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All Journal ComEngApp : Computer Engineering and Applications Journal VALENSI JURNAL KIMIA SAINS DAN APLIKASI Jurnal Natur Indonesia Teknika Jurnal Riset Kimia SEMIRATA 2015 Jurnal Pengabdian UntukMu NegeRI Jurnal Surya Medika Jurnal CoreIT Indonesian Journal of Chemistry JSFK (Jurnal Sains Farmasi & Klinis) JURNAL PHOTON JURNAL PENDIDIKAN TAMBUSAI J-Dinamika: Jurnal Pengabdian Kepada Masyarakat Building of Informatics, Technology and Science Jurnal Yustitia Zonasi: Jurnal Sistem Informasi JOURNAL OF INFORMATION SYSTEM RESEARCH (JOSH) Journal of Computer System and Informatics (JoSYC) Community Development Journal: Jurnal Pengabdian Masyarakat Jurnal Pengabdian kepada Masyarakat Nusantara Information System Journal (INFOS) KLIK: Kajian Ilmiah Informatika dan Komputer JUSTIN (Jurnal Sistem dan Teknologi Informasi) Dinamika Lingkungan Indonesia Makara Journal of Science MASALIQ: Jurnal Pendidikan dan Sains Aurelia: Jurnal Penelitian dan Pengabdian Masyarakat Indonesia Counseling and Humanities Review Jurnal Aplikasi IPTEK Indonesia AHKAM : Jurnal Hukum Islam dan Humaniora Mestaka: Jurnal Pengabdian Kepada Masyarakat Journal Of Artificial Intelligence And Software Engineering Journal of Hypermedia & Technology-Enhanced Learning Jurnal Pengabdian Nusantara JKM: Jurnal Kemitraan Masyarakat Jurnal Kesehatan Masyarakat
Jasril Jasril
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Journal : VALENSI

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A Novel Benzenesulfonylurea-Substituted Pyridazinone Derivative with Antidiabetic Effect as the Peroxisome Proliferator-activated Receptor (PPAR-γ) Agonist Fatisa, Yuni; Yasthophi, Arif; Elviyenti, Elviyenti; Ikhtiaruddin, Ihsan; Frimayanti, Neni; Teruna, Hilwan Yuda; Jasril, Jasril
Jurnal Kimia Valensi Jurnal Kimia VALENSI, Volume 11, No. 1, May 2025
Publisher : Department of Chemistry, Faculty of Science and Technology Syarif Hidayatullah Jakarta State Islamic University

