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All Journal Jurnal Farmasi Sains dan Terapan (Journal of Pharmacy Science and Practice) Indonesian Journal of Cancer Chemoprevention MPI (Media Pharmaceutica Indonesiana) INDONESIAN JOURNAL OF PHARMACY JURNAL FARMASI DAN ILMU KEFARMASIAN INDONESIA Indonesian Journal of Chemistry Berkala Ilmiah Kimia Farmasi Berkala Penelitian Hayati Pharmaceutical Sciences and Research (PSR) Jurnal Farmasi Sains dan Terapan (Journal of Pharmacy Science and Practice)
Tutuk Budiati
Department Of Pharmaceutical Chemistry, Faculty Of Pharmacy Universitas Airlangga, Surabaya
Agriculture, Biological Sciences & Forestry Biochemistry, Genetics & Molecular Biology Chemical Engineering, Chemistry & Bioengineering Chemistry Education Health Professions Immunology & microbiology Materials Science & Nanotechnology Medicine & Pharmacology Other

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Journal : INDONESIAN JOURNAL OF PHARMACY

 1 
Synthesis and Molecular Docking Studies of N’-benzoylsalicylhydrazide derivatives as antituberculosis through InHA enzym inhibition Harry Santosa; Galih Satrio Putra; Tegar Achsendo Yuniarta; Tutuk Budiati
Indonesian Journal of Pharmacy Vol 29 No 4, 2018
Publisher : Faculty of Pharmacy Universitas Gadjah Mada, Yogyakarta, Skip Utara, 55281, Indonesia

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (1120.908 KB) | DOI: 10.14499/indonesianjpharm29iss4pp198

Abstract

The specific aims of this study is to synthesize and to study the possible mechanism of N’-benzoylsalicylhydrazide derivatives as an antituberculosis agent through InhA (Enoyl acyl carrier protein reductase) inhibition using in silico method. Five analogues of N’-benzoylsalicylhydrazide were synthesized using microwave irradiation from methyl salicylate as starting material, which yielded 80-90% product on average. This indicates a considerable improvement in terms of effectivity and efficiency, compared to the more conventional method using reflux condition. Character-ization of the compounds were subsequently carried out by UV, FTIR, 1H-NMR, 13C-NMR spectroscopy, which confirmed that the compounds had been successfully synthesized. Ultimately, molecular docking was performed using Molegro Virtual Docker (MVD) on the active site of InhA enzyme to predict the activity of the compounds. The results showed that all compounds performed comparatively well against N-(4-Methylbenzoyl)-4-benzylpiperidine as the native ligand and also yielded lower docking score than isoniazide (INH). From this study it can be concluded that N’-benzoylsalicylhydrazide derivatives could be synthesized using microwave irradiation with good product yield and all of the synthesized analogues are suggested to possess antituberculosis activity via InhA enzyme inhibition. In vitro activity will have to be determined in the future to validate whether N’-benzoylsalicylhydrazide derivatives perform well as a potential antituberculosis agent.
Synthesis, analgesic and anti-inflammatory activities of substituted benzoylthioureas Tutuk Budiati; Suzana .; Siti Surdijati
Indonesian Journal of Pharmacy Vol 21 No 1, 2010
Publisher : Faculty of Pharmacy Universitas Gadjah Mada, Yogyakarta, Skip Utara, 55281, Indonesia

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (261.607 KB) | DOI: 10.14499/indonesianjpharm0iss0pp68-76

Abstract

Three compounds (i.e.  benzoylthiourea,  4-nitrobenzoylthiourea,  and  4-chlorobenzoylthiourea) have  been  synthesized  from  ammonium  thiocyanate, substituted benzoyl chlorides, and ammonia as starting materials. The structures of  sythesized  compounds  were  confirmed  by  means  of  ultra-violet,  infrared, magnetic resonance, and mass spectroscopy. All compounds were evaluated for their  analgesic  and  anti-inflamatory  activities  by  tail-flick  technique  and carragenan-induced  paw  oedema  test  respectively.  Substitution of p-NO2 and p-Cl  group  to  benzoylthiourea  increased  the  analgesic  and  anti-inflamatory activities.  The  two  compounds,  4-nitrobenzoylthiourea  and  4-chlorobenzoylthiourea,  were  significantly  more  potent  as  analgesic  but  their  antiinflamatory actvity was weaker than Na-diclofenac.Keywords: benzoylthioureas, p-Cl dan p-NO2substituents, analgesic and anti-inflamator activities
Co-Authors Adam Hermawan Aline Puspita Kusumadjaja Anita Puspa Widiyana Ardhayanti, Erlina Caroline Catherine Caroline Edy Meiyanto Edy Meiyanto Elisabeth Catherina Widjajakusuma Farida Suhud Galih Satrio Putra Galih Satrio Putra Harry Santosa Ivonne Soeliono Jessica Jessica Jessica, Maria Anabella Juni Ekowati Kholis Amalia Nofianti Luthfi Ahmad Muchlashi Marcellino Rudyanto Melanny Ika Sulistyowaty Mellany Ika Sulistyowaty Ni Nyoman Tri Puspaningsih Nunuk Irawati Nunuk Irawati Putri, Navyanti Firda Sajidan Shigeru Sasaki Shigeru Sasaki Siswandono, Siswandono Siti Surdijati Soewandi, Ami Stephanie D.A. Sukardiman Suzana SUZANA, SUZANA Tegar Achsendo Yuniarta Wahyu Dewi Tamayanti, Wahyu Dewi