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HUBUNGAN STRUKTUR TURUNAN N-KLOROBENZOILAMOKSISILIN DAN AKTIVITAS ANTIBAKTERINYA TERHADAP Pseudomonas aeruginosa ATCC 27853 Kusumowati, Ika Trisharyanti Dian; Siswandono, .; Rudyanto, Marcellino
JFIOnline | Print ISSN 1412-1107 | e-ISSN 2355-696X Vol 5, No 3 (2011)
Publisher : Indonesian Research Gateway

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Abstract

The aim of this research is to determine structure-activity relationship N-chlorobenzoylamoxicillin derivatives against Pseudomonas aeruginosa ATCC 27853. Antibacterial activities of the N-benzoylamoxicillin­ derivatives against Pseudomonas aeruginosa ATCC 27853 were tested using dilution method. The result showed that there was significance MIC of amoxycillin with N-benzoylamoxycillin, N-2-chlorobenzoylamoxycillin, and N-3-chlorobenzoylamoxycillin. Non linier regression between log MIC and lypophilic parameter N-chlorobenzoylamoxycillin derivatives showed -log KHM = 3,963 p2 - 3,001 p - 2,477, r = 0,906. To see more clearly quantitative strucuture-activity relationship of N-benzoylamoxicillin derivatives, further similar studies need to be done by increasing numbers of another N-benzoylamoxicillin derivative compounds.  ABSTRAK Penelitian ini bertujuan mengetahui hubungan struktur-aktivitas antibakteri senyawa-senyawa turunan N-kolorobenzoilamoksisilin terhadap Pseudomonas aeruginosa ATCC 27853. Uji aktivitas antibakteri turunan senyawa N-klorobenzoilamoksisilin terhadap Pseudomonas aeruginosa ATCC 27853 dilakukan dengan metode dilusi. Nilai KHM menunjukkan adanya perbedaan aktivitas yang bermakna antara amoksisilin dengan N-benzoilamoksisilin, N-2-klorobenzoilamoksisilin, dan N-3-klorobenzoilamoksisilin. Persamaan non linier log KHM dengan sifat lipofilik senyawa turunan N-klorobenzoilamoksisilin diperoleh -log KHM = 3,963 p2 - 3,001 p - 2,477, dengan harga r = 0,906.
HUBUNGAN STRUKTUR TURUNAN N-KLOROBENZOILAMOKSISILIN DAN AKTIVITAS ANTIBAKTERINYA TERHADAP Pseudomonas aeruginosa ATCC 27853 Kusumowati, Ika Trisharyanti Dian; Siswandono, .; Rudyanto, Marcellino
Jurnal Farmasi Indonesia Vol 5, No 3 (2011)
Publisher : Jurnal Farmasi Indonesia

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.35617/jfi.v5i3.49

Abstract

The aim of this research is to determine structure-activity relationship N-chlorobenzoylamoxicillin derivatives against Pseudomonas aeruginosa ATCC 27853. Antibacterial activities of the N-benzoylamoxicillin­ derivatives against Pseudomonas aeruginosa ATCC 27853 were tested using dilution method. The result showed that there was significance MIC of amoxycillin with N-benzoylamoxycillin, N-2-chlorobenzoylamoxycillin, and N-3-chlorobenzoylamoxycillin. Non linier regression between log MIC and lypophilic parameter N-chlorobenzoylamoxycillin derivatives showed -log KHM = 3,963 p2 - 3,001 p - 2,477, r = 0,906. To see more clearly quantitative strucuture-activity relationship of N-benzoylamoxicillin derivatives, further similar studies need to be done by increasing numbers of another N-benzoylamoxicillin derivative compounds.  ABSTRAK Penelitian ini bertujuan mengetahui hubungan struktur-aktivitas antibakteri senyawa-senyawa turunan N-kolorobenzoilamoksisilin terhadap Pseudomonas aeruginosa ATCC 27853. Uji aktivitas antibakteri turunan senyawa N-klorobenzoilamoksisilin terhadap Pseudomonas aeruginosa ATCC 27853 dilakukan dengan metode dilusi. Nilai KHM menunjukkan adanya perbedaan aktivitas yang bermakna antara amoksisilin dengan N-benzoilamoksisilin, N-2-klorobenzoilamoksisilin, dan N-3-klorobenzoilamoksisilin. Persamaan non linier log KHM dengan sifat lipofilik senyawa turunan N-klorobenzoilamoksisilin diperoleh -log KHM = 3,963 p2 - 3,001 p - 2,477, dengan harga r = 0,906.
Sintesis O-(Isoleusil) Parasetamol dan Uji Aktivitas Analgesik terhadap Mencit (Mus musculus) dengan Metode Hot Plate Parwitha, Ida Ayu Andri; Siswodihardjo, Siswandono
Jurnal Farmasi Sains dan Terapan Vol 7, No 2 (2020): Oktober
Publisher : Jurnal Farmasi Sains dan Terapan

