http://chineseinput.net/에서 pinyin(병음)방식으로 중국어를 변환할 수 있습니다.
변환된 중국어를 복사하여 사용하시면 됩니다.
Bathina Venkateswararao,Devarapalli Ramesh,García Márquez Fausto Pedro 대한전기학회 2023 Journal of Electrical Engineering & Technology Vol.18 No.3
An electrical power system is a vast interlocked network that needs a vigilant design to sustain the system with an uninterrupted power flow operation without any restrictions, called optimal power flow (OPF). OPF problem requires robust and fast optimization techniques to volve it due to its complexity. Cuckoo Search (CS) is one method that is being applied in OPF problems, and it has many advantages, e.g., ease use and littler tuning parameters. But it is not good enough, falling into local optimal resolutions and slow converges. Therefore, recently developed Grey Wolf Optimization (GWO) algorithm is used to solve OPF, but it has low accuracy and inadequate local searching ability. To overcome these problems, this paper proposed to combine CS with GWO to create a novel the Hybrid algorithm, called here HCSGWO. The main objective is to deduce the emission, true power generation cost, true power losses, and voltage stability, being a multi-objective problem. THCSGWO are validated by solving the OPF problem considering the calssic IEEE57 bus system. The results are compared with GWO and other algorithms employed in the literature.
Study on IL-5 Inhibitory Activity of Novel Chromenone Derivatives
Eeda Venkateswararao,Vinay K. Sharma,Ki-Cheul Lee,Eunmiri Roh,Youngsoo Kim,Sang-Hun Jung 충남대학교 약학대학 의약품개발연구소 2013 藥學論文集 Vol.28 No.-
A novel series of chromenone analogs were synthesized and evaluated for their inhibitory activity against interleukin-5. Among them compounds 5-(cyclohexylmethoxy)-N-(4-hydroxy-3-(hydroxymethyl)phenyl)-4-oxo-4H-chromene-3-carboxamide (8e, 54% inhibition at 30 μM) and ethyl 3-(5-(cyclohexylmethoxy)- 4-oxo-4H-chromene-3-carboxamido)benzoate (8g, 62% inhibition at 30 μM) showed the most potent activity. The SAR activity of these chromenones indicated that the bulky substituents at ring B increases the inhibition against IL-5 though none of the compound showed potent inhibition. The reason for less activity of the chromenones 8a-h may be due to the rigidity of amine linkage.
Hitesh B. Jalani,Eeda Venkateswararao,Manoj Manickam,Sang-Hun Jung 대한화학회 2016 Bulletin of the Korean Chemical Society Vol.37 No.12
An efficient, practical, straight forward, and transition metal-free three-component synthesis of diversely substituted imidazoles and 2H-imidazolones from β-ketoamines, acylating agents, and ammonium acetate has been described herein. This approach involves [3+1+1] cyclization through consecutive formation of three C–N bonds as a sequence of initial amidation of β-ketoamines with acylating agent, β-iminoketoamide formation with ammonia, and acid catalyzed concomitant cyclodehydration to afford the imidazoles and 2H-imidazolones. This methodology has advantages such as single flask operation, readily available starting materials, mild conditions, broad functional groups tolerance, and simple work-up procedure.
PullaReddy Boggu,Eeda Venkateswararao,Manoj Manickam,김영수,정상헌 대한약학회 2017 Archives of Pharmacal Research Vol.40 No.4
A novel series of 2-benzylbenzimidazole analogswas designed, synthesized and investigated for theirin vitro activities against LPS induced NF-jB inhibitionin RAW 264.7 cells using the SEAP assay. Amongthem, 4-((4-(cyclohexylmethoxy)-1H-benzo[d]imidazol-2-yl)methyl)phenol (6e,[100% inhibition at 30 lM, IC50 =3.0 lM), 4-((5-(cyclohexylmethoxy)-1H-benzo[d]imidazol-2-yl)methyl)phenol (6j, 96% inhibition at 30 lM,IC50 = 4.0 lM) and 2-((4-(cyclohexylmethoxy)-1H-benzo[d]imidazol-2-yl)methyl)phenol (6k, 95% inhibition at30 lM, IC50 = 5.0 lM) showed strong inhibitory activity. The structure activity relationship confirmed that thesubstitution on benzimidazole ring A with hydrophobiccyclohexylmethoxy group at position 4 or 5 markedlyenhances the activity. In addition, the hydrophilic hydrogenbonding donor group (OH) at position 2 or 4 on phenyl ringB connected with one methylene spacer to the benzimidazolering is favorable for the inhibitory activity. However,hydrophobic (–OCH3 and –Cl) groups on phenyl ringB decrease the activity.
