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Design, synthesis and SAR study of bridged tricyclic pyrimidinone carboxamides as HIV-1 integrase inhibitors.
Patel, Manoj; Naidu, B Narasimhulu; Dicker, Ira; Higley, Helen; Lin, Zeyu; Terry, Brian; Protack, Tricia; Krystal, Mark; Jenkins, Susan; Parker, Dawn; Panja, Chiradeep; Rampulla, Richard; Mathur, Arvind; Meanwell, Nicholas A; Walker, Michael A.
Afiliação
  • Patel M; Departments of Discovery Chemistry and Molecular Technologies, 5 Research Parkway, Wallingford, CT 06492, USA; ViiV Healthcare, 36 East Industrial Parkway, Branford, CT 06405, USA. Electronic address: manoj.m.patel@viivhealthcare.com.
  • Naidu BN; Departments of Discovery Chemistry and Molecular Technologies, 5 Research Parkway, Wallingford, CT 06492, USA; ViiV Healthcare, 36 East Industrial Parkway, Branford, CT 06405, USA.
  • Dicker I; Virology, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, USA; ViiV Healthcare, 36 East Industrial Parkway, Branford, CT 06405, USA.
  • Higley H; Virology, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, USA.
  • Lin Z; Virology, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, USA.
  • Terry B; Virology, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, USA.
  • Protack T; Virology, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, USA.
  • Krystal M; Virology, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, USA; ViiV Healthcare, 36 East Industrial Parkway, Branford, CT 06405, USA.
  • Jenkins S; Departments of Discovery Chemistry and Molecular Technologies, 5 Research Parkway, Wallingford, CT 06492, USA; ViiV Healthcare, 36 East Industrial Parkway, Branford, CT 06405, USA.
  • Parker D; Departments of Discovery Chemistry and Molecular Technologies, 5 Research Parkway, Wallingford, CT 06492, USA; ViiV Healthcare, 36 East Industrial Parkway, Branford, CT 06405, USA.
  • Panja C; Biocon-Bristol-Myers Squibb Research Center, Plot 2 & 3, Bommasandra Industrial Estate - Phase-IV, Bommasandra-Jigani Link Road, Bengaluru, Karnataka 560099, India.
  • Rampulla R; Department of Discovery Chemistry Synthesis, Bristol-Myers Squibb Research and Development, PO Box 4000, Princeton, NJ 08543-4000, USA.
  • Mathur A; Department of Discovery Chemistry Synthesis, Bristol-Myers Squibb Research and Development, PO Box 4000, Princeton, NJ 08543-4000, USA.
  • Meanwell NA; Departments of Discovery Chemistry and Molecular Technologies, 5 Research Parkway, Wallingford, CT 06492, USA.
  • Walker MA; Departments of Discovery Chemistry and Molecular Technologies, 5 Research Parkway, Wallingford, CT 06492, USA; Assembly Biosciences, Inc. 331 Oyster Point Blvd, San Francisco, CA 94080, USA.
Bioorg Med Chem ; 28(13): 115541, 2020 07 01.
Article em En | MEDLINE | ID: mdl-32389483
ABSTRACT
The design, synthesis and structure-activity relationships associated with a series of bridged tricyclic pyrimidinone carboxamides as potent inhibitors of HIV-1 integrase strand transfer are described. Structural modifications to these molecules were made in order to examine the effect on potency towards wild-type and clinically-relevant resistant viruses. The [3.2.2]-bridged tricyclic system was identified as an advantageous chemotype, with representatives exhibiting excellent antiviral activity against both wild-type viruses and the G140S/Q148H resistant virus that arises in response to therapy with raltegravir and elvitegravir.
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Antivirais / Pirrolidinonas / Infecções por HIV / Inibidores de Integrase de HIV / Integrase de HIV / Imidazóis Idioma: En Ano de publicação: 2020 Tipo de documento: Article
Texto completo
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Antivirais / Pirrolidinonas / Infecções por HIV / Inibidores de Integrase de HIV / Integrase de HIV / Imidazóis Idioma: En Ano de publicação: 2020 Tipo de documento: Article