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.33508/jfst.v7i2.2676

Abstract

Parasetamol merupakan obat analgesik lini pertama yang digunakan dalam tata laksana nyeri. Penggunaan obat tersebut dalam jangka waktu panjang dengan dosis besar berpotensi memunculkan efek samping hepatotoksik. Guna meminimalkan efek samping dan meningkatkan aktivitas analgesik dari Parasetamol maka dilakukan modifikasi struktur –OH pada gugus parasetamol. Tujuan dari penelitian ini adalah mensintesis senyawa O-(isoleusil)parasetamol melalui reaksi Schotten Baumann antara Parasetamol dan Isoleusil klorida. Senyawa sintesis tersebut diuji aktivitas analgesiknya pada Mencit. Pemurnian senyawa hasil sintesis melalui proses rekristalisasi menggunakan campuran pelarut etanol:air (1:2) dan diperoleh senyawa berbentuk serbuk berbau menyengat dengan rendemen hasil 32%. Setelah senyawa terbukti murni maka dilanjutkan dengan identifikasi struktur senyawa menggunakan spektrofotometer inframerah dan spektrometer 1H-NMR. Hasil uji menunjukkan bahwa senyawa hasil síntesis sesuai yang diharapkan. Pengujian aktivitas analgesik senyawa dilaksanakan pada Mencit (Mus musculus) dengan metode hot plate. Dosis yang digunakan dalam penelitian ini adalah 12,5; 25; 50; 100; 200 mg/kg BB diberikan secara intraperitoneal dan parasetamol dengan dosis sama sebagai senyawa pembanding. Hasil penelitian menunjukkan nilai ED50 O-(isoleusil) parasetamol 50 mg/kg BB dan ED50 parasetamol adalah 66 mg/kg BB. Berdasarkan nilai ED50 dapat disimpulkan bahwa O-(isoleusil)parasetamol memiliki aktivitas analgesik yang lebih tinggi dibanding parasetamol. Hasil uji statistik Tukey HSD menunjukkan bahwa aktivitas analgesik parasetamol dan O-(isoleusil)parasetamol tidak berbeda bermakna.
Evaluation of N-benzoylthiourea derivatives as possible analgesic agents by predicting their physicochemical and pharmacokinetic properties, toxicity, and analgesic activity Suko Hardjono; Siswandono Siswandono; Rina Andayani
Indonesian Journal of Biotechnology Vol 22, No 2 (2017)
Publisher : Universitas Gadjah Mada

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (708.701 KB) | DOI: 10.22146/ijbiotech.27171

