Design and synthesis of caffeoyl-anilides as portmanteau inhibitors of HIV-1 integrase and CCR5 |
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Authors: | Bodiwala Hardik S Sabde Sudeep Gupta Pawan Mukherjee Ruchira Kumar Rajender Garg Prabha Bhutani Kamlesh Kumar Mitra Debashis Singh Inder Pal |
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Institution: | Department of Natural Products, National Institute of Pharmaceutical Education and Research, Sector-67, S.A.S. Nagar, Punjab 160 062, India. |
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Abstract: | Designing multi-functional ligands is a recent strategy by which multiple targets can be inhibited by a single entity. A series of caffeoyl-anilide compounds based on structures of various integrase and CCR-5 inhibitors have been designed and synthesized as anti-HIV agents in the present study. Most of the compounds exhibited potent anti-HIV activity at micromolar concentration in CEM-GFP CD4+ T cells infected with HIV-1NL4.3 virus. Compound 14 showed a lower EC(50) and better TI as compared to AZT. Mechanism based studies suggest that these compounds inhibit either one or in some cases, both the targets. The experimental data and the docking results showed that these compounds are potential inhibitors for both HIV-1 IN and CCR5. |
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