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Identification of Novel Compounds with Anti-Mycobacterial Activity Using in Silico Screening and Pharmacophore Modeling Targeting Mycobacterium Thymidine Monophosphate Kinase
Get PDF九州工業大学博士学位論文 学位記番号:情工博甲第298号 学位授与年月日:平成27年3月25日1. Introduction||2. Results||3. Discussion||4. Conclusion||5. Materials and methodsThe increasing prevalence of drug-resistant tuberculosis (TB), which is resistant to effective multiple antibiotic, remains a major public health menace. The Mycobacterium tuberculosis (M. tuberculosis) thymidine monophosphate kinase (mtTMPK), which is an essential enzyme for the maintenance of the thymidine triphosphate pools, is considered a potential enzymatic target for the development of effective antibiotics against TB. In this study, I attempted to identify novel compounds with anti-mycobacterial activity specifically targeting mtTMPK. I performed in silico structure-based drug screening (SBDS) with a large-scale virtual compound library (6,192,932 compounds) and phramacophore-based in silico screening with a compound library of 461,383 compounds. I then evaluated the inhibitory effects of candidate compounds on model mycobacteria strains. As a result, I found that compounds K10, KTP3, KTPS1, and KTPS2, completely inhibited the growth of Mycobacterium vanbaalenii (M. vanbaalenii) and/or Mycobacterium smegmatis (M. smegmatis). In addition, I experimentally demonstrated that two compounds (KTPS1 and KTPS2) directly inhibited
mtTMPK catalytic activity to some extent. Moreover, the most potent chemical compounds, KTPS1, did not exhibit any significant toxic effects on the growth of model intestinal bacteria (Escheichila coli: E. coli) and several mammalian cells. The structural and experimental information regarding these chemical compounds is likely useful for the development of novel antibiotics for the treatment of TB
地域と世界的気候様相を組み合わせた集中豪雨予想法とそのマレーシア地方への適応
No full text九州工業大学博士学位論文 学位記番号:情工博甲第297号 学位授与年月日:平成27年3月25日1 Introduction||2 Literature Review||3 Methodology of the study||4 Data and application of methods||5 Results and discussions||6 ConclusionSuccessive days of precipitation are known to cause flooding in monsoon-susceptible countries.
The analysis of extreme precipitation trends is important for the prediction of high precipitation events. Forecasting of daily precipitation facilitates the prediction of the occurrences of rainfall and number of wet days. Using the maximum five-day accumulated precipitation (MX5d) index, we can predict the magnitude of precipitation in a specific period as it may indicate the extreme precipitation.
Traditionally, a data-driven model is built on a whole data set describing the phenomenon within the data. This type of model does not considered the seasonal processes embedded in the data.
Therefore, there is a need to built a model that encompassing different time scale and localized.
One of the ways of doing this is to discover the different physically embedded relationships in precipitation process at different seasonal period and to built separate localized models for each of these seasonal periods. The use of committee models such as modular and ensemble models in weather and hydrological forecasting are increasing day by day. The study uses the modular concept by separating the heavy precipitation events based on sub-processes which are the seasonal monsoon and trained the subset of seasonal data using data driven models.
Besides that, the study is carried out to evaluate the influence of global climate indices on local precipitation. It is interesting to see the influence of combining global and local predictors on local precipitation events. The method used past MX5d data and global climate indices such as Southern Oscillation Index (SOI), Madden Julian Oscillation (MJO), and Dipole Mode Index (DMI) in Kuantan and Kota Bharu, Malaysia using modular model trained on subset of data that represent the seasonal monsoon.
