Literature DB >> 22090663

MAOS ls for the general synthesis and lead optimization of 3,6-disubstituted-[1,2,4]triazolo[4,3-b]pyridazines.

Leslie N Aldrich1, Evan P Lebois, L Michelle Lewis, Natalia T Nalywajko, Colleen M Niswender, C David Weaver, P Jeffrey Conn, Craig W Lindsley.   

Abstract

General, high-yielding MAOS protocols for the expedient synthesis of functionalized 3,6-disubstituted-[1,2,4]triazolo[4,3-b]pyridazines are described amenable to an iterative analog library synthesis strategy for the lead optimization of an M1 antagonist screening hit. Optimized compounds proved to be highly selective M1 antagonists.

Entities:  

Year:  2009        PMID： 22090663      PMCID： PMC3214729          DOI： 10.1016/j.tetlet.2008.10.127

Source DB:  PubMed          Journal:  Tetrahedron Lett        ISSN： 0040-4039            Impact factor:   2.415


  8 in total

Review 1.  Application of combinatorial chemistry science on modern drug discovery.

Authors:  J Phillip Kennedy; Lyndsey Williams; Thomas M Bridges; R Nathan Daniels; David Weaver; Craig W Lindsley
Journal:  J Comb Chem       Date:  2008-01-26

2.  Synthesis and SAR of selective muscarinic acetylcholine receptor subtype 1 (M1 mAChR) antagonists.

Authors:  L Michelle Lewis; Douglas Sheffler; Richard Williams; Thomas M Bridges; J Phillip Kennedy; J T Brogan; Matthew J Mulder; Lyndsey Williams; Natalia T Nalywajko; Colleen M Niswender; Charles D Weaver; P Jeffrey Conn; Craig W Lindsley
Journal:  Bioorg Med Chem Lett       Date:  2008-01-04       Impact factor: 2.823

3.  Discovery of 3-aminopiperidines as potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitors.

Authors:  Jason M Cox; Bart Harper; Anthony Mastracchio; Barbara Leiting; Ranabir Sinha Roy; Reshma A Patel; Joseph K Wu; Kathryn A Lyons; Huaibing He; Shiyao Xu; Bing Zhu; Nancy A Thornberry; Ann E Weber; Scott D Edmondson
Journal:  Bioorg Med Chem Lett       Date:  2007-06-02       Impact factor: 2.823

4.  Allosteric Akt (PKB) inhibitors: discovery and SAR of isozyme selective inhibitors.

Authors:  Craig W Lindsley; Zhijian Zhao; William H Leister; Ronald G Robinson; Stanley F Barnett; Deborah Defeo-Jones; Raymond E Jones; George D Hartman; Joel R Huff; Hans E Huber; Mark E Duggan
Journal:  Bioorg Med Chem Lett       Date:  2005-02-01       Impact factor: 2.823

Review 5.  Muscarinic toxins from the green mamba.

Authors:  K N Bradley
Journal:  Pharmacol Ther       Date:  2000-02       Impact factor: 12.310

6.  Efficient synthesis of imidazoles from aldehydes and 1,2-diketones using microwave irradiation.

Authors:  Scott E Wolkenberg; David D Wisnoski; William H Leister; Yi Wang; Zhijian Zhao; Craig W Lindsley
Journal:  Org Lett       Date:  2004-04-29       Impact factor: 6.005

7.  6-(Alkylamino)-3-aryl-1,2,4-triazolo[3,4-a]phthalazines. A new class of benzodiazepine receptor ligands.

Authors:  G Tarzia; E Occelli; E Toja; D Barone; N Corsico; L Gallico; F Luzzani
Journal:  J Med Chem       Date:  1988-06       Impact factor: 7.446

8.  3-phenyl-6-(2-pyridyl)methyloxy-1,2,4-triazolo[3,4-a]phthalazines and analogues: high-affinity gamma-aminobutyric acid-A benzodiazepine receptor ligands with alpha 2, alpha 3, and alpha 5-subtype binding selectivity over alpha 1.

Authors:  Robert W Carling; Kevin W Moore; Leslie J Street; Deborah Wild; Catherine Isted; Paul D Leeson; Steven Thomas; Desmond O'Connor; Ruth M McKernan; Katherine Quirk; Susan M Cook; John R Atack; Keith A Wafford; Sally A Thompson; Gerard R Dawson; Pushpinder Ferris; José L Castro
Journal:  J Med Chem       Date:  2004-03-25       Impact factor: 7.446
  8 in total
  1 in total

Review 1.  Controlled microwave heating in modern organic synthesis: highlights from the 2004-2008 literature.

Authors:  C Oliver Kappe; Doris Dallinger
Journal:  Mol Divers       Date:  2009-04-21       Impact factor: 2.943
  1 in total

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