Literature DB >> 15081015

Solid-phase synthesis and SAR of 4-carboxy-2-azetidinone mechanism-based tryptase inhibitors.

James C Sutton1, Scott A Bolton, Malcolm E Davis, Karen S Hartl, Bruce Jacobson, Arvind Mathur, Martin L Ogletree, William A Slusarchyk, Robert Zahler, Steven M Seiler, Gregory S Bisacchi.   

Abstract

A series of nonguanidine N1-activated C4-carboxy azetidinone tryptase inhibitors was prepared by solid-phase methodology to quickly assess the SAR associated with distal functionality on the N1-activating group. From these studies, potent inhibitors with improved specificity were discovered.

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Year:  2004        PMID: 15081015     DOI: 10.1016/j.bmcl.2004.02.012

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


  4 in total

1.  Penicillin Derivatives Inhibit the SARS-CoV-2 Main Protease by Reaction with Its Nucleophilic Cysteine.

Authors:  Tika R Malla; Lennart Brewitz; Dorian-Gabriel Muntean; Hiba Aslam; C David Owen; Eidarus Salah; Anthony Tumber; Petra Lukacik; Claire Strain-Damerell; Halina Mikolajek; Martin A Walsh; Christopher J Schofield
Journal:  J Med Chem       Date:  2022-05-12       Impact factor: 8.039

2.  Synthesis of novel N-sulfonyl monocyclic beta-lactams as potential antibacterial agents.

Authors:  Aliasghar Jarrahpour; Maaroof Zarei
Journal:  Molecules       Date:  2006-01-31       Impact factor: 4.411

3.  Synthesis and antimicrobial activities of some novel diastereoselective monocyclic cis-β-lactams using 2-ethoxy carbonyl DCPN as a carboxylic acid activator.

Authors:  Mahesh Kumar Mishra; Vedeshwar Narayan Singh; Khursheed Ahmad; Sitaram Sharma
Journal:  Mol Divers       Date:  2020-05-13       Impact factor: 2.943

4.  Crystal structure of 1-(4-meth-oxy-phen-yl)-4-(4-nitro-phen-yl)-3-phen-oxy-azetidin-2-one.

Authors:  Sevim Türktekin Çelikesir; Mehmet Akkurt; Aliasghar Jarrahpour; Habib Allah Shafie; Ömer Çelik
Journal:  Acta Crystallogr E Crystallogr Commun       Date:  2015-01-01
  4 in total

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