The analysis started with evaluating the local and global inputs (MX5d with SOI, MJO, and DMI) in order to investigate the concurrent effect of lagged values of local precipitation data and global climate indices on seasonal extreme precipitation. Four subset of data are sampled representing two major seasonal variations in Malaysia. The experimental data are focused on the east coast area of Malaysia such that the effect of northeast monsoon season causes heavy precipitation events. The results showed that the combination of local and global modes in a modular model is favourable than a single localized mode. The proposed modular model is promising an encouraging result when different subset of data are trained on separate methods with different parameter values
下水余剰汚泥の嫌気消化によるメタン生産と汚泥減量化を促進するための生物化学的アプローチ
No full text九州工業大学博士学位論文 学位記番号:生工博甲第235号 学位授与年月日:平成27年3月25日1. Introduction||2. Effect of azithromycin on enhancement of methane production from waste activated sludge||3. Enhancement of sludge reduction and methane production by removing extracellular polymeric substances from waste activated sludge||4. Conclusions and suggestio
Study on ensemble classifiers for event-related potential based brain computer interfaces
No full text九州工業大学博士学位論文 学位記番号:生工博甲第238号 学位授与年月日:平成27年3月25日第1章 序論||第2章 ブレイン?コンピュータ・インタフェース||第3章 ERP-based BCI の構成||第4章 オーバーラップト・パーティショニングを用いたERP-based BCI の集合識別器||第5章 結
自己燃焼化におけるアブラヤシの空果房炭化に関する研究と山仙式炭化法によるバイオチャーの製造
No full text九州工業大学博士学位論文 学位記番号:生工博甲第236号 学位授与年月日:平成27年3月25日1. Introduction and literature review||2. Temperature profiles and gaseous emission during selfsustained carbonization of opefb biomass in a pilot scale reactor (30 kg capacity).||3. The effect of exhausted gas flow rate and opefb biomass particle size on biochar yield and quality under self-sustained carbonization in a pilot scale (30 kg capacity) reactor||4. The effect of opefb biochar yield and quality in a scaled-up pool type reactor under self-sustained carbonization (3 tones capacity).||5. The effect of energy balance and potential energy saving of raw opefb and biochar in a scaled-up pool type self-sustained carbonization reactor (3 tones capacity)||6. Conclusion and remarksThe usage of OPEFB biomass as an alternative source for renewable energy such as biochar has a great potential to overcome the shortage of fossil fuel. Moreover, the utilization of biomass as a source of biofuel can reduce the problem of environmental pollution particularly on the issues related to greenhouse gases. Being the second largest oil palm producer in the world, Malaysia has a great potential to produce clean renewable energy from biomass. The selfsustained carbonization was proposed and tested in this study, whereby oil palm biomass itself was combusted to provide heat for self-carbonization in inadequate oxygen without electrical heating element. In the first chapter, the reviews on the literature pertaining Malaysia palm oil industry, current carbonization technologies, proposed self-sustained carbonization to produce biochar and the objectives of this study have been discussed.
In the second chapter, the temperature profiles and gaseous emission concentration during self-sustained carbonization of empty fruit bunch biomass in a pilot scale reactor (30 kg capacity) at different particles sizes (100-150, 30-99 and less than 29 mm) was evaluated. For self-sustained carbonization with natural exhausted gas flow rate, the maximum temperatures ranging 417-580 oC at all particle sizes were tested and found to be suitable for biochar production. The average concentration of CO2, CO and CH4 released during the carbonization process were between 2.8-4.1, 0.38-0.51 and 0.17-0.26 %, respectively. For self-sustained carbonization with fixed exhausted gas flow rate, the maximum temperatures were slightly similar when compared to self-sustained carbonization with natural exhausted gas flow rate which was between 493-564 oC at all particle size tested. The average concentration of CO2, CO and CH4 released during the carbonization process were between 3.65-5.59, 0.56-0.72 and 0.29-0.39 %, respectively. SO2 and HCl were not detected while NOx and particulate matter, (PM10) were well below permitted level set by the Department of Environment, Malaysia for both natural and fixed exhausted gas flow rate. Gaseous pollutant in this study can be considered low and the self-sustained carbonization process was environmental friendly when compared to other studies using same palm oil biomass carbonization.
In the third chapter, the effect of exhausted gas flow rate and OPEFB biomass particle sizes on biochar yield and quality in a pilot scale (30 kg capacity) reactor under self-sustained carbonization were evaluated. For self-sustained carbonization with natural exhausted gas flow rate, harvesting carbonization temperature of < 500 oC of OPEFB biomass at the particle size ranging from 100-150 mm produced the highest biochar yield and CV between 23-25 % and 22.6-24.7 MJ/kg, respectively. The carbonization retention time was between 790-893 min and less compared to other particle sizes tested. This particle size, without further size reduction, is needed to reduce the energy requirement at production line. For self-sustained carbonization temperature with fixed exhausted gas flow rate, the OPEFB biochar yield at particle size 100-150 mm produced the highest yield (25-27 %), harvested at carbonization temperature of < 500 oC compared to other particle sizes in the same condition. Moreover, this yield was also high as compared to self-sustained carbonization with natural exhausted gas flow rate. The CV were found between 23.0-24.4 MJ/kg which were also comparable with other studies. The carbonization retention time between 280-462 min were found less when compared to natural exhausted gas flow rate which contributed to high yield. More consistent result can be achieved under self-sustained carbonization temperature with fixed exhausted gas flow rate but energy required from the usage of exhaust gas blower. In this study, as the carbonization harvesting temperature decreased, the biochar yield decreases, the carbonization retention time increased.
