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All Journal Majalah Farmasi dan Farmakologi (Trends in Pharmacy and Pharmaceutical Sciences) JOPS (Journal Of Pharmacy and Science) Molekul: Jurnal Ilmiah Kimia
Adel Zamri
Universitas Riau
Biochemistry, Genetics & Molecular Biology Chemistry Health Professions Immunology & microbiology Materials Science & Nanotechnology Medicine & Pharmacology Public Health

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Sintesis Dan Uji Aktivitas Antioksidan Senyawa Flavonol 2-(3,4,5-Dimetoksifenil)-3-Hidroksi-4h-Kromen-4-On Muhamad Rokhim; Adel Zamri; Hilwan Yuda Teruna
JURNAL FARMASI DAN MAKANAN Vol 2 No 2 (2019): Journal Of Pharmacy and Science
Publisher : LPPM Universitas Abdurrab

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.36341/jops.v2i2.847

Abstract

Flavonols derivatives of 2'-hydroxycalone have been synthesized under basic condition (KOH). The structures of all compounds were characterized based on the interpretation of spectroscopic data including HPLC, UV, FTIR, NMR and HRMS. Antioxidant activity was evaluated using the DPPH assay which showed that the flavonol 2'-hydroxycalone derivative was potentially active as antioxidants with IC50 values <1000 µg / mL.
SINTESIS, KARAKTERISASI STRUKTUR, DAN KAJIAN MOLECULAR DOCKING SENYAWA 4’-METOKSI FLAVONOL SEBAGAI INHIBITOR MAIN PROTEASE (MPro) SARS-CoV-2 Ihsan Ikhtiarudin; Nesa Agistia; Neni Frimayanti; Enda Mora; Rahma Dona; Nofriyanti; Rosnita Dewi Rahmawati; Adel Zamri
Majalah Farmasi dan Farmakologi Vol. 26 No. 1 (2022): MFF
Publisher : Faculty of Pharmacy, Hasanuddin University

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.20956/mff.v26i1.18652

Abstract

Main protease (MPro) merupakan salah satu protein yang memiliki peran penting dalam proses replikasi virus SARS-CoV-2. Beberapa studi in silico dan in vitro telah menunjukkan bahwa senyawa flavonoid baik alami maupun sintetis memiliki potensi yang menjanjikan untuk dikembangkan sebagai antivirus SARS-CoV-2. Penelitian ini bertujuan untuk mensintesis senyawa 4'-metoksi flavonol dan mengeksplorasi potensinya sebagai inhibitor MPro SARS-CoV-2. Sintesis dilakukan menggunakan senyawa awal 2'-hidroksi-4-metoksi kalkon melalui reaksi Algar-Flynn-Oyamada (AFO) dengan metode pengadukan (stirring method). Selanjutnya, kajian molecular docking dilakukan menggunakan struktur kristal MPro SARS-CoV-2 yang diunduh dari website RCSB Protein Data Bank (PDB ID: 6M2N). Hasil sintesis senyawa 4'-metoksi flavonol diperoleh rendemen produk sebesar 37,72 % dan struktur produk hasil sintesis telah dikonfirmasi melalui analisis spektroskopi UV-Vis, FT-IR, dan 1H NMR. Selanjutnya, hasil kajian molecular docking menunjukkan bahwa senyawa 4’-metoksi flavonol dapat membentuk ikatan hidrogen dengan dua residu penting pada sisi aktif 6M2N, yaitu Glu166 dan Gln189, dengan nilai energi bebas ikatan sebesar -7,13 kcal/mol dan nilai RMSD sebesar 1,45. Hasil kajian ini menunjukkan bahwa senyawa 4'-metoksi flavonol dapat terikat dengan lebih mudah pada sisi aktif MPro SARS-CoV-2 dibandingkan dengan baicalein sebagai senyawa flavonoid pembanding yang telah terbukti secara in vitro dapat menghambat aktivitas proteolitik MPro SARS-CoV-2.
Synthesis and Evaluation of Some Sulfonamide-Substituted of 1,3,5-Triphenyl Pyrazoline Derivatives as Tyrosinase Enzyme Inhibitors Nofal Herfindo; Neni Frimayanti; Ihsan ikhtiarudin; Yum eryanti; Adel zamri
Molekul Vol 18 No 2 (2023)
Publisher : Universitas Jenderal Soedirman

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.20884/1.jm.2023.18.2.6936

Abstract

Pyrazoline is well-known as heterocycles compound that can exhibit many biological effects. In this work, we synthesized a series of sulfonamide-substituted 1,3,5-triphenyl pyrazoline compounds as a promising tyrosinase inhibitor agent. These compounds prepared by multicomponent reaction of corresponding aldehyde, ketone, and hydrazine using seal-vessel reactor. Pyrazolines compound were tested for their tyrosinase inhibitor activity through in vitro assay. The test result found that compound 4c, 4d, and 4e possessed better tyrosinase inhibitory activity compared to the reference drug, kojic acid. Compound 4c exhibited the strongest tyrosinase inhibitory effect with an IC50 value of 30.14 µM. The results suggested that hydroxyl and methoxy substituent at para position are preferable. Furthermore, molecular docking studies result match the pattern of in vitro assay where the compound will provide a stronger binding interaction and lower binding free energies.
Co-Authors Enda Mora Hilwan Yuda Teruna Ihsan Ikhtiarudin Muhamad Rokhim Neni Frimayanti Nesa Agistia Nofal Herfindo Nofriyanti Rahma Dona Rosnita Dewi Rahmawati Yum eryanti