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Abstract
Seven novel N-arylsulfonyl-3-(2-yl-ethanone)-6-methylindole derivatives 4a–f and 6 were readily synthesized and have been identified as inhibitors of human immunodeficiency virus type-1 (HIV-1) replication. Initial biological studies indicated that among these derivatives, N-(p-ethyl)phenylsulfonyl-3-[2-morpholinoethanone]-6-methylindole (4f) and N-(p-ethyl)phenylsulfonyl-3-[2-(5-phenyl-1,3,4-oxadiazole-2-yl-thio)ethanone]-6-methylindole (6) showed the most promising activity against HIV-1 replication. The effective concentration (EC50) and therapeutic index (TI) values of 4f and 6 were 9.42/4.62 μM, and >49.77/66.95, respectively. The cytotoxicity of these compounds has also been assessed. No significant cytotoxicities were found for any of these compounds.
Highlights
The use of chemotherapy to suppress replication of the human immunodeficiency virus (HIV) has transformed the face of acquired immunodeficiency syndrome (AIDS) in the developed world.Pronounced reductions in illness and death have been achieved and healthcare utilization has diminished.HIV therapy has provided many new insights into the pathogenesis and the viral and cellular dynamics of HIV infection, but challenges remain
As a continuation of the research program of our laboratory searching for anti-human immunodeficiency virus type-1 (HIV-1) agents [7,8,9], we report the design and synthesis of some novel N-arylsulfonyl-3-(2-yl-ethanone)-6-methylindoles derivatives 4a–f and 6 (Schemes 1 and 2), which can inhibit HIV-1 replication
Initial biological studies indicated that N-(p-ethyl)phenylsulfonyl-3-[2-morpholinoethanone]-6-methylindole (4f) and
Summary
The use of chemotherapy to suppress replication of the human immunodeficiency virus (HIV) has transformed the face of acquired immunodeficiency syndrome (AIDS) in the developed world. HIV therapy has provided many new insights into the pathogenesis and the viral and cellular dynamics of HIV infection, but challenges remain. Treatment does not suppress HIV replication in all patients, and the emergence of drug-resistant virus hinders subsequent treatment. Chronic therapy can Pharmaceuticals 2015, 8 result in toxicity. These challenges prompt the continued search for new drugs and new therapeutic strategies to control chronic viral replication [1,2,3,4]. The design and synthesis of brand new, specific, efficacious, safe chemotherapeutic drugs for the prevention of the spread of HIV-1 infection is imperative.
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