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Biologically Active C-Alkylated Flavonoids from Dodonaea viscosa
Akhtar Muhammad,Itrat Anis,Ajmal Khan,Bishnu P. Marasini,Muhammad Iqbal Choudhary,Muhammad Raza Shah 대한약학회 2012 Archives of Pharmacal Research Vol.35 No.3
A new C-alkylated flavonoid (5,7-dihydroxy-3'-(4''-acetoxy-3''-methylbutyl)-3,6,4'-trimethoxyflavone (1), along with two known C-alkylated flavonoids (5,7-dihydroxy-3'-(3-hydroxymethylbutyl)-3,6,4'-trimethoxyflavone (2), 5,7,4'-trihydroxy-3'-(3-hyroxymethylbutyl)-3,6-dimethoxyflavone (3) and two new source C-alkylated flavonoids (5,7-dihydroxy-3'-(2-hydroxy-3-methyl-3-butenyl)-3,6,4'-trimethoxyflavone (4), 5,7,4'-trihydroxy-3,6-dimethoxy-3'-isoprenyl-flavone (5) were isolated from the aerial parts of Dodonaea viscosa. The structures of all compounds were established on the basis of 1D and 2D NMR spectroscopy and mass spectrometry. The isolated compounds were evaluated for their inhibitory effect on urease and α-chymotrypsin enzyme. All the compounds (1-5) exhibited mild inhibition against urease but remained recessive in case of α-chymotrypsin.
Muhammad, Wazir,Hussain, Ayaz,Shah, Syed Ali Raza,Shah, Jalal,Bhutto, Zuhaibuddin,Thaheem, Imdadullah,Ali, Shamshad,Masrour, Salman International Journal of Computer ScienceNetwork S 2021 International journal of computer science and netw Vol.21 No.11
Recently, image super-resolution techniques used in convolutional neural networks (CNN) have led to remarkable performance in the research area of digital image processing applications and computer vision tasks. Convolutional layers stacked on top of each other can design a more complex network architecture, but they also use more memory in terms of the number of parameters and introduce the vanishing gradient problem during training. Furthermore, earlier approaches of single image super-resolution used interpolation technique as a pre-processing stage to upscale the low-resolution image into HR image. The design of these approaches is simple, but not effective and insert the newer unwanted pixels (noises) in the reconstructed HR image. In this paper, authors are propose a novel single image super-resolution architecture based on synchronized depthwise separable convolution with Dense Skip Connection Block (DSCB). In addition, unlike existing SR methods that only rely on single path, but our proposed method used the synchronizes path for generating the SISR image. Extensive quantitative and qualitative experiments show that our method (SDCN) achieves promising improvements than other state-of-the-art methods.
LDCSIR: Lightweight Deep CNN-based Approach for Single Image Super-Resolution
Muhammad, Wazir,Shaikh, Murtaza Hussain,Shah, Jalal,Shah, Syed Ali Raza,Bhutto, Zuhaibuddin,Lehri, Liaquat Ali,Hussain, Ayaz,Masrour, Salman,Ali, Shamshad,Thaheem, Imdadullah International Journal of Computer ScienceNetwork S 2021 International journal of computer science and netw Vol.21 No.spc12
Single image super-resolution (SISR) is an image processing technique, and its main target is to reconstruct the high-quality or high-resolution (HR) image from the low-quality or low-resolution (LR) image. Currently, deep learning-based convolutional neural network (CNN) image super-resolution approaches achieved remarkable improvement over the previous approaches. Furthermore, earlier approaches used hand designed filter to upscale the LR image into HR image. The design architecture of such approaches is easy, but it introduces the extra unwanted pixels in the reconstructed image. To resolve these issues, we propose novel deep learning-based approach known as Lightweight deep CNN-based approach for Single Image Super-Resolution (LDCSIR). In this paper, we propose a new architecture which is inspired by ResNet with Inception blocks, which significantly drop the computational cost of the model and increase the processing time for reconstructing the HR image. Compared with the other state of the art methods, LDCSIR achieves better performance in terms of quantitively (PSNR/SSIM) and qualitatively.
