Literature DB >> 19902958

Solid phase synthesis of novel pyrrolidinedione analogs as potent HIV-1 integrase inhibitors.

Annapurna Pendri1, Timothy L Troyer, Michael J Sofia, Michael A Walker, B Narasimhulu Naidu, Jacques Banville, Nicholas A Meanwell, Ira Dicker, Zeyu Lin, Mark Krystal, Samuel W Gerritz.   

Abstract

A novel series of HIV-1 integrase inhibitors were identified from a 100 member (4R(1) x 5R(2) x 5R(3)) library of pyrrolidinedione amides. A solid-phase route was developed which facilitates the simultaneous variation at R(1), R(2), and R(3) of the pyrrolidinedione scaffold. The resulting library samples were assayed for HIV-1 integrase activity and analyzed to determine the R(1), R(2), and R(3) reagent contributions towards the activity.

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Year:  2010        PMID: 19902958     DOI: 10.1021/cc9001026

Source DB:  PubMed          Journal:  J Comb Chem        ISSN: 1520-4766


  1 in total

1.  Synthesis and Biological Activity Characterization of Novel 5-Oxopyrrolidine Derivatives with Promising Anticancer and Antimicrobial Activity.

Authors:  Karolina Kairytė; Birutė Grybaitė; Rita Vaickelionienė; Birutė Sapijanskaitė-Banevič; Povilas Kavaliauskas; Vytautas Mickevičius
Journal:  Pharmaceuticals (Basel)       Date:  2022-08-06
  1 in total

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