satya chilla | University of Mons (original) (raw)

Papers by satya chilla

Tetrahedron, Sep 1, 2014

In the present work a modular pathway towards the synthesis of a new versatile MRI contrast agent... more In the present work a modular pathway towards the synthesis of a new versatile MRI contrast agent is reported and its physico-chemical properties are described. Two different functional groups were attached on two arms of the gadolinium 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetate (DOTA) in order to get a platform able to bind one probe designed to target specific biological marker and a fluorescent molecule likely to be used for optical imaging. The nuclear magnetic relaxation dispersion (NMRD) profile, the oxygen-17 relaxometric NMR study and stability assessment versus transmetalation of the Gd-complex show that this new contrast agent has a relaxivity and transmetalation stability similar to GdeDOTA.

Bioorganic & Medicinal Chemistry, 2017

A new facile synthetic strategy was developed to prepare bifunctional monophosphinic acid Ln-DOTA... more A new facile synthetic strategy was developed to prepare bifunctional monophosphinic acid Ln-DOTA derivatives, Gd-DO2AGAP NBn and Gd-DO2AGAP ABn. The relaxivities of the Gd-complexes are enhanced compared to Gd-DOTA. Monophosphinic acid arm of these Gd-complexes affords enhancement of inner sphere water exchange rate due to its steric bulkiness. The different functionalities of DO2AGAP NBn were appended in trans positions and are designed to conjugate identical or different vectors according to the potential applications. The conjugation of Gd-DO2AGAP ABn with E3 peptide known to target apoptosis was successfully performed and in vivo MRI allowed cell death detection in a mouse model.

Bioorganic & medicinal chemistry letters, Jun 13, 2017

Designing drug candidates exhibiting polypharmacology is one of the strategies adopted by medicin... more Designing drug candidates exhibiting polypharmacology is one of the strategies adopted by medicinal chemists to address multifactorial diseases. Metabolic disease is one such multifactorial disorder characterized by hyperglycaemia, hypertension and dyslipidaemia among others. In this paper we report a new class of molecular framework combining the pharmacophoric features of DPP4 inhibitors with those of ACE inhibitors to afford potent dual inhibitors of DPP4 and ACE.

Inorganica Chimica Acta, 2005

In this paper, we report the synthesis and the characterization of a novel series of lanthanide (... more In this paper, we report the synthesis and the characterization of a novel series of lanthanide (III) complexes with two potentially hexadentate ligands. The ligands contain a rigid phenanthroline moiety and two flexible hydrazonic arms with different donor atom sets (NNN 0 N 0 OO and NNN 0 N 0 N 00 N 00 , respectively for H 2 L 1 (2,9-diformylphenanthroline)bis(benzoyl)hydrazone and H 2 L 2 (2,9-diformylphenanthroline)bis(2-pyridyl)hydrazone). Both nitrate and acetate complexes of H 2 L 1 with La, Eu, Gd, and Tb were prepared and fully characterized, and the X-ray crystal structure of the complex [Eu(HL 1)(CH 3 COO) 2 ] AE 5H 2 O is presented. The stability constants of the equilibria Ln 3+ + H 2 L 1 = [Ln(H 2 L 1)] 3+ and Ln 3+ + (L 1) 2À = [Ln(L 1)] + (Ln = La(III), Eu(III), Gd(III), and Tb(III)) are determined by UV spectrophotometric titrations in DMSO at t = 25°C. The nitrate complexes of H 2 L 2 with La, Eu, Gd and Tb were also synthesized, and the X-ray crystal structures of [La(H 2 L 2)(NO 3) 2 (H 2 O)](NO 3), [Eu(H 2 L 2)(NO 3) 2 ](NO 3) and [Tb(H 2 L 2)(NO 3) 2 ](NO 3) are discussed.

Polymers, Dec 2, 2019

Reactive extrusion and magnesium (II) N-heterocyclic carbene catalyst are successfully employed i... more Reactive extrusion and magnesium (II) N-heterocyclic carbene catalyst are successfully employed in continuous polylactide synthesis. The possibility of using six-membered N-heterocyclic carbene adducts to act as efficient catalysts towards the sustainable synthesis of poly(l-lactide) through ring-opening polymerization of l-lactide (LA) is first investigated in bulk batch reactions. Under optimized solvent-free conditions, polylactide (PLA) of moderate to high molecular weights and excellent optical activities are successfully achieved. These promising results are further applied in the continuous production of PLA in an extruder.

Israel Journal of Chemistry

Molecules (Basel, Switzerland), Jan 21, 2018

Non-invasive imaging and quantification of human beta cell mass remains a major challenge. We per... more Non-invasive imaging and quantification of human beta cell mass remains a major challenge. We performed pre-clinical in vivo validation of a peptide previously discovered by our group, namely, P88 that targets a beta cell specific biomarker, FXYD2γa. We conjugated P88 with DOTA and then complexed it with GdCl₃ to obtain the MRI (magnetic resonance imaging) contrast agent (CA) Gd-DOTA-P88. A scrambled peptide was used as a negative control CA, namely Gd-DOTA-Scramble. The CAs were injected in immunodeficient mice implanted with EndoC-βH1 cells, a human beta cell line that expresses FXYD2γa similarly to primary human beta cells. The xenograft-bearing mice were analyzed by MRI. At the end, the mice were euthanized and the CA biodistribution was evaluated on the excised tissues by measuring the Gd concentration with inductively coupled plasma mass spectrometry (ICP-MS). The MRI and biodistribution studies indicated that Gd-DOTA-P88 accumulates in EndoC-βH1 xenografts above the level obs...