LDCSIR: Lightweight Deep CNN-based Approach for Single Image Super-Resolution
Muhammad, Wazir,Shaikh, Murtaza Hussain,Shah, Jalal,Shah, Syed Ali Raza,Bhutto, Zuhaibuddin,Lehri, Liaquat Ali,Hussain, Ayaz,Masrour, Salman,Ali, Shamshad,Thaheem, Imdadullah International Journal of Computer ScienceNetwork S 2021 International journal of computer science and netw Vol.21 No.12
Single image super-resolution (SISR) is an image processing technique, and its main target is to reconstruct the high-quality or high-resolution (HR) image from the low-quality or low-resolution (LR) image. Currently, deep learning-based convolutional neural network (CNN) image super-resolution approaches achieved remarkable improvement over the previous approaches. Furthermore, earlier approaches used hand designed filter to upscale the LR image into HR image. The design architecture of such approaches is easy, but it introduces the extra unwanted pixels in the reconstructed image. To resolve these issues, we propose novel deep learning-based approach known as Lightweight deep CNN-based approach for Single Image Super-Resolution (LDCSIR). In this paper, we propose a new architecture which is inspired by ResNet with Inception blocks, which significantly drop the computational cost of the model and increase the processing time for reconstructing the HR image. Compared with the other state of the art methods, LDCSIR achieves better performance in terms of quantitively (PSNR/SSIM) and qualitatively.
Abbasi, Muhammad Athar,Hassan, Mubashir,Aziz-ur-Rehman, Mubashir,Siddiqui, Sabahat Zahra,Raza, Hussain,Shah, Syed Adnan Ali,Seo, Sung-Yum Elsevier 2018 Bioorganic & medicinal chemistry Vol.26 No.13
<P><B>Abstract</B></P> <P>The present article describes the synthesis, <I>in vitro</I> urease inhibition and <I>in silico</I> molecular docking studies of a novel series of bi-heterocyclic bi-amides. The synthesis of title compounds was initiated by benzoylation, with benzoyl chloride (<B>1</B>), of the key starter ethyl 2-(2-amino-1,3-thiazol-4-yl)acetate (<B>2</B>) in weak basic aqueous medium followed by hydrazide formation, <B>4</B>, and cyclization with CS<SUB>2</SUB> to reach the parent bi-heterocyclic nucleophile, <I>N</I>-{4-[(5-sulfanyl-1,3,4-oxadiazol-2-yl)methyl]-1,3-thiazol-2-yl}benzamide (<B>5</B>). Various electrophiles, <B>8a–l</B>, were synthesized by a two-step process and these were finally coupled with <B>5</B> to yield the targeted bi-heterocyclic bi-amide molecules, <B>9a–l</B>. The structures of the newly synthesized products were corroborated by IR, <SUP>1</SUP>H NMR, <SUP>13</SUP>C NMR, EI-MS and elemental analysis. The <I>in vitro</I> screening of these molecules against urease explored that most of the compounds exhibit potent inhibitory potential against this enzyme. The compound <B>9j</B>, with IC<SUB>50</SUB> value of 2.58 ± 0.02 µM, exhibited most promising inhibitory activity among the series, relative to standard thiourea having IC<SUB>50</SUB> value of 21.11 ± 0.12 µM. <I>In silico</I> studies fully augmented the experimental enzyme inhibition results. Chemo-informatics analysis showed that synthesized compounds (<B>9a–l</B>) mostly obeyed the Lipinski's rule. Molecular docking study suggested that ligand <B>9j</B> exhibited good binding energy value (−7.10 kcal/mol) and binds within the active region of target protein. So, on the basis of present investigation, it was inferred that <B>9j</B> may serve as a novel scaffold for designing more potent urease inhibitors.</P> <P><B>Graphical abstract</B></P> <P>[DISPLAY OMISSION]</P>
Athar Abbasi, Muhammad,Raza, Hussain,Aziz-ur-Rehman, Hussain,Zahra Siddiqui, Sabahat,Adnan Ali Shah, Syed,Hassan, Mubashir,Seo, Sung-Yum Elsevier 2019 Bioorganic chemistry Vol.83 No.-
<P><B>Abstract</B></P> <P>Present work aimed to synthesize some unique bi-heterocyclic benzamides as lead compounds for the <I>in vitro</I> inhibition of urease enzyme, followed by <I>in silico</I> studies. These targeted benzamides were synthesized in good yields through a multi-step protocol and their structures were confirmed by IR, <SUP>1</SUP>H NMR, <SUP>13</SUP>C NMR, EI-MS and elemental analysis. The <I>in vitro</I> screening results showed that most of the ligands exhibited good inhibitory potentials against the urease. Chemo-informatics analysis envisaged that all these compounds obeyed the Lipinski's rule. Molecular docking results showed that <B>7h</B> exhibited good binding energy value (−8.40 kcal/mol) and was bound within the active region of urease enzyme. From the present investigation, it was inferred that some of these potent urease inhibitors might serve as novel templates in drug designing.</P> <P><B>Highlights</B></P> <P> <UL> <LI> Synthesis of bi-heterocyclic scaffolds. </LI> <LI> Structural characterization with spectral analysis. </LI> <LI> Urease inhibition and structure-activity relationship. </LI> <LI> Chemo-informatics and validation of Lipinski rule. </LI> <LI> Molecular docking analysis to ascertain interactions. </LI> </UL> </P> <P><B>Graphical abstract</B></P> <P>[DISPLAY OMISSION]</P>
Face recognition invariant to partial occlusions
( Azeem Aisha ),( Sharif Muhammad ),( Shah Jamal Hussain ),( Raza Mudassar ) 한국인터넷정보학회 2014 KSII Transactions on Internet and Information Syst Vol.8 No.7
Face recognition is considered a complex biometrics in the field of image processing mainly due to the constraints imposed by variation in the appearance of facial images. These variations in appearance are affected by differences in expressions and/or occlusions (sunglasses, scarf etc.). This paper discusses incremental Kernel Fisher Discriminate Analysis on sub-classes for dealing with partial occlusions and variant expressions. This framework focuses on the division of classes into fixed size sub-classes for effective feature extraction. For this purpose, it modifies the traditional Linear Discriminant Analysis into incremental approach in the kernel space. Experiments are performed on AR, ORL, Yale B and MIT-CBCL face databases. The results show a significant improvement in face recognition.