Novel analogs of N-acylhydroxyethylaminomethyl-4H-chromen-4-one scaffold as IL-5 inhibitors
Yang, H.S.,Venkateswararao, E.,Boggu, P.R.,Sharma, V.K.,Kim, Y.,Jung, S.H. Pergamon 2017 Bioorganic & medicinal chemistry Vol.25 No.16
A number of N-acyl substituted hydroxyethylaminomethyl-4H-chromen-4-ones 6a-u were prepared and evaluated for their IL-5 inhibitory activity. Among them, the compound 6r (95.0% inhibition at 30@?M, IC<SUB>50</SUB>=10.0@?M, ClogP=4.1549) showed most potent inhibitory activity. The structure activity relationship revealed that the bulkier or hydrophobic substituents at urea, carbamate or amide group resulted in good inhibitory activity against IL-5. Moreover, electron donating group at phenyl ring (6g and 6s) is much more active than electron withdrawing group (6f). Finally, replacement of cyclohexylmethoxy group at 5<SUP>th</SUP> position of ring A with bulky aliphatic substituents resulted in the loss of activity.
Discovery of novel 3-(hydroxyalkoxy)-2-alkylchromen-4-one analogs as interleukin-5 inhibitors
Boggu, P.R.,Venkateswararao, E.,Manickam, M.,Kim, Y.,Jung, S.H. S.E.C.T. [etc.] ; Elsevier Science Ltd 2017 European journal of medicinal chemistry Vol.139 No.-
A series of novel chromen-4-one analogs 9a-d and 10a-u was designed, synthesized and evaluated for their IL-5 inhibitory activity. Most of the chromen-4-one analogs showed strong inhibitory activity in low micro molar potency. Among them, 5-(cyclohexylmethoxy)-3-(3-hydroxypropoxy)-2-isopropyl-4H-chromen-4-one (10t, 90.0% inhibition at 30 μM, IC<SUB>50</SUB> = 5.5 μM, CLogP = 4.76887) and 2-cyclohexyl-5-(cyclohexylmethoxy)-3-(3-hydroxypropoxy)-4H-chromen-4-one (10u, 95.5% inhibition at 30 μM, IC<SUB>50</SUB> = 3.0 μM, CLogP = 5.96187) showed the best inhibition. The structure activity relationship reveals that the hydrophobic cyclohexylmethoxy group at the position 5 of the chromen-4-one ring A is preferable than at position 6 and the dual hydrogen bonding acceptor property on the chromen-4-one ring should be important for the inhibitory activity. In addition, the optimum length of the side chain at position 3 of chromen-4-one ring is critical for the donation of hydrogen to the binding site and the 3-hydroxypropoxy group showed the best activity. Moreover, the conformational restrictor (isopropyl, cyclohexyl group) at position 2 is much more favorable for the formation of effective conformer of side chain with hydrogen bonding donor property of these chromen-4-one analogs.
Design and synthesis of sulfonamidophenylethylureas as novel cardiac myosin activator
Manickam, Manoj,Jalani, Hitesh B.,Pillaiyar, Thanigaimalai,Boggu, Pulla Reddy,Sharma, Niti,Venkateswararao, Eeda,Lee, You-Jung,Jeon, Eun-Seok,Son, Min-Jeong,Woo, Sun-Hee,Jung, Sang-Hun Elsevier 2018 European Journal of Medicinal Chemistry Vol.143 No.-
<P><B>Abstract</B></P> <P>To optimize the lead urea scaffold <B>1</B> and <B>2</B> as selective cardiac myosin ATPase activator, a series of urea derivatives have been synthesized to explore its structure activity relationship. Among them <I>N,N</I>-dimethyl-4-(2-(3-(3-phenylpropyl)ureido)ethyl)benzenesulfonamide (<B>13</B>, CMA = 91.6%, FS = 17.62%; EF = 11.55%), <I>N,N</I>-dimethyl-4-(2-(1-methyl-3-(3-phenylpropyl)ureido)ethyl)benzene sulfonamide (<B>40</B>, CMA = 52.3%, FS = 38.96%; EF = 24.19%) and <I>N,N</I>-dimethyl-4-(2-(3-methyl-3-(3-phenylpropyl)ureido)ethyl)benzenesulfonamide (<B>41</B>, CMA = 47.6%, FS = 23.19%; EF = 15.47%) proved to be efficient to activate the cardiac myosin <I>in vitro</I> and <I>in vivo</I>. Further the % change in ventricular cell contractility at 5 μM of <B>13</B> (47.9 ± 3.2), <B>40</B> (45.5 ± 2.4) and <B>41</B> (63.5 ± 2.2) showed positive inotropic effect in isolated rat ventricular myocytes. The potent compounds <B>13, 40, 41</B> were highly selective for cardiac myosin over skeletal and smooth muscle myosin, thus proving them these new urea derivatives is a novel scaffold for discovery of cardiac myosin activators for the treatment of systolic heart failure.