Abstract:
:A diversity of novel 2-aryl-3-heteroaryl-2-ylmethyl-1,3-thiazolidin-4-ones were designed and synthesized by reacting heteroaryl-2-ylmethyl amine with various 2,6-dihalosubstituted benzaldehydes and mercaptoacetic acid. The title compounds were evaluated for human immunodeficiency virus type-1 (HIV-1) reverse transcriptase (RT) inhibitory activity. The results of in vitro assays showed that some of the compounds were effective inhibitors of HIV-1 reverse transcriptase enzyme at micromolar concentrations with less cytotoxicity in both MT-4 cells as well as acutely infected human T-lymphoid CEM cells. Compounds 4h and 4k emerged as moderately more potent with EC(50) are at 0.20 and 0.21 microM as compared to reference parent compound thiazolobenzimidazoles EC(50) 0.35 microM in MT-4 cells.
journal_name
Chem Biol Drug Desjournal_title
Chemical biology & drug designauthors
Rawal RK,Tripathi R,Kulkarni S,Paranjape R,Katti SB,Pannecouque C,De Clercq Edoi
10.1111/j.1747-0285.2008.00683.xsubject
Has Abstractpub_date
2008-08-01 00:00:00pages
147-54issue
2eissn
1747-0277issn
1747-0285pii
JPP683journal_volume
72pub_type
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