Synthesis and study of anti-HIV-1 RT activity of 5-benzoyl-4-methyl-1,3,4,5-tetrahydro-2H-1,5-benzodiazepin-2-one derivatives |
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| Institution: | 1. Medicinal Chemistry Research Laboratory, Department of Pharmacy, Birla Institute of Technology & Science, Pilani 333031, Rajasthan, India;2. Key Laboratory of Bioactive Peptides of Yunnan Province/Key Laboratory of Animal Models and Human Disease Mechanisms of Chinese Academy of Sciences, Kunming Institute of ZoologyChinese Academy of Sciences, Kunming, Yunnan 650223, China;3. Department of Chemistry, Faculty of Science, Universiti Teknologi Malaysia, 81310 Johor Bahru, Johor, Malaysia;4. LCM Laboratory, FSO, University of Mohammed Premier, Oujda 60000, Morocco;5. School of Pharmaceutical Science & Yunnan Key Laboratory of Pharmacology for Natural Products, Kunming Medical University, Kunming, Yunnan 650500, China;1. Department of Chemistry, Faculty of Sciences, Persian Gulf University, Bushehr, 75169, Iran;2. Department of Medicinal Chemistry, Faculty of Pharmacy, Zahedan University of Medical Sciences, Zahedan, Iran;1. Medicinal Chemistry Research Laboratory, Department of Pharmacy, Birla Institute of Technology & Science, Pilani 333031, India;2. Departmento de Ciencias Biomedicas, Facultad de Veterinaria, Universidad de Leon, Leon 24071, Spain;1. Dept. of Textile Chemistry, The South India Textile Research Association, Coimbatore 641014, India;2. Dept. of Biotech., School of Bio-Sciences and Technology, Vellore Institute of Technology, Vellore 632014, Tamil Nadu, India;3. Dept. of Chemistry, Bishop Heber College, Tiruchirappalli 17, Tamil Nadu, India;4. Department of Chemistry, B. S. Abdur Rahman Crescent University, Vandalur, Chennai 600 048, India;1. University of Monastir, Research Unit of Applied Chemistry and Environment/ UR13ES63, Department of Chemistry, Faculty of Sciences of Monastir, 5000, Monastir, Tunisia;2. University of Monastir, Laboratory of Heterocyclic Chemistry Natural Products and Reactivity/CHPNR, Department of Chemistry, Faculty of Sciences of Monastir, 5000, Monastir, Tunisia;3. IBMM, Univ Montpellier, CNRS, ENSCM, 34296, Montpellier, France;1. School of Medicine, Zhejiang University City College, Hangzhou 310015, Zhejiang, China;2. State Key Laboratory of Biotherapy & Cancer Center, West China Hospital, Sichuan University, and Collaborative Innovation Center of Biotherapy, Chengdu 610041, Sichuan, China;3. State Key Laboratory of Stomatology, West China Hospital of Stomatology, Sichuan University, Chengdu 610041, China |
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| Abstract: | In the present study, a series of fourteen 5-benzoyl-4-methyl-1,3,4,5-tetrahydro-2H-1,5-benzodiazepin-2-one derivatives were designed, synthesized and characterized by appropriate spectral analysis. Further, titled compounds were in-vitro screened against wild HIV-1 RT enzyme using ELISA based colorimetric assay, in which four compounds significantly inhibited the RT activity with IC50 ≤ 25 µM. Moreover, two significantly active compounds of the series, A10 and A11 exhibited IC50 values 8.62 and 6.87 µM respectively, during the in-vitro assay. Structure Activity Relationship (SAR) studies were performed for the synthesized compounds in order to estimate the effect of substitution pattern on the RT inhibitory potency. The cytotoxicity of the synthesized compounds was evaluated against T lymphocytes. Further, putative binding modes of the significantly active (A11) and the least active (A4) compounds with wild HIV-1 RT were also investigated using docking studies. |
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