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Jalani, Ghulam,Jung, Chan Woo,Lee, Jae Sang,Lim, Dong Woo Dove Medical Press 2014 International journal of nanomedicine Vol.9 No.1
<P>Stimuli-responsive, polymer-based nanostructures with anisotropic compartments are of great interest as advanced materials because they are capable of switching their shape via environmentally-triggered conformational changes, while maintaining discrete compartments. In this study, a new class of stimuli-responsive, anisotropic nanofiber scaffolds with physically and chemically distinct compartments was prepared via electrohydrodynamic cojetting with side-by-side needle geometry. These nanofibers have a thermally responsive, physically-crosslinked compartment, and a chemically-crosslinked compartment at the nanoscale. The thermally responsive compartment is composed of physically crosslinkable poly(N-isopropylacrylamide) poly(NIPAM) copolymers, and poly(NIPAM-co-stearyl acrylate) poly(NIPAM-co-SA), while the thermally-unresponsive compartment is composed of polyethylene glycol dimethacrylates. The two distinct compartments were physically crosslinked by the hydrophobic interaction of the stearyl chains of poly(NIPAM-co-SA) or chemically stabilized via ultraviolet irradiation, and were swollen in physiologically relevant buffers due to their hydrophilic polymer networks. Bicompartmental nanofibers with the physically-crosslinked network of the poly(NIPAM-co-SA) compartment showed a thermally-triggered shape change due to thermally-induced aggregation of poly(NIPAM-co-SA). Furthermore, when bovine serum albumin and dexamethasone phosphate were separately loaded into each compartment, the bicompartmental nanofibers with anisotropic actuation exhibited decoupled, controlled release profiles of both drugs in response to a temperature. A new class of multicompartmental nanofibers could be useful for advanced nanofiber scaffolds with two or more drugs released with different kinetics in response to environmental stimuli.</P>
Controlled biohybrid nanoprobes with silver nanoparticle clusters for Raman imaging
Jalani, Ghulam,Lee, Sangyeop,Jung, Chan Woo,Jang, Hongdeok,Choo, Jaebum,Lim, Dong Woo The Royal Society of Chemistry 2013 The Analyst Vol.138 No.17
<P>A new class of biohybrid nanoprobes has been developed for surface-enhanced Raman scattering-based bioimaging. Silver nanoparticle clusters were encapsulated in polymeric nanoparticles using electrohydrodynamic jetting, followed by stabilization and bioconjugation. Controlled SERS intensity with high sensitivity, chemical stability, and biocompatibility makes the SERS biohybrid nanoprobes useful for bioimaging.</P> <P>Graphic Abstract</P><P>A new class of controlled biohybrid nanoprobes was developed by electrohydrodynamic jetting of polymer solutions with a homogeneous suspension of silver nanoparticle clusters for SERS-based imaging of biological markers. The control of SERS intensity with high sensitivity, chemical stability, and biocompatibility makes SERS biohybrid nanoprobes useful for bioimaging. <IMG SRC='http://pubs.rsc.org/services/images/RSCpubs.ePlatform.Service.FreeContent.ImageService.svc/ImageService/image/GA?id=c3an00943b'> </P>
Practical Synthetic Procedure for Preparation of Omecamtiv Mecarbil
Hitesh B. Jalani,Sang-Hun Jung 忠南大學校 醫藥品開發硏究所 2019 藥學論文集 Vol.34 No.-
An economical, efficient and safe process for the synthesis of omecamtiv mecarbil is described herein. The successful synthesis of key intermediate methyl 4-(3-amino-2-fluorobenzyl)piperazine-1-carboxylate was achieved through relatively convenient three steps form 2-fluoro-3-nitrotoluene. The bromination of 2-fluoro-3-nitrotoluene gave 1-(bromomethyl)-2-fluoro-3-nitrobenzene and its condensation with methyl piperazinecarboxylate generated methyl 4-(3-nitro-2-fluorobenzyl)piperazine-1-carboxylate. The subsequent reduction of this nitro compound produced the key intermediate, which was converted to omecamtiv mecarbil by the reaction with triphosgene and then 5-amino-2-picoline. This process avoids the use of poisonous reagents such as sodium cyanide and pyrophoric DIBAL and expensive materials, which were used in previous methods. This process uses simple, economical and commercially available starting materials with very good yield as compared to earlier reported methods.
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.
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.
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>