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.15408/jkv.v11i1.42187

Abstract

Peroxisome Proliferator-activated Receptor (PPAR-γ) protein is one of the target proteins for insulin sensitivity therapy in Type 2 DM. PPAR-γ has a key role as a nuclear receptor that regulates the expression of several metabolism-related genes. This research aims to   synthesize a novel   benzenesulfonylurea-substituted   pyridazinone     derivative, namely (E)-N'-(1-(4-(3-(4-methoxyphenyl)-6-oxopyridazin-1(6H)- yl)phenyl)ethylidene)-4-methylbenzenesulfonohydrazide (8) and predicted it activity as the PPAR-γ agonist using a molecular docking approach and ADMET profiles. The compound 8 was obtained through a Schiff base condensation reaction between compound 6, p-tosyl hydrazine, and a glacial acetic acid catalyst using monowave. The purity of the compound was determined by TLC test, and melting point measurement. The structure was confirmed through FTIR, 1H-NMR, C-NMR and HRMS analysis. Molecular docking studies were carried out on the crystal structure of the human PPAR-γ Ligand Binding Domain target protein in complex with the α-aryloxyphenyl acetic acid agonist (PDB ID 1ZEO). The results of the docking show that compound 8 has a lower binding free energy than rosiglitazone (positive control) with a free energy value (S score) = -13.513 kcal/mol and -8.3089 kcal/mol, respectively. Compound 8 can form two hydrogen bonds with residues His323 and Ser289, π-π interactions with Phe363 and π-H interactions with Cys285.  The interactions are similar to the interaction between the native ligand agonists α-aryloxyphenyl acetic acid and rosiglitazone with the target protein. Furthermore, compound 8 is predicted to have a moderate ADME profile. The results support that compound 8 can be developed as a PPAR-γ agonist candidate for the antidiabetic therapeutic agent.
Co-Authors - Aisyah - Nurlaili -, Sulismayati A, Muhammad Rizki Abdul Aziz Adel Zamri Adel Zamri Afrita, Indra agistia, nesa Ahmad Fauzan Ainil Mardiyah Aisyah Aisyah Aisyah, - Akbar, Unggul Al Fiqri, M. Faiz Alfarabi.B, Alif Ananda, Muthia Ananda, Sherly Anggita, Anggi Fisi Anori, Sartika Aprilia, Tasya Asmawati Asmawati Baehaqi Bintal Amin Christine Jose Christine Jose Dampang, Hasria Darian Alfatos Delsi K Delsi K Delsina Faiza Denai Wahyuni Denai Wahyuni Desviana, Laila Dewi, Erna Puspita Elin Haerani Elka Yuslinda Elvia Budianita Elviyenti, Elviyenti Fadhilah Syafria Fadhli, Irfan Faladhin, Johan Fauzi, Faradiba Kamilia Fawrin, Heralda Febi Yanto Fernando, Rivan Fiffah, Chainul Firmathoina, Aisyah Fitra Perdana Fitri Insani Fitria Novitasari Frischa Meivilona Yendi Guspriadi, Yan Gusti, Siska Kurnia Haiyul Fadhli Hamersat, Danu Haresman, Haresman Hariansyah, Jul Hasmalina Nasution Hendra, Rudi Hilwan Yuda Teruna Hurria, Hurria Ihsan Ikhtiarudin Iis Afrianty Ika Parma Dewi Ikhtiaruddin, Ihsan Illahi, Ridho Indah Wulandari Işık, Kenan Isnaniar Iswantir M Jufrizal Syahri Laila Desviana Lazulva Lazulva, Lazulva Lestari Handayani Lisa Utami Mar'arif, Muhammad Mulky Masykur HZ Masykur Hz Muhammad Affandes Muhammad Irsyad Muhdarina Muhdarina Muhdarina Muliani, Sarifah Muslim Syaifullah, Mhd Nazir, Alwis Nazruddin Safaat H Negara, Benny Sukma Neni Frimayanti Nofirda, Fitri Ayu Novianty, Riryn Nuraini Ramadhani Nurhayati Nurlaili Nurlaili Nurlaili, - Nurwijayanti Oktavia, Lola Perdana , Fitra Pranata, Joni Prasetya Prasetya, Prasetya Putra, Ade Herdian Putra, Rido Putri, Atika Putri, Rahmayani Indah Rahayu, Anggi Putri Rahma Dona Rahmadini Syafri Rahmiwati Hilma Ramadhani, Eka Ramadhani, Siti Ramadhanti, Aulia Rizki Retno Hidayati Rudi Hendra Sardi, Hajra Sari, Meidita Kemala Sari, Nila Puspita Silvera Devy Siregar, Alfi Salimah Siregar, Sri Hilma Siregar, srihilma Soeci Izzati Adlya Sofyan Husein Siregar Sulismayati - Surya Agustian Suwanto Sanjaya Sya'ban, Andrian Nur Thamrin Tri Windarti Tri Windarti Tria Harlianti Triana, Yeni Umar Hamdan, Umar Veithzal Rivai Zainal Wan, Xue Wenni, Osriza Wulan Sari, Wulan Yasthophi, Arif Yeni, Wila Mutiara Yuana Nurulita Yuca, Verlanda Yuharmen - Yum Eryanti Yuni Fatisa Zadrian Ardi Zahra, Fadhila Az Zahri, Firman Zikra, Nadila `Nasution, Hasmalina