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Larik, Fayaz Ali,Faisal, Muhammad,Saeed, Aamer,Channar, Pervaiz Ali,Korabecny, Jan,Jabeen, Farukh,Mahar, Ihsan Ali,Kazi, Mehar Ali,Abbas, Qamar,Murtaza, Ghulam,Khan, Gul Shahzada,Hassan, Mubashir,Seo, Academic Press 2019 Bioorganic chemistry Vol.86 No.-
<P><B>Abstract</B></P> <P>The increasing resistance of pathogens to common antibiotics, as well as the need to control urease activity to improve the yield of soil nitrogen fertilization in agricultural applications, has stimulated the development of novel classes of molecules that target urease as an enzyme. In this context, the newly developed compounds on the basis of 1-heptanoyl-3-arylthiourea family were evaluated for Jack bean urease enzyme inhibition activity to validate their role as potent inhibitors of this enzyme. 1-Heptanoyl-3-arylthioureas were obtained in excellent yield and characterized through spectral and elemental analysis. All the compounds displayed remarkable potency against urease inhibition as compared to thiourea standard. It was found that novel compounds fulfill the criteria of drug-likeness by obeying Lipinski’s rule of five. Particularly compound <B>4a</B> and <B>4c</B> can serve as lead molecules in 4D (drug designing discovery and development). Kinetic mechanism and molecular docking studies also carried out to delineate the mode of inhibition and binding affinity of the molecules.</P> <P><B>Highlights</B></P> <P> <UL> <LI> A new family of 1-heptanoyl-3-arylthioureas (<B>4a-4j</B>) was synthesized in excellent yield. </LI> <LI> The synthesized 1-heptanoyl-3-arylthiourea family were evaluated for Jack bean urease enzyme inhibition activity. </LI> <LI> Particularly compound <B>4a</B> and <B>4c</B> can serve as lead molecules in 4D (drug designing discovery and development). </LI> <LI> Kinetic mechanism and molecular docking studies also carried out to delineate the mode of inhibition and binding affinity. </LI> </UL> </P> <P><B>Graphical abstract</B></P> <P>[DISPLAY OMISSION]</P>
Ahmed, Attique,Channar, Pervaiz Ali,Saeed, Aamer,Kalesse, Markus,Kazi, Mehar Ali,Larik, Fayaz Ali,Abbas, Qamar,Hassan, Mubashir,Raza, Hussain,Seo, Sung-Yum Elsevier 2019 Bioorganic chemistry Vol.86 No.-
<P><B>Abstract</B></P> <P>Selective inhibition of carbonic anhydrase (CA) enzyme is an active area of research for medicinal chemists. In the current account, a hybrid pharmacophore approach was employed to design sulfonamide, amide and amine containing new series of potent carbonic anhydrase II inhibitors. The aromatic fragment associated with pharmacophore was altered suitably in order to find effective inhibitors of CA-II. All the derivatives <B>4a-4m</B> showed better inhibition compared to the standard acetazolamide. In particular, compound <B>4l</B> exhibited significant inhibition with IC<SUB>50</SUB> value of 0.01796 ± 0.00036 µM. The chemo-informatics analysis justified that all the designed compounds possess <10 HBA and <5 HBD. The ligands-protein binding analyses showed that <B>4l</B> confined in the active binding pocket with three hydrogen bonds observed with His63, Asn66 and Thr197 residues.</P> <P><B>Highlights</B></P> <P> <UL> <LI> Hybrid pharmacophore containing sulfonamide, amide and amine designed and synthesized. </LI> <LI> All the derivatives <B>4a-4m</B> showed better inhibition than acetazolamide, with <B>4l</B> exhibiting momentous inhibition. </LI> <LI> The chemo-informatics and ligands-protein binding analyses carried out. </LI> </UL> </P> <P><B>Graphical abstract</B></P> <P>[DISPLAY OMISSION]</P>
Mahar, Jamaluddin,Saeed, Aamer,Belfield, Kevin D.,Ali Larik, Fayaz,Ali Channar, Pervaiz,Ali Kazi, Mehar,Abbas, Qamar,Hassan, Mubashir,Raza, Hussain,Seo, Sung-Yum Elsevier 2019 Bioorganic chemistry Vol.84 No.-
