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Microwave-assisted synthesis of hydroxybenzylidene-andrographolides and its inhibitory activity against HIV-1 protease
Megantara S.a,b, Halimah H.b, Putrianty A.b, Tjahjono D.H.a, Kartasasmita R.E.a, Iwo M.I.a, Levita J.b, Ibrahim S.a
a School of Pharmacy, Bandung Institute of Technology, West Java, 40132, Indonesia
b Faculty of Pharmacy, Universitas Padjadjaran, Jatinangor, West Java, 45363, Indonesia
[vc_row][vc_column][vc_row_inner][vc_column_inner][vc_separator css=”.vc_custom_1624529070653{padding-top: 30px !important;padding-bottom: 30px !important;}”][/vc_column_inner][/vc_row_inner][vc_row_inner layout=”boxed”][vc_column_inner width=”3/4″ css=”.vc_custom_1624695412187{border-right-width: 1px !important;border-right-color: #dddddd !important;border-right-style: solid !important;border-radius: 1px !important;}”][vc_empty_space][megatron_heading title=”Abstract” size=”size-sm” text_align=”text-left”][vc_column_text]© 2018 Sandra Megantara et al.Andrographolide, a lacton diterpenoid, due to its many biological activities, was subjected to a semi-synthetic work by reacting andrographolide (a) with hydroxybenzaldehyde under microwave irradiation. This reaction led to three new andrographolide analogues, which are 3,19-2-hydroxybenzylidene andrographolide (b), 3,19-3-hydroxybenzylidene andrographolide (c), and 3,19-4-hydroxybenzylidene andrographolide (d), respectively. The yields were 85%, 86%, 86% for compounds b, c, d respectively. These new compounds had already been studied previously by pharmacophore screening and molecular docking simulation, which revealed their affinity to HIV-1 protease. Furthermore, their inhibitory activity against HIV-1 protease was measured by in vitro fluorometric method at (Ex/Em) = 330/450 nm which resulted 18.14, 10.72, 9.93, 8.32 μM respectively for IC50 value. The increased activity of these compounds may reflect the binding of the hydroxybenzaldehyde moiety with the hydrophobic area of the HIV-1 protease.[/vc_column_text][vc_empty_space][vc_separator css=”.vc_custom_1624528584150{padding-top: 25px !important;padding-bottom: 25px !important;}”][vc_empty_space][megatron_heading title=”Author keywords” size=”size-sm” text_align=”text-left”][vc_column_text][/vc_column_text][vc_empty_space][vc_separator css=”.vc_custom_1624528584150{padding-top: 25px !important;padding-bottom: 25px !important;}”][vc_empty_space][megatron_heading title=”Indexed keywords” size=”size-sm” text_align=”text-left”][vc_column_text]Andrographolide,ARVs,HIV,HIV-1 protease inhibitors,Hydroxybenzylidene andrographolide[/vc_column_text][vc_empty_space][vc_separator css=”.vc_custom_1624528584150{padding-top: 25px !important;padding-bottom: 25px !important;}”][vc_empty_space][megatron_heading title=”Funding details” size=”size-sm” text_align=”text-left”][vc_column_text][/vc_column_text][vc_empty_space][vc_separator css=”.vc_custom_1624528584150{padding-top: 25px !important;padding-bottom: 25px !important;}”][vc_empty_space][megatron_heading title=”DOI” size=”size-sm” text_align=”text-left”][vc_column_text]https://doi.org/10.7324/JAPS.2018.8302[/vc_column_text][/vc_column_inner][vc_column_inner width=”1/4″][vc_column_text]Widget Plumx[/vc_column_text][/vc_column_inner][/vc_row_inner][/vc_column][/vc_row][vc_row][vc_column][vc_separator css=”.vc_custom_1624528584150{padding-top: 25px !important;padding-bottom: 25px !important;}”][/vc_column][/vc_row]