Hassan, Mubashir,Abbasi, Muhammad Athar,Aziz-ur-Rehman, Muhammad Athar,Siddiqui, Sabahat Zahra,Shahzadi, Saba,Raza, Hussain,Hussain, Ghulam,Shah, Syed Adnan Ali,Ashraf, Muhamamd,Shahid, Muhammad,Seo, Academic Press 2019 Bioorganic chemistry Vol.91 No.-
<P><B>Abstract</B></P> <P>In the designed research work, a series of 2-furoyl piperazine based sulfonamide derivatives were synthesized as therapeutic agents to target the Alzheimer’s disease. The structures of the newly synthesized compounds were characterized through spectral analysis and their inhibitory potential was evaluated against butyrylcholinesterase (BChE). The cytotoxicity of these sulfonamides was also ascertained through hemolysis of bovine red blood cells. Furthermore, compounds were inspected by Lipinki Rule and their binding profiles against BChE were discerned by molecular docking. The protein fluctuations in docking complexes were recognized by dynamic simulation. From our <I>in vitro</I> and <I>in silico</I> results <B>5c</B>, <B>5j</B> and <B>5k</B> were identified as promising lead compounds for the treatment of targeted disease.</P> <P><B>Highlights</B></P> <P> <UL> <LI> Sulfonamide derivatives were synthesized as therapeutic agents to target the Alzheimer’s disease. </LI> <LI> The inhibitory potential of newly synthesized compounds were evaluated against butyrylcholinesterase (BChE). </LI> <LI> The cytotoxicity of these sulfonamides was also ascertained through hemolysis of bovine red blood cells. </LI> <LI> Computational analysis was performed to check their binding profile against target protein. </LI> </UL> </P> <P><B>Graphical abstract</B></P> <P>[DISPLAY OMISSION]</P>
( Ayaz Anwar ),( Ruqaiyyah Siddiqui ),( Muhammad Raza Shah ),( Naveed Ahmed Khan ) 한국미생물 · 생명공학회 2019 Journal of microbiology and biotechnology Vol.29 No.1
Parasitic infections have remained a significant burden on human and animal health. In part, this is due to lack of clinically-approved, novel antimicrobials and a lack of interest by the pharmaceutical industry. An alternative approach is to modify existing clinically-approved drugs for efficient delivery formulations to ensure minimum inhibitory concentration is achieved at the target site. Nanotechnology offers the potential to enhance the therapeutic efficacy of drugs through modification of nanoparticles with ligands. Amphotericin B, nystatin, and fluconazole are clinically available drugs in the treatment of amoebal and fungal infections. These drugs were conjugated with gold nanoparticles. To characterize these goldconjugated drug, atomic force microscopy, ultraviolet-visible spectrophotometry and Fourier transform infrared spectroscopy were performed. These drugs and their gold nanoconjugates were examined for antimicrobial activity against the protist pathogen, Acanthamoeba castellanii of the T4 genotype. Moreover, host cell cytotoxicity assays were accomplished. Cytotoxicity of these drugs and drug-conjugated gold nanoparticles was also determined by lactate dehydrogenase assay. Gold nanoparticles conjugation resulted in enhanced bioactivity of all three drugs with amphotericin B producing the most significant effects against Acanthamoeba castellanii (p < 0.05). In contrast, bare gold nanoparticles did not exhibit antimicrobial potency. Furthermore, amoebae treated with drugs-conjugated gold nanoparticles showed reduced cytotoxicity against HeLa cells. In this report, we demonstrated the use of nanotechnology to modify existing clinically-approved drugs and enhance their efficacy against pathogenic amoebae. Given the lack of development of novel drugs, this is a viable approach in the treatment of neglected diseases.