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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>
Hassan, Mubashir,Abbasi, Muhammad Athar,Aziz-ur-Rehman, Muhammad Athar,Siddiqui, Sabahat Zahra,Hussain, Ghulam,Shah, Syed Adnan Ali,Shahid, Muhammad,Seo, Sung-Yum Elsevier 2018 Journal of theoretical biology Vol.458 No.-
<P><B>Abstract</B></P> <P>A new series of multifunctional amides has been synthesized having moderate enzyme inhibitory potentials and mild cytotoxicity. 2-Furyl(1-piperazinyl)methanone (<B>1</B>) was coupled with 3,5-dichloro-2-hydroxybenzenesulfonyl chloride (<B>2</B>) to form {4-[(3,5-dichloro-2-hydroxyphenyl)sulfonyl]-1-piperazinyl}(2-furyl)methanone (<B>3</B>). Different elecrophiles were synthesized by the reaction of various un/substituted anilines (<B>4a-o</B>) with 2-bromoacetylbromide (<B>5</B>), 2‑bromo‑<I>N</I>-(un/substituted-phenyl)acetamides (<B>6a-o</B>). Further, equimolar ratios of <B>3</B> and <B>6a-o</B> were allowed to react in the presence of K<SUB>2</SUB>CO<SUB>3</SUB> in acetonitrile to form desired multifunctional amides (<B>7a-o</B>). The structural confirmation of all the synthesized compounds was carried out by their EI-MS, IR, <SUP>1</SUP>H NMR and <SUP>13</SUP>C NMR spectral data. Enzyme inhibition activity was performed against acetyl and butyrylcholinestrase enzymes, whereby <B>7e</B> showed very good activity having IC<SUB>50</SUB> value of 5.54 ± 0.03 and 9.15 ± 0.01 <I>μ</I>M, respectively, relative to eserine, a reference standard. Hemolytic activity of the molecules was checked to asertain their cytotoxicity towards red blood cell membrance and it was observed that most of the compounds were not toxic up to certain range. Moreover, chemoinformatic protepties and docking simulation results also showed the significance of <B>7e</B> as compared to other compounds. Based on <I>in vitro</I> and <I>in silico</I> analysis <B>7e</B> could be used as a template for the development of new drugs against Alzheimer's disease.</P> <P><B>Highlights</B></P> <P> <UL> <LI> Designing of multifunctional amides derivatives as acetyl and butyrylcholinesterase inhibitors. </LI> <LI> Chemoinformatic, molecular docking and simulation analysis was against most potent inhibitor <B>7e.</B> </LI> <LI> In vitro and in silico results showed the significance of <B>7e</B> and could be used as a template for novel drugs against Alzheimer's disease. </LI> </UL> </P>
Hassan Abolghasemi,Yunes Panahi,Minoo Ahmadinejad,Gholamreza Toogeh, MD,Mehran Karimi,Aziz Eghbali,Nargess Bigom Mirbehbahani,Bighan Keikhaei Dehdezi,Zahra Badiee,Hamid Hoorfar,Peyman Eshghi,Nader Mag 대한약침학회 2018 Journal of pharmacopuncture Vol.21 No.2
Objective: This study compared the safety and efficacy of Safacto® versus xyntha® in patients with severe hemophilia A. Methods: Thirty-three male patients with severe hemophilia A were randomly divided into two groups. Seventeen patients received Safacto® and 16 patients received Xyntha® for four consecutive times. The dosage of FVIII was 40-50 IU/kg for each injection. Plasma level of FVIII activity was evaluated before every injection, 15 minutes after the injection and one month after the start of the trial. The rate of factor VIII activity, pain and joint motion were also assessed before and after the treatment. Results: Plasma level of FVIII clotting activity in Safacto® and Xyntha® were 1.96±0.5 IU/dl and 1.63±0.5 IU/dl and increased to 88.84±25.2 IU/dl and 100.09±17.8 IU/ dl, respectively (P<0.001). Pain score and range of motion improvement were 9.3±0.9 and 8.7±0.1 in Safacto® (P=0.17); and 9.4±0.8 and 8.8±0.3 in Xyntha® (P=0.35), respectively. No allergic or other unfavorable reactions was observed with either of the preparations. Conclusion: This study showed that Safacto® has a favorable efficacy and safety profile.
Abolghasemi, Hassan,Panahi, Yunes,Ahmadinejad, Minoo.,Toogeh, Gholamreza,Karimi, Mehran,Eghbali, Aziz,Mirbehbahani, Nargess Bigom,Dehdezi, Bighan Keikhaei,Badiee, Zahra,Hoorfar, Hamid,Eshghi, Peyman,M KOREAN PHARMACOPUNCTURE INSTITUTE 2018 Journal of pharmacopuncture Vol.21 No.2
Objective: This study compared the safety and efficacy of $Safacto^{(R)}$ versus $xyntha^{(R)}$ in patients with severe hemophilia A. Methods: Thirty-three male patients with severe hemophilia A were randomly divided into two groups. Seventeen patients received $Safacto^{(R)}$ and 16 patients received $Xyntha^{(R)}$ for four consecutive times. The dosage of FVIII was 40-50 IU/kg for each injection. Plasma level of FVIII activity was evaluated before every injection, 15 minutes after the injection and one month after the start of the trial. The rate of factor VIII activity, pain and joint motion were also assessed before and after the treatment. Results: Plasma level of FVIII clotting activity in $Safacto^{(R)}$ and $Xyntha^{(R)}$ were $1.96{\pm}0.5IU/dl$ and $1.63{\pm}0.5IU/dl$ and increased to $88.84{\pm}25.2IU/dl$ and $100.09{\pm}17.8IU/dl$, respectively (P<0.001). Pain score and range of motion improvement were $9.3{\pm}0.9$ and $8.7{\pm}0.1$ in $Safacto^{(R)}$ (P=0.17); and $9.4{\pm}0.8$ and $8.8{\pm}0.3$ in $Xyntha^{(R)}$ (P=0.35), respectively. No allergic or other unfavorable reactions was observed with either of the preparations. Conclusion: This study showed that $Safacto^{(R)}$ has a favorable efficacy and safety profile.