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The structure-activity profile of mercaptobenzamides' anti-HIV activity suggests that thermodynamics of metabolism is more important than binding affinity to the target.
Nikolayevskiy, Herman; Robello, Marco; Scerba, Michael T; Pasternak, Evan H; Saha, Mrinmoy; Hartman, Tracy L; Buchholz, Caitlin A; Buckheit, Robert W; Durell, Stewart R; Appella, Daniel H.
Affiliation
  • Nikolayevskiy H; Synthetic Bioactive Molecules Section, LBC, NIDDK, NIH, 8 Center Drive, Room 404, Bethesda, MD, 20892, USA.
  • Robello M; Synthetic Bioactive Molecules Section, LBC, NIDDK, NIH, 8 Center Drive, Room 404, Bethesda, MD, 20892, USA.
  • Scerba MT; Synthetic Bioactive Molecules Section, LBC, NIDDK, NIH, 8 Center Drive, Room 404, Bethesda, MD, 20892, USA.
  • Pasternak EH; Synthetic Bioactive Molecules Section, LBC, NIDDK, NIH, 8 Center Drive, Room 404, Bethesda, MD, 20892, USA.
  • Saha M; Synthetic Bioactive Molecules Section, LBC, NIDDK, NIH, 8 Center Drive, Room 404, Bethesda, MD, 20892, USA.
  • Hartman TL; ImQuest Biosciences, 7340 Executive Way, Suite R, Frederick, MD, 21704, USA.
  • Buchholz CA; ImQuest Biosciences, 7340 Executive Way, Suite R, Frederick, MD, 21704, USA.
  • Buckheit RW; ImQuest Biosciences, 7340 Executive Way, Suite R, Frederick, MD, 21704, USA.
  • Durell SR; Laboratory of Cell Biology, NCI, NIH, 9000 Rockville Pike, Bethesda, MD, 20892, USA.
  • Appella DH; Synthetic Bioactive Molecules Section, LBC, NIDDK, NIH, 8 Center Drive, Room 404, Bethesda, MD, 20892, USA. Electronic address: appellad@niddk.nih.gov.
Eur J Med Chem ; 178: 818-837, 2019 Sep 15.
Article in En | MEDLINE | ID: mdl-31252286
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Thermodynamics / Benzamides / HIV-1 / Anti-HIV Agents Limits: Humans Language: En Journal: Eur J Med Chem Year: 2019 Document type: Article Affiliation country: Estados Unidos Country of publication: Francia
Fulltext
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Thermodynamics / Benzamides / HIV-1 / Anti-HIV Agents Limits: Humans Language: En Journal: Eur J Med Chem Year: 2019 Document type: Article Affiliation country: Estados Unidos Country of publication: Francia