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.
Synthesis octyl p-methoxycinnamate substance as sunblock, has been done by transesterification reaction. The starting material of the reaction was ethyl pmethoxycinnamate isolated from Kaempferia galanga L.The transesterification reaction was carried out by reacting ethyl p-methoxycinnamate with octanol. The product was identified by UV-VIS, Infra Red and Mass Spectroscopy. The result of measurements on erythemic %T at various concentrations demonstrate that octyl p-methoxycinnamate is applicable as a sunblock compound.
Ethyl p-methoxycinnamate, major ingredient of Kaempferia galanga rhizome, have been reported not only has analgesic -anti inflammatory activities like NSAIDs which inhibited cyclooxygenase, but also inhibit tumor cell proliferation in specimen of mouse epidermis. Therefore, it will be interesting to carry out synthetic studies on the derivates of ethyl pmethoxycinnamate and searching their citotoxic activity on WiDr cell. We wish to report of structure modification on carboxyl moiety of ethyl p-methoxycinnamate and evaluation on their citotoxic activity on WiDr cell. Isolation of ethyl p-methoxycinnamate from Kaempferia galanga rhizome was carried out by percolation with ethanol 96% as solvent. Hydrolysis of ethyl p-methoxycinnamate in basic condition was performed to obtain p-methoxycinnamic acid. Preparation of some thiourea derivates of ethyl p-methoxycinnamate was carried out by microwave irradiation. Citotoxicity assay was carried out by MTT method for 48 h.Modification of carboxyl group of ethyl p-methoxycinnamate to its thiourea form could be carried out by microwave irradiation gave; (E)-3-(4-methoxyphenyl)-N-(phenylcarbamothioyl)acrylamide (50%); (E)-3-(4-methoxyphenyl)-N-(4-methoxyphenylcarbamothioyl)acrylamide (26%) and (E)-3-(4-methoxyphenyl)-N-(4-methylphenylcarbamothioyl) acrylamide (54%), yield calculated for 2 step from the acid chloride. All compounds showed no citotoxic effect on WiDr cell at 48 h incubation.
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.
Phytase is enzyme which hydrolysis phytic acid to anorganic phosphate and myo-inositol pentakis-, tetrakis-, tris-, bis-, and monophosphate. The use of phytase in feed industry can overcome environment and nutrition problems which were arisen from unmetabolism phytic acid or its salt by poultry, swine and fish. The feed industry needs a thermostable enzyme due to the need of high temperature in pelleting process, i.e. 81 °C. By using thermostabile phytase, the pelleting process will not affect the enzyme activity. Thermostabile phytase can be isolated from microorganism live in hot spring water or volcano crater. In this study, the screening of thermophylic microorganism having thermostabile phytase activity in Ijen Crater, Banyuwangi, has been done. From this process, it was obtained 33 isolates that produce phytase enzyme. Isolate was code by AP-17 yields highest phytase activity, that is 0.0296 U/mL, so this isolate was choosen for further study. The activity of crude phytase enzyme was measured based on the amount of anorganic phosphate that was produced in enzymatic reaction using UV-VIS spectrophotometer at 392 nm. Based on morphology test to identify the gram type of microorganism, isolate AP-17 has a bacill cell type and identified as positive gram bacteria. This isolate was assumed as Bacillus type. Keywords: Phytase, thermophilic microorganism, phytase activity
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