In the fourth chapter, self-sustained carbonization of pressed-shredded and whole bunch
OPEFB in large scale pool type reactor (3000 kg) from the development of YAMASEN oven (Shimane) were successfully adopted and tested. The pressed-shredded OPEFB was found suitable to be carried out under an open carbonization system while closed carbonization system was preferable for whole bunch OPEFB. The maximum self-sustained carbonization temperature were ranged 583-695 oC for pressed-shredded and bunch OPEFB biomass. In terms of CV, large scale biochar production for open and closed system under self-sustained carbonization produced in between 21.9-24.3 and 19.6-22.9 MJ/kg, respectively which is comparable to small scale biochar production.
In the fifth chapter, the energy balance and potential energy saving of raw and biochar
OPEFB (pressed-shredded and whole bunch) in a scaled-up pool type self-sustained carbonization reactor (3 tones capacity) was evaluated. The ratio energy output/input for pressedshredded biochar, whole bunch biochar and raw pressed-shredded OPEFB briquette were positive which were 12, 15 and 8 respectively. Whole bunch biochar is still the highest ratio energy output/input biochar production although without pressed-shredder machine process step resulting in more energy produced than energy consumed. Briquetting raw pressed-shredded without carbonization process step also showed viable energy produced, however drying step with moisture below than 10 % is required.
In conclusion and remarks, the self-sustained carbonization was successfully materialized, producing high yield and comparable CV in a small scale followed by scaling-up production of OPEFB biochar. This proposed system is preferable to the industry due to its simplicity, ease of operation and low energy requirement
Research on performance improvement method of the contact-type sensor
Get PDF九州工業大学博士学位論文 学位記番号:工博甲第395号 学位授与年月日:平成27年9月25日1 緒論||2 配管内移動ロボットに搭載する回転式センサ位置制御法の開発||3 走査型接触式センサシステムのセンサ部振動抑制制御法||4 EMATによる超音波入射方向可変システムの開発||5 結
Formation of Wear Resistance Cladding Layer on the Surface of A6061 by an Electric Resistance Cladding Method
No full text九州工業大学博士学位論文 学位記番号:工博甲第403号 学位授与年月日:平成27年9月25日第1章 緒論||第2章 高炭素鋼を内在するクラッド層のミクロ組織及び耐摩耗特性に及ぼす溶接電流の影響||第3章 超硬合金を内在するクラッド層のミクロ組織及び耐摩耗特性に及ぼすWC粉末割合の影響||第4章 超硬合金を内在する複合クラッド層のミクロ組織及び耐摩耗特性に及ぼすWC粉末粒径の影響||第5章 超硬合金を内在する複合クラッド層の耐摩耗特性及び摩耗挙動に及ぼす摩耗相手材の影響||第6章 総
An Analytical Expression for the Direct Correlation Function of a Hard-sphere Liquid Derved from the Extended Scaled Particle Theory
No full text九州工業大学博士学位論文 学位記番号:情工博甲第306号 学位授与年月日:平成27年9月25日1 序||2 方法||3 結果||4 考察||5 謝
分子内環化反応を利用した非天然アミノ酸及びプロリン誘導体の効率的合成法に関する研究
No full text九州工業大学博士学位論文 学位記番号:工博甲第401号 学位授与年月日:平成27年9月25日1. Introduction||2. Instrumentation||3. Intramolecular cyclization of epoxy amino acids produced from allylglycines to prepare four stereoisomers of 4-hydroxyproline derivatives||4. Chemoenzymatic synthesis of 5-hydroxy pipecolic acid via Jacobsen's hydrolytic kinetic resolution of epoxy amino acids||5 Regioselective cyclization and facile separation of 5-hydroxypipecolic acid||6. General ConclusionCyclic amino acids (imino acids) were synthesized from intramolecular cyclization of amino
acids functionalized with side chain epoxides; The allyl glycine and homo allyl glycine
derivatives were obtained from the diethyl 2-aminomalonate derivatives, in a series of
reaction which finally gave a racemic mixture of allyl glycine/homo allyl glycine. These
racemic mixture were well resolved and separated by one of these commercially available
enzymes, L-acylase, ?-chymotrypsin and subtilisin Carlsberg. The epoxides were obtained by
epoxidation of the side chain of enatiomerically pure 2-amino-4-pentenoic acid and its higher homologue 2-amino-5-hexenoic acid (homo allyl glycine). The epoxides were then
intramolecularly cyclized to form 4-hydroxyproline from epoxide of allyl glycine or
5-hydroxypipecolic acid from epoxide of homo allyl glycine.