<P><B>Abstract</B></P> <P>A novel series of silyl-yne containing chalcone derivatives <B>5a-5j</B> was synthesized by exploiting Sonogashira coupling reaction and Claisen-Schimdt condensation reaction. The synthesized derivative were characterized by spectroscopic and elemental analysis. The selective inhibition of carbonic anhydrases is considered critical in the field of medicinal chemistry because carbonic anhydrases exits in several isoforms. Synthesized compounds were subjected to carbonic anhydrase –II assay. Except <B>5j</B>, the other derivatives exhibited better potential than standard acetazolamide. Compound <B>5e</B> was found to be potent derivative in the series with IC<SUB>50</SUB> value 0.054 ± 0.001 µM. Binding analysis revealed that most potent derivative 5e binds in the active site of CA-II and single π-π stacking interaction was observed between ring structure of ligand and Phe129 having bond length 4.90 Å. Pharmacokinetics elicited that compounds obey Lipinski’s rule and show significant drug score.</P> <P><B>Highlights</B></P> <P> <UL> <LI> Sonogashira coupling reaction was used to synthesized novel silicon containing alkyne compounds. </LI> <LI> Synthesized compounds were evaluated against carbonic anhydrase II enzyme. </LI> <LI> Binding analysis and pharmacokinetics was explored. </LI> </UL> </P> <P><B>Graphical abstract</B></P> <P>[DISPLAY OMISSION]</P>
A new anti-Helicobacter pylori juglone from Reynoutria japonica
Atif Ali Khan Khalil,박우성,Jeehoon Lee,김혜진,Kazi Marjahan Akter,Young-Min Goo,Ji-Yeong Bae,Man-Seog Chun,Junghwan Kim,Mi-Jeong Ahn 대한약학회 2019 Archives of Pharmacal Research Vol.42 No.6
A 70% ethanol extract from the root portion of Reynoutria japonica afforded one new and three known juglone derivatives, namely, 2-methoxy-6-acetyl-7-methyljuglone (1), 2-ethoxy-6-acetyl-7-methyljuglone (2), 2-methoxy-7-acetonyljuglone (3), and 3-acetyl-7-methoxy-2-methyljuglone (4) together with two phenolics (5 and 6), an anthraquinone (7), a stilbene (8) and a phthalide (9). Their structures were elucidated on the basis of comprehensive spectroscopic studies including IR, MS, and 1H, 13C, 2D NMR spectra. Compound 3 is a new compound in nature, and compounds 4–6 have been isolated for the first time from R. japonica. The isolates were evaluated for their antibacterial activity against three strains (43504, 51, and 26695) of Helicobacter pylori. The four isolated juglone derivatives (1–4) showed potent growth inhibitory activity. Among them, compounds 1–3 exhibited stronger inhibitory activity than those of the positive controls, juglone and metronidazole, for the three strains and that of another reference, clarithromycin, for the 43504 and 51 strains. Specifically, the new juglone compound 3 displayed the most potent antibacterial activity against all three strains, 43504, 51, and 26695, with MIC values of 0.06, 0.06 and 0.13 μM, respectively, and MIC50 values of 0.14, 0.11 and 0.15 μM, respectively.
A Multi-Stage Encryption Technique to Enhance the Secrecy of Image
( Arindom Mondal ),( Kazi Md ),( Rokibul Alam ),( G. G. Md. Nawaz Ali ),( Peter Han Joo Chong ),( Yasuhiko Morimoto ) 한국인터넷정보학회 2019 KSII Transactions on Internet and Information Syst Vol.13 No.5
This paper proposes a multi-stage encryption technique to enhance the level of secrecy of image to facilitate its secured transmission through the public network. A great number of researches have been done on image secrecy. The existing image encryption techniques like visual cryptography (VC), steganography, watermarking etc. while are applied individually, usually they cannot provide unbreakable secrecy. In this paper, through combining several separate techniques, a hybrid multi-stage encryption technique is proposed which provides nearly unbreakable image secrecy, while the encryption/decryption time remains almost the same of the exiting techniques. The technique consecutively exploits VC, steganography and one time pad (OTP). At first it encrypts the input image using VC, i.e., splits the pixels of the input image into multiple shares to make it unpredictable. Then after the pixel to binary conversion within each share, the exploitation of steganography detects the least significant bits (LSBs) from each chunk within each share. At last, OTP encryption technique is applied on LSBs along with randomly generated OTP secret key to generate the ultimate cipher image. Besides, prior to sending the OTP key to the receiver, first it is converted from binary to integer and then an asymmetric cryptosystem is applied to encrypt it and thereby the key is delivered securely. Finally, the outcome, the time requirement of encryption and decryption, the security and statistical analyses of the proposed technique are evaluated and compared with existing techniques.