Abstract

This study aimed to predict the physicochemical properties, pharmacokinetic properties (ADME), toxicity, and analgesic activity of 30 compounds of N-benzoylthiourea derivatives that are potential analgesic drugs. One of the mechanisms of action of N-benzoylthiourea derivatives is the inhibition of the cyclooxygenase-2 (COX-2) isoenzyme. An in silico test was performed by docking a compound that would predict its activity with the target COX-2 isoenzyme, PDB ID: 1PXX, using the MVD (Molegro Virtual Docker) program. The result of the docking was a form of energy bond indicated by the value of the rerank score (RS), where compounds that had lower RS values were predicted to have a higher activity. The pkCSM and Protox online tools were used to predict various physicochemical properties. Based on the RS values, the N-benzoylthiourea derivatives can be predicted to have lower analgesic activity than diclofenac, the reference ligand. Three of the N-benzoylthiourea derivatives—N-(2,4-bis-trifluoromethyl)-benzoylthiourea, N-(3,5-bis-trifluoromethyl)benzoylthiourea, and N-(3-trifluoromethoxy)-benzoylthiourea—had RS values of -90.82, -94.73, and -92.76,  respectively, suggesting that these compounds were predicted to have analgesic activity relatively similar to diclofenac (RS value = -95.16). Furthermore, the majority of the  N-benzoylthiourea derivatives were predicted to have good pharmacokinetic properties (ADME), and cause relatively low toxicity.
Introducing a two‐dimensional graph of docking score difference vs. similarity of ligand‐receptor interactions Mohammad Rizki Fadhil Pratama; Hadi Poerwono; Siswandono Siswodihardjo
Indonesian Journal of Biotechnology Vol 26, No 1 (2021)
Publisher : Universitas Gadjah Mada

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.22146/ijbiotech.62194

Abstract

Observation of molecular docking results was generally performed by analyzing the docking score and the interacting amino acid residues separately either in tables or graphs. Sometimes it was not easy to rank the tested ligands’ docking results, especially if there were many ligands. This study aims to introduce a new way to analyze docking results with a two‐dimensional graph between the difference in docking score and the similarity of ligand‐receptor interactions. Molecular docking was performed with one reference ligand and several test ligands. The docking score difference was obtained between the test and the reference ligands as the graph’s x‐axis. Meanwhile, the y‐axis contains the similarity of ligand‐receptor interactions, obtained from the ratio of amino acid residues and the types of interactions between the test and reference ligands. Docking result analysis was more straightforward because two critical parameters were presented in one graph. This graph could be used to support the analysis of the docking results.
Sintesis dan Uji Aktivitas Senyawa 1-Benzil-3-benzoilurea Tersubstitusi Bromo, Kloro, Floro dan Triflorometil pada posisi para sebagai Agen Antiproliferatif Farida Suhud; Siswandono Siswandono; Tutuk Budiati
MPI (Media Pharmaceutica Indonesiana) Vol. 1 No. 3 (2017): JUNE
Publisher : Fakultas Farmasi, Universitas Surabaya

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (745.845 KB) | DOI: 10.24123/mpi.v1i3.266

Abstract

Sintesis dan uji aktivitas 1-benzil-3-benzoilurea tersubstitusi F, Cl, Br dan CF3 pada posisipara sebagai agen antiproliferatif telah dilakukan. Tujuan dari studi ini untuk membandingkanaktivitas sebagai agen antiproliferatif senyawa 1-benzil-3-benzoilurea dengan substituen golonganhalogen. Untuk mencapai tujuan tersebut uji aktivitas secara in-silico terhadap reseptor 1-UWH diprediksidengan Molegro Virtual Docker (MVD) 5 dan hidroksiurea digunakan sebagai pembanding.Selanjutnya uji aktivitas secara in-vitro terhadap kultur sel MCF-7 dilakukan dengan MTT-assay. Hasildidapatkan senyawa 1-benzil-3-(4-CF3-benzoil)urea lebih poten dibandingkan yang lain. Sangatdirekomendasikan untuk dilakukan prediksi bioavailabilitas dan toksisitas serta uji lebih lanjut senyawa1-benzil-3-(4 CF3-benzoil)urea sebagai calon obat dengan aktivitas antiproliferatif.
Identification of Physical Interaction in Binary Systems of Acyclovir – Succinic Acid Agnes Nuniek Winanta; Dwi Setyawan; Siswandono Siswandono
JURNAL FARMASI DAN ILMU KEFARMASIAN INDONESIA Vol. 3 No. 1 (2016): Jurnal Farmasi dan Ilmu Kefarmasian Indonesia
Publisher : Universitas Airlangga

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (94.891 KB) | DOI: 10.20473/jfiki.v3i12016.27-31

