Synthesis and Anti-HIV-1 Activity of a Novel Series of Aminoimidazole Analogs

GANGULY S., MURUGESAN S., PRASANTHİ N., Alpturk O., Herman B., Sluis-Cremer N.

LETTERS IN DRUG DESIGN & DISCOVERY, cilt.7, sa.5, ss.318-323, 2010 (SCI-Expanded) identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 7 Sayı: 5
  • Basım Tarihi: 2010
  • Doi Numarası: 10.2174/157018010791163424
  • Dergi Adı: LETTERS IN DRUG DESIGN & DISCOVERY
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Sayfa Sayıları: ss.318-323
  • İstanbul Teknik Üniversitesi Adresli: Hayır

Özet

There is still an urgent need to develop nonnucleoside reverse transcriptase (RT) inhibitors (NNRTI) with a high-genetic barrier to resistance that facilitate patient adherence and allow durable suppression of HIV-1 replication. In this study, we describe the synthesis of a novel series of N-aminoimidazole (NAIM) analogs. Each of the NAIM analogs display potent activity against wild-type recombinant purified HIV-1 RT as well as RTs containing the K103N or Y181C resistance mutations. The analogs, however, do not exhibit significant antiviral activity in cell culture and were, in general, cytotoxic. Nevertheless, these data suggest that the NAIM backbone may provide a suitable scaffold from which inhibitors active against NNRTI-resistant HIV-1 could be developed.