A5005831943- Synthesis and Biological Evaluation
- Synthesis and Reactivity of Heterocycles
- Catalytic C–H Functionalization Methods
- Catalytic Cross-Coupling Reactions
- Crystallization and Solubility Studies
- X-ray Diffraction in Crystallography
- Phenothiazines and Benzothiazines Synthesis and Activities
- Synthesis of heterocyclic compounds
- Synthesis and Reactions of Organic Compounds
- Synthesis and Characterization of Heterocyclic Compounds
- Synthesis and biological activity
- Chemical Synthesis and Analysis
- Chemical synthesis and alkaloids
- Synthesis of Organic Compounds
- Chemical Reaction Mechanisms
- Multicomponent Synthesis of Heterocycles
- Quinazolinone synthesis and applications
- Sulfur-Based Synthesis Techniques
- Synthesis and Catalytic Reactions
- Coordination Chemistry and Organometallics
- Cyclopropane Reaction Mechanisms
- Chemical Synthesis and Reactions
- Asymmetric Synthesis and Catalysis
- Circadian rhythm and melatonin
- Cancer therapeutics and mechanisms
Institut de Chimie Organique et Analytique
2015-2024
Centre National de la Recherche Scientifique
2014-2024
Université d'Orléans
2015-2024
Euro-Mediterranean University of Fes
2014-2024
Euromedic
2021-2022
Kansas State University
2019
University of Hassan II Casablanca
2019
Université de Montréal
2019
University of Toronto
2019
Université de Tours
2001-2018
G protein-coupled receptors (GPCRs) are classically characterized as cell-surface transmitting extracellular signals into cells. Here we show that central components of a GPCR signaling system comprised the melatonin type 1 receptor (MT
Abstract This review surveys recent developments (reported in the last fifteen years) organometallic‐chemistry‐based methods for functionalization of imidazo[1,2‐ a ]pyridines, particular decoration pyridine and imidazole rings by means reactions such as Sonogashira, Heck, Negishi, Suzuki–Miyaura, Stille cross‐coupling, well C–H activation, C‐arylation, C‐alkenylation, carbonylation. Results relating to one‐pot double two different positions on ]pyridine system are also reviewed. Procedures...
We report two prototype Ln3+complexes that address requirements for both MRI and luminescence imaging we demonstrate the presence of H2O molecules bound to Ln3+, beneficial applications Gd3+ analogue, is not a major limitation development NIR luminescent agents.
Among 25 3-aryl-2-quinolone derivatives synthesized, the antitumor activity of some them was characterized both in vitro and vivo. In this series, no compound appeared to be cytotoxic vitro, as known by colorimetric MTT assay carried out on 12 distinct human cancer cell lines obtained from American Type Culture Collection. Indeed, concentration values decreasing growth at least 50% (IC50 index) were always higher than 10-5 M. We then made use a computer-assisted phase-contrast...
This report aims to review the advances made in C–H arylation of 5,6, 6,6 and 5,5 fused-heterocyclic systems.
The design, synthesis, and screening of dual PI3K/mTOR inhibitors that gave nanomolar enzymatic cellular activities on both targets with an acceptable kinase selectivity profile are described. A docking study was performed to understand the binding mode compounds explain differences in biological activity. In addition, effects best were determined six cancer cell lines compared those a healthy diploid line for cytotoxicity. Two highly potent cells submicromolar range without any toxicity...
[reaction: see text] Palladium-catalyzed cross-coupling of vinyl- and arylstannanes with pi-electron-deficient heteroaromatics was performed in good yields. This Stille-type reaction carried out a methylthioether function as an electrophile the presence copper(I) bromide-dimethyl sulfide complex.
A new and efficient method for the synthesis of 2,3,6-trisubstituted imidazo[1,2-a]pyridine derivatives using a microwave-assisted one-pot, two-step Suzuki/heteroarylation or three-step cyclization/Suzuki/heteroarylation was developed. Polysubstituted compounds are obtained in good yield from 2-amino-5-halogenopyridines, 2-halogenocarbonyl derivatives, boronic acids, heteroaryl bromides.
The first palladium-catalyzed oxidative alkenylation of (1H)- and (2H)-indazole derivatives with various olefins is described. use Pd(OAc)2 as the catalyst Ag2CO3 oxidant promoted selective C3-monoalkenylation (1H)-indazoles (2H)-indazoles, affording desired products in good yields. An original C7-alkenylation 3-substituted was also developed. (1H)-indazole successfully applied to total synthesis drug candidate gamendazole a step- atom-economical fashion.
Background and Purpose The paradigm that GPCRs are able to prolong or initiate cellular signalling through intracellular receptors recently emerged. Melatonin binds G protein‐coupled MT 1 2 receptors. In contrast most other hormones targeting GPCRs, melatonin its synthetic analogues amphiphilic molecules easily penetrating into cells, but the existence of is still unclear mainly due a lack appropriate tools. Experimental Approach We therefore designed synthesized series hydrophilic receptor...
2-(4,5-Dihydro-1H-imidazol-2-yl)-3,4-dihydro-2H-1,4-benzoxazine derivatives and tricyclic analogues with a fused additional ring on the nitrogen atom of benzoxazine moiety have been prepared evaluated for their cardiovascular effects as potential antihypertensive agents. The imidazoline was generated by reaction corresponding ethyl ester ethylenediamine. Affinities binding sites (IBS) I1 I2 α1 α2 adrenergic receptors were well mean arterial blood pressure (MAP) heart rate (HR) spontaneously...
The development of CDK and GSK3 inhibitors has been regarded as a potential therapeutic approach, substantial number diverse structures have reported to inhibit CDKs GSK-3β in recent years. Only few molecules gone through or are currently undergoing clinical trials GSK inhibitors. In this paper, we prepared valmerins, new family containing the tetrahydropyrido[1,2-a]isoindone core. fused heterocycle was with straightforward synthesis that functionalized by (het)arylurea. Twelve valmerins...
Abstract The first example of intermolecular C–H arylation substituted 1 H ‐indazoles is reported. Various 1‐substituted indazoles were used as starting materials, and (hetero)aryl bromides iodides investigated coupling partners. Different reaction conditions investigated. best results obtained using Pd(OAc) 2 catalyst, 1,10‐phenanthroline ligand, K CO 3 base, DMA solvent. crucial role the ligand on highlighted.
A novel direct C7-arylation of indazoles with iodoaryls is described using Pd(OAc)2 as catalyst, 1,10-phenanthