meyers; Walter C Hubbard
Journal:  J Chromatogr B Analyt Technol Biomed Life Sci       Date:  2010-10-08       Impact factor: 3.205

2.  Towards discovering dual functional inhibitors against both wild type and K103N mutant HIV-1 reverse transcriptases: molecular docking and QSAR studies on 4,1-benzoxazepinone analogues.

Authors:  Zhenshan Zhang; Mingyue Zheng; Li Du; Jianhua Shen; Xiaomin Luo; Weiliang Zhu; Hualiang Jiang
Journal:  J Comput Aided Mol Des       Date:  2006-08-08       Impact factor: 3.686

3.  Actions of the small molecule ligands SW106 and AH-3960 on the type-1 parathyroid hormone receptor.

Authors:  Percy H Carter; Thomas Dean; Brijesh Bhayana; Ashok Khatri; Raj Rajur; Thomas J Gardella
Journal:  Mol Endocrinol       Date:  2015-01-13

4.  Synthesis of triazolo-fused benzoxazepines and benzoxazepinones via Passerini reactions followed by 1,3-dipolar cycloadditions.

Authors:  Fabio De Moliner; Martina Bigatti; Chiara De Rosa; Luca Banfi; Renata Riva; Andrea Basso
Journal:  Mol Divers       Date:  2014-06-04       Impact factor: 2.943

5.  Discovery of a small molecule antagonist of the parathyroid hormone receptor by using an N-terminal parathyroid hormone peptide probe.

Authors:  Percy H Carter; Rui-Qin Liu; William R Foster; Joseph A Tamasi; Andrew J Tebben; Margaret Favata; Ada Staal; Mary Ellen Cvijic; Michele H French; Vanessa Dell; Donald Apanovitch; Ming Lei; Qihong Zhao; Mark Cunningham; Carl P Decicco; James M Trzaskos; Jean H M Feyen
Journal:  Proc Natl Acad Sci U S A       Date:  2007-04-11       Impact factor: 11.205

6.  Access to benzo-fused nine-membered heterocyclic alkenes with a trifluoromethyl carbinol moiety via a double decarboxylative formal ring-expansion process under palladium catalysis.

Authors:  Pulakesh Das; Satoshi Gondo; Punna Nagender; Hiroto Uno; Etsuko Tokunaga; Norio Shibata
Journal:  Chem Sci       Date:  2018-02-23       Impact factor: 9.825

7.  Design, synthesis, crystal structure and fungicidal activity of (E)-5-(methoxyimino)-3,5-dihydrobenzo[e][1,2]oxazepin-4(1H)-one analogues.

Authors:  Dongyan Yang; Chuan Wan; MengMeng He; Chuanliang Che; Yumei Xiao; Bin Fu; Zhaohai Qin
Journal:  Medchemcomm       Date:  2017-03-08       Impact factor: 3.597
  7 in total

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