The enatiomers of allyl glycine were separated by effective resolution aided by
subtilisin Carlsberg or L-acylase. The enatiomerically pure allyl glycine derivatives with
(Boc) protection were epoxidized with m-CPBA which generated the inseparable
diastereomeric epoxide. Upon removal of the Boc protection generated highly nucleophilic
amine which attacked the side-chain epoxide intramolecularly at the C5 carbon generating 4-
hydroxyproline derivatives. Due to presence of 2 chiral centers formed during the
epoxidation trans- and cis- isomers of 4-hydroxyprolines are formed. Fortunately the cisisomer was transformed to a lactone with the removal of alcohol. The cis-conformation of the hydroxyl and ester was necessary for the intramolecular reaction; the trans- isomer remained as such without lactone formation. Due to the selective intramolecular lactonization of the cis- isomer into an hydrophobic lactone, the separation of the lactone from the hydrophilic trans- isomer was facile and easy. Similarly starting from the D- isomers two diastereomers 6 of 4-hydroxyproline were synthesized.
Similarly racemic mixture of 2-amino-5-hexenoic acid were synthesized from diethyl
malonate derivatives. This racemic mixture of 2-amino-5-hexenoic acid was separated by
resolution aided by L-acylase or ?-chymotrypsin. The separated enatiomerically pure amino
acids with tert-butoxycarbonyl (Boc) protection were oxidized with excess amount of 3-
chloroperbenzoic acid (m-CPBA). The oxidation by m-CPBA generates two inseparable
diastereomeric epoxides which are formed due to new chiral center at C5 carbon. One of the
diastereomeric epoxide in the inseparable mixture was selectively converted to a dihydroxyl
compound catalyzed by Jacobsen's hydrolytic kinetic resolution (HKR) which was easily
separated from the remaining diastereomeric epoxide. The epoxide was converted to a vicinal
halohydrin, with bromide attacking on terminal C6 carbon. Upon (Boc) deprotection of the
halohydrin, the free amine attacked the C6 carbon, generating 5-hydroxypipecolic acid which
was isolated in good yield after protection of the amine with (Boc) group. In a similar manner the dihydroxyl component which was converted to an halohydrin by efficient regioselective mono-tosylation with catalytic (Bu2SnO) followed tosyl replacment by iodine substitution.
The halohydrin was used to synthesize 5-hydroxypipecolic acid derivative by Boc removal
with acid treatment, intramolecular cyclization, N- reprotection and isolation. The same
sequence was repeated for D- isomers.
Finally racemic mixture of 2-amino-5-hexenoic acid were prepared by the same
sequence described above. This racemates were subjected to subtilisin carlsberg based
resolution, which gave chiraly pure 2-amino-5-hexenoic acid. The alkene side chain of the
fully protected amino acids were oxidized with m-CPBA, which gave the diastereomers,
which were not separable. On treating the epoxide with acid led to the removal of N-Boc
group and formation of the free amine. This amine was allowed to attack the epoxide, by
treating the amine with base, which led to the neutralization of the acid. The amine
7 regioselective attacked the C6 carbon to generate the 5-hydroxypipecolic acid derivatives.
The amine was again reprotected with Boc2O to generate the fully protected 5-hydroxy
pipecolic acid derivatives Due to the diastereomeric nature of the starting material, two
product were formed (cis-) and (trans)-5-hydroxypipecolic acid. But in our reaction
conditions the cis- isomer due to the close proximity of the hydroxyl and ester group
underwent in-situ lactonization to form the hydrophobic lactone. The lactone was easily
isolated from the trans- ester. Similarly starting from the L- isomer two isomers of 5-
hydroxypipecolic acid were obtained