Abstract

Background: Acyclovir, a guanosine analogue antiviral drug with low solubility of water. Due to its poor solubility and permeability, causes low oral bioavailability. Objective: The aim of this research is to investigate the physical interaction in binary systems acyclovir-succinic acid (AS). Methods: The msystem was prepared by solvent evaporation method. Results: Thermogram Differential Scanning Calorimetry showed endothermic peaks at 172.68oC (ethanol) and 171.84oC (methanol). The Powder X-Ray Diffraction (PXRD) pattern of AS was different from pure component and physical mixtures. Furthermore, physical characterization showed the binary system of AS have unique crystal habit by polarization microscope. Conclusion: New crystalline phase is formed from the interaction between acyclovir and succinic acid by solvent evaporation method using ethanol and methanol.  
Synthesis and Activity Test of 1-Allyl-3-(4-tertiary-Butylbenzoyl) Thioureaas a Candidate of an Analgesic Drug Rais Razak; Siswandono Siswandono; Juni Ekowati
JURNAL FARMASI DAN ILMU KEFARMASIAN INDONESIA Vol. 9 No. 1 (2022): JURNAL FARMASI DAN ILMU KEFARMASIAN INDONESIA
Publisher : Universitas Airlangga

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.20473/jfiki.v9i12022.17-23

Abstract

Background: Urea derivatives showed good analgesic activity compared to diclofenac sodium.  The addition of the allyl group to the thiourea and 4-tertiary-butylbenzoyl chlorideis expected to provide a better analgesic effect. Objective: The research aimed to synthesize 1-allyl-3-(4-tertiary-Butylbenzoyl) Thiourea and determine its analgesic activity in mice (Mus musculus). Methods: The synthesis was carried out by a modified Schotten-Baumann reaction, via nucleophilic substitution reaction of allylthiourea on 4-tertiary-butylbenzoyl chloride.  A writhing test was performed to observe analgesic activity in the test compound.  Confirmation of the structure of pure 1-allyl-3-(4-tertiary-Butylbenzoyl) Thiourea was obtained through UV, IR, 1H-NMR, and 13C-NMR data. Results: The compound showed better pain inhibition activity compared to diclofenac sodium, with ED5019,018 mg/kg BW. Conclusion: The compound 1-allyl-3-(4-tertiary-butylbenzoyl) thiourea showed better analgesic activity than diclofenac sodium.
Phase Diagram and Thermodynamic Properties of Ketoprofen-Succinic Acid Binary Mixtures Yudi Wicaksono; Dwi Setyawan; S. Siswandono
Jurnal ILMU DASAR Vol 19 No 2 (2018)
Publisher : Fakultas Matematika dan Ilmu Pengetahuan Alam Universitas Jember

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (373.972 KB) | DOI: 10.19184/jid.v19i2.5521

Abstract

The equilibrium phase diagram and thermodynamic properties of a mixture of drugs and additives are information related to various possible interaction processes between components. Therefore, we conducted a study of the phase diagrams and thermodynamic properties of binary mixtures of ketoprofen-succinic acid to estimate the types of interactions that may occur between these materials. The solid-liquid phase diagram of ketoprofen-succinic acid binary mixtures was determined by differential scanning calorimetry and composition of eutectic system was determined accurately using a Tamman diagram. The measurement of binary mixtures of ketoprofen-succinic acid with differential scanning calorimeter obtained the value of melting temperature and heat of fusion of ketoprofen- succinic acid system. The solid-liquid phase diagram of ketoprofen- succinic acid showed the formation of eutectic type phase diagram. The Tamman diagram showed accurately composition of the eutectic system of the Kp-SA binary mixtures at the mole fraction of Kp 0.87 and temperature 96.9oC.Keywords: ketoprofen, phase diagram, eutectic system, Tamman diagram
REVITALISASI USAHA KECIL MENENGAH DHARMA BOGA BOJONEGORO MELALUI PELATIHAN CARA PRODUKSI DAN REGISTRASI PANGAN YANG BAIK SERTA HALAL Isnaeni; Noor Erma Nasution; Sugijanto; Hadi Poerwono; Juni Ekowati; Siswandono; Marcellino Rudyanto; Kholis Amalia Nofianti; Achmad Syahrani; Suzana
Panrita Abdi - Jurnal Pengabdian pada Masyarakat Vol. 5 No. 2 (2021): Jurnal Panrita Abdi - April 2021
Publisher : LP2M Universitas Hasanuddin

