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Eeda Venkateswara Rao,Vinay Kumar Sharma,Niti Sharma,Young-Soo Kim,Sang-Hun Jung 충남대학교 약학대학 의약품개발연구소 2014 藥學論文集 Vol.29 No.-
To define the role of substituents of chalcones as potent MD-2 inhibitors, we designed and synthesized analogs of 1-(2-hydroxy-6-(isopentyloxy)phenyl)-3-(4-hydroxyphenyl)prop-2-en-1-one (1) for their in vitro activities against RAW 264.7 cell using the SEAP assay as well as for LPS displacement assay. Among all the derivatives, compound 5 (IC50=27.3 μM), showed good inhibition of NF-κB activation by blocking the TLR4-mediated NF-κB activation signalling in RAW 264.7 as well as the rhMD-2 binding to immobilized LPS with 53% inhibition at 30 μM. The SAR studies indicated that small alkyl group like 3-methylbutoxy at 6-position of ring A and substituent with hydrogen bonding capability at 4-position of ring B of chalcone should be very important for inhibition of LPS induced NF-κB activation and LPS displacement of MD-2.
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.
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.
Pakkath, Rajeesh,Reddy, Eeda Koti,Kuriakose, Sheena,Saritha, C,Sajith, Ayyiliath M,Karuvalam, Ranjith Pakkath,Haridas, Karickal Raman Korean Chemical Society 2019 대한화학회지 Vol.63 No.5
The most important parameter of organic molecules for energy harvesting application focuses mainly on their band gap (HOMO-LUMO). In this report, we synthesized differently substituted 1,3,5-triazine based organic molecule which on future processing can be used in organic electronics like solar cells and OLED's. The energy gap of the synthesized novel analogue was calculated using cyclic voltammetry, UV-Visible spectroscopy and compared with density functional theory (DFT) studies.
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.
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>
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>