A Hybrid Control Approach for Precise Positioning of a Piezo-Actuated Stage
M. Nafea,S. Kazi,Z. Mohamed,M. S. Mohamed Ali 제어로봇시스템학회 2014 제어로봇시스템학회 국제학술대회 논문집 Vol.2014 No.10
Piezo-actuated stages are composed of a piezoelectric actuator (PEA) and a positioning mechanism. Hysteresis behavior of PEAs limits the position accuracy of the piezo-actuated stages. This paper presents a hybrid control approach for precise positioning of a piezo-actuated stage, where Bouc-Wen hysteresis model is used to represent the hysteresis behavior of the PEA. A Luenberger observer-based feedforward controller is designed, and then integrated with a Particle Swarm Optimization (PSO)-based Proportional-Integral-Derivative (PID) controller to form a hybrid controller. Optimal PID gains are obtained based on a fitness function proposed to reduce the displacement error and achieve fast response time. The results show that using the proposed hybrid controller reduces the hysteresis effect significantly, and thus the maximum error is minimized to 0.127 μm, which is 0.17 % of the maximum displacement of 72.1 μm.
Faheem Shah,Naeemullah,Tasneem Gul Kazi,Rafaqat Ali Khan,Murtaza Sayed,Hassan Imran Afridi,Khizar Hussain Shah,Jan Nisar 한국공업화학회 2017 Journal of Industrial and Engineering Chemistry Vol.48 No.-
A novel restricted access sorbents based micro solid phase extraction (RAS-mSPE) for the extraction ofheavy metal from biological samples has been developed. Cadmium (Cd) and manganese (Mn) weredirectly extracted skipping the tedious, time consuming and expensive sample preparation stepexcluding all of the existing proteins. Sorbent’s (activated carbon cloths) surface was modified withbovine serum albumin through glutaraldehyde to make restricted access sorbent (RAS). Differentvariables affecting the extraction efficiency were selected for optimization. The limits of detectionobtained for Cd and Mn were 0.252 and 0.214 mg L 1, respectively. Analyte recoveries in fortified humanwhole blood serum and milk samples were found in the range of 90.3–103.9%. The procedure waseffectively used for Cd and Mn extraction in real samples devoid of any pretreatment step.
An Offline Electronic Payment System Based on an Untraceable Blind Signature Scheme
( Md. Abdullah Al Rahat Kutubi ),( Kazi Md. Rokibul Alam ),( Rafaf Tahsin ),( G. G. Md Nawaz Ali ),( Peter Han Joo Chong ),( Yasuhiko Morimoto ) 한국인터넷정보학회 2017 KSII Transactions on Internet and Information Syst Vol.11 No.5
This paper proposes a new offline electronic payment (e-payment) system that satisfies the major security requirements of e-payment, i.e. anonymity, unlinkability, unforgeability, double spending control, conditional traceability, and fraud prevention. The central idea is the use of Hwang et al.`s RSA-based untraceable blind signature (BS), which disables the link between the e-coin and its owner and ensures the anonymity of both the customer and the merchant. It attaches an expiration, a deposit and the transaction dates to each e-coin in order to manage the database of the bank effectively, to correctly calculate the interest on the e-coin and to aid arbitration if a dishonest customer attempts to double-spend the coin. It also ensures the anonymity of the customer as long as the coin is spent legitimately. Only when a fraudulent e-coin transaction is detected can the bank, with the help of the central authority (a trusted entity), determine the identity of the dishonest customer. The system is referred to as offline since the bank does not need to be concurrently involved in transactions between a customer and a merchant. Finally, analyses of the performance of the prototype and the primary security requirements of the proposed system are also presented.
Mariam S. Arain,Tasneem G. Kazi,Hassan I. Afridi,Muhammad Bilal,Jamshed Ali,Abdul Haseeb 한국공업화학회 2018 Journal of Industrial and Engineering Chemistry Vol.62 No.-
It is reported in literature that zinc (Zn2+) has antidepressant activity. In present study Zn2+ was analyzed in blood serum of male patients having various psychiatric disorders (schizophrenia, depression, bipolar). As it is usually present in trace levels. Hence a novel, environmental friendly, dual-cloud point extraction (d-CPE) method was developed for the enrichment of its trace levels in acid digested serum samples. In the first step of d-CPE, Zn2+ was complexed with 1-(2-pyridylazo)-2-naphthol (PAN), and the complex was entrapped in a nonionic surfactant (Triton X-114). After achieving cloud point by heating, the mixture was separated into two layers i.e. aqueous and surfactant-rich by centrifugation. In second step of d-CPE, the analyte complex in the surfactant-rich phase was treated wih acid to extract back the metal analytes in acidic aqueous phase, the mixture was again heated upto cloud point and the whole procedure was repeated. This time the aqueous phase, having the metals, was taken and subjected to FAAS using conventional nebulization. The accuracy of the developed methodologies (conventional and d-CPE), were verified by their application to certified reference material of serum (CRM). Reliability of the method was checked by relative standard deviation (%RSD), which was found to be <5%. The limit of detection and limit of quantification were calculated for the proposed method as 1.09 μg/L, and 3.63 respectively and enhancement factor was found to be 40. The developed procedure was successfully applied to the serum samples of patients (male) having different psychiatric disorders and non-psychiatric control subjects for the determination of Zn2+.