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.20956/pa.v5i2.5754

Abstract

Abstract. The independence of food supply in Indonesia is supported by the abundant diversity of natural ingredients from vegetable, animal and mineral sources. Compared to drugs, dependence on food products in other countries is relatively lower, because the fabrication requires facilities and infrastructure that can be fulfilled domestically. The regulatory system managed by the Republic of Indonesia Drug and Food Control Agency (BPOM-RI) has been implemented to ensure that food products consumed by the public are of high quality, nutritious, safe, halal, and affordable and with a taste that satisfies user communities. Circular-worthy products must at least meet the registration requirements of halal aspects, maximum microbial limits and chemical contamination. The growth of Micro, Small and Medium Enterprises (MSMEs) is also facilitated by the government. Dharma Boga is one of the Small and Medium Enterprises (UKM) in Klangon sub-district, Bojonegoro which is engaged in food production for more than 10 years. Some problems related to registration, halal certification and handling of production, especially food additives that meet requirements, has been communicated to the Community Service Team (PENMAS) Faculty of Pharmacy, Airlangga University (FFUA). Alhamdulillah, PENMAS activities with training materials on how to produce and register good and halal food have been carried out with satisfactory results, although it still needs to be followed up with a partnership for the MSME revitalization program in the future. Of the three parameters used to measure participants' understanding of training material, the average obtained more than 30% showed an increase. For the introduction of the halal logo and the dangers of formaldehyde, 100% of the message is understood. The training involved experts and stakeholders in the authority of the East Java Indonesian Ulama Council and the teaching staff and the Airlangga University Faculty of Pharmacy Testing Service Unit.         Abstrak. Kemandirian penyediaan pangan di Indonesia didukung oleh diversitas bahan alam yang melimpah baik dari sumber nabati, hewani, maupun mineral. Dibandingkan obat, ketergantungan produk pangan pada negara lain relatif lebih rendah, karena fabrikasinya membutuhkan fasilitas dan infrastruktur yang dapat terpenuhi di dalam negeri. Sistem regulasi yang dikelola oleh Badan Pengawas Obat dan Makanan Republik Indonesia (BPOM-RI) telah diberlakukan untuk menjamin produk makanan yang dikonsumsi masyarakat berkualitas, bergizi, aman, halal, dan terjangkau serta dengan rasa yang memuaskan selera masyarakat. Produk yang laik edar minimal harus memenuhi persyaratan registrasi dari aspek halal, batas maksimum mikroba dan cemaran bahan kimia. Tumbuh kembangnya Usaha Mikro, Kecil dan Menengah (UMKM) juga difasilitasi oleh pemerintah. Dharma Boga adalah salah satu Usaha Kecil Menengah (UKM) di kecamatan Klangon, Bojonegoro yang bergerak dibidang produksi makanan selama lebih dari 10 tahun. Beberapa permasalahan terkait registrasi, sertifikasi halal dan penanganan produksi terutama bahan tambahan makanan yang memenuhi persyaratan, telah dikomunikasikan kepada Tim Pengabdian kepada Masyarakat (PENMAS) Fakultas Farmasi Univeritas Airlangga (FFUA). Alhamdulillah kegiatan PENMAS dengan materi pelatihan cara produksi dan registrasi pangan yang baik serta halal telah dilaksanakan dengan hasil yang memuaskan, walaupun masih perlu ditindaklanjuti dengan jalinan kerjasama untuk program revitalisasi UMKM di masa mendatang. Dari tiga parameter yang digunakan untuk mengukur pemahaman peserta terhadap materi pelatihan, rerata yang diperoleh lebih dari 30% menunjukkan peningkatan. Untuk pengenalan logo halal dan bahaya formalin, 100% peserta sudah paham. Pelatihan melibatkan pakar dan pemangku kewenangan dari Majelis Ulama Indonesia Jawa Timur dan para staf pengajar serta Unit Layanan Pengujian Fakultas Farmasi Universitas Airlangga.