</P> <P><B>Highlights</B></P> <P> <UL> <LI> SAR study of sulfonamidophenylethylureas discovered highly potent inotrope. </LI> <LI> These urea analogs are selective cardiac myosin ATPase activators. </LI> <LI> Compound <B>13</B>, <B>40</B>, <B>41</B> shows 17.6, 38.9, 23.2% fractional shortening in the echocardiographic study with rat. </LI> <LI> The cell contractility of <B>13</B>, <B>40</B>, <B>41</B> shows 47.9, 45.5, 63.5% at 5 µM in rat ventricle cells. </LI> </UL> </P> <P><B>Graphical abstract</B></P> <P>[DISPLAY OMISSION]</P>
Manickam, M.,Jalani, H.B.,Pillaiyar, T.,Sharma, N.,Boggu, P.R.,Venkateswararao, E.,Lee, Y.J.,Jeon, E.S.,Jung, S.H. S.E.C.T. [etc.] 2017 European journal of medicinal chemistry Vol.134 No.-
A series of flexible urea derivatives have been synthesized and demonstrated as selective cardiac myosin ATPase activator. Among them 1-phenethyl-3-(3-phenylpropyl)urea (1, cardiac myosin ATPase activation at 10 μM = 51.1%; FS = 18.90; EF = 12.15) and 1-benzyl-3-(3-phenylpropyl)urea (9, cardiac myosin ATPase activation = 53.3%; FS = 30.04; EF = 18.27) showed significant activity in vitro and in vivo. The change of phenyl ring with tetrahydropyran-4-yl moiety viz., 1-(3-phenylpropyl)-3-((tetrahydro-2H-pyran-4-yl)methyl)urea (14, cardiac myosin ATPase activation = 81.4%; FS = 20.50; EF = 13.10), and morpholine moiety viz., 1-(2-morpholinoethyl)-3-(3-phenylpropyl)urea (21, cardiac myosin ATPase activation = 44.0%; FS = 24.79; EF = 15.65), proved to be efficient to activate the cardiac myosin. The potent compounds 1, 9, 14 and 21 were found to be selective for cardiac myosin over skeletal and smooth myosins. Thus, these urea derivatives are potent scaffold to develop as a newer cardiac myosin activator for the treatment of systolic heart failure.
Exploration of diphenylalkyloxadiazoles as novel cardiac myosin activator
Manickam, Manoj,Boggu, Pulla Reddy,Pillaiyar, Thanigaimalai,Sharma, Niti,Jalani, Hitesh B.,Venkateswararao, Eeda,Jung, Sang-Hun Elsevier 2018 Bioorganic & medicinal chemistry letters Vol.28 No.14
<P><B>Abstract</B></P> <P>To explore novel cardiac myosin activator, a series of diphenylalkyl substituted 1,3,4-oxadiazoles and 1,2,4-oxadiazoles have been prepared and tested for cardiac myosin ATPase activation <I>in vitro</I>. In all cases, three carbon spacer between the oxadiazole core and one of the phenyl ring was considered crucial. In case of 1,3,4-oxadiazole, zero to two carbon spacer between oxadiazole core and other phenyl ring are favorable. Phenyl ring can be replaced by cyclohexyl moiety. In case of 1,2,4-oxadiazole, zero or one carbon spacer between the oxadiazole and other phenyl ring are favorable. Introduction of hydrogen bonding donor (NH) group at the 2<SUP>nd</SUP> position of the 1,3,4-oxadiazole enhances the activity. Substitutions on either of the phenyl rings or change of phenyl ring to other heterocycle are not tolerated for both the oxadiazoles. The prepared oxadiazoles showed selective activation for cardiac muscle over smooth and skeleton muscles.</P> <P><B>Highlights</B></P> <P> <UL> <LI> The diphenylalkyl oxadiazoles were identified as novel cardiac myosin ATPase activator. </LI> <LI> Three carbon spacer between oxadiazole core and one of the phenyl ring is crucial. </LI> <LI> Introduction of NH group at the 2nd position of the 1,3,4-oxadiazole is favored. </LI> <LI> These oxadiazoles are selective activators for cardiac myosin. </LI> </UL> </P> <P><B>Graphical abstract</B></P> <P>[DISPLAY OMISSION]</P>