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. Characterization of the compounds were subsequently carried out by UV, FTIR, 1 H-NMR, 13 C-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)-4benzylpiperidine 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.
ABSTRAKTujuan penelitian ini adalah untuk mengetahui pengaruh penggunaan campuran bahan organik dan tanah mineral sebagai media sapih terhadap pertumbuhan dan indeks mutu bibit mindi. Penelitian dilakukan di Balai Penelitian Kehutanan Ciamis pada bulan Juni 2008 s/d Januari 2009. Rancangan yang digunakan dalam penelitian ini adalah CRD (Complete Random Design) dengan tujuh perlakuan yaitu C1 (tanah + pupuk kandang (3:1)), C2 (tanah), C3 (tanah + pupuk kandang + sekam padi (1:1:1)), C4 (tanah + pupuk kandang + pasir (1:1:1)), C5(tanah + pupuk kandang + serbuk sabut kelapa (1:1:1)), C6 ((tanah + pupuk kandang + serutan kayu gergajian (1:1:1)) dan C7 ( tanah + pupuk kandang + abu sekam padi (1:1:1)). Hasil penelitian menujukkan bahwa tujuh media yang diujikan berpengaruh nyata terhadap pertumbuhan diameter, tinggi, berat kering total dan indeks mutu bibit mindi. Pertumbuhan tinggi dan diameter bibit mindi dengan media C1 (41,175 cm/0,305 cm) dan C4 (37,789 cm/0,326 cm) yang berbeda nyata lebih baik dibanding media lainnya. Berat kering total bibit mindi pada media C1 (2,189 gram) dan C4 (2,785 gram) yang relatif lebih baik meskipun tidak berbeda nyata dengan media C3 (2,123 gram), C5 (2,067 gram) dan C7 (2,140 gram). Indeks mutu bibit dengan media C3 (0,033) yang relatif lebih baik tetapi tidak berbeda nyata dengan C1 (0,026), C4 (0,025) dan C7 (0,031).Kata kunci : Bahan organik, indeks mutu bibit dan Melia azedarach L.
Tujuan penelitian ini adalah melakukan sintesis senyawa propan-2-il-tetradekanoat dari asam miristat dan 2-propanol dengan katalis asam sulfat pekat. Ada dua metode yang digunakan yaitu metode konvensional dan kombinasi melalui iradiasi gelombang mikro. Hasil penelitian ini menunjukkan bahwa metode iradiasi gelombang mikro memberikan persentase produk yang lebih baik (85%) dibandingkan dengan metode konvensional (64%). Uji kemurnian hasil sintesis menggunakan KLT dengan berbagai fase gerak menunjukkan keberhasilan baik metode konvensional maupun iradiasi gelombang mikro dalam menghasilkan senyawa produk. Senyawa propan-2-il tetradekanoat yang diperoleh kemudian dikarakterisasi sifat fisikanya dan diperoleh data antara lain titik didih = 237-240°C (210 mmHg); indeks bias (nD) = 1,4353 (20°C) ; densitas = 0,8518 (25°C). Data karakterisasi struktur menggunakan IR dan NMR juga berhasil mengonfirmasi terbentuknya senyawa propan-2-il tetradekanoat yang ditunjukkan dengan adanya gugus fungsi ester serta total proton beserta lingkungan kimianya.
N-Benzolamoxicillin and N-3,4-dichlorobenzolamoxicillin were synthesized from amoxicillin by acylation with benzoylchloride and 3,4-dichlorobenzoylchloride respectively. Structure characterization of the amoxicillin derivative compounds were done by UV, IR and 1H-NMR spectroscopy. Both derivative compound has antibacterial antivity against Staphylococcus aureus and Escherichia coli. The activity of N-3,4-dichlorobenzolamoxicillin is more active than N-Benzolamoxicillin.
2-Hydroxy-N′-(4-fluorobenzoyl)benzohydrazide was synthesized in two steps using methyl salicylate as the starting material. The reaction took place via microwave-aided hydrazinolysis, followed by acylation using 4-fluorobenzoyl chloride at low temperature to yield the target compound.
To find new compounds acting on central nervous system (CNS), this research has been done the synthesis of benzoylthiourea by acylating the thiourea with benzoyl chloride, using tetrahydrofuran as solvent. Reaction temperature were respectively done at 90oC, 100oC, 110oC and 120oC, and heating duration was respectively accomplished at 0.5 hours, 1.0 hours, 1.5 hours, 2.0 hours and 2.5 hours. This research was aimed at finding out optimal heating duration and temperature to obtain maximal percentage yield of benzoylthiourea synthesis. The highest percentage yield of 59.89% obtained in optimum temperature 100oC and 2.0 hours heating duration. The purity test of the synthesis product is shown by the single spot on the thin layer chromatogram (TLC) and narrow range of melting point. Based on the structure identification with UV and IR spectrophotometries, H-NMR spectrometries and Gas Chromatography- Mass Spectrometries (GC-MS), it was concluded that the structure of the synthesis product was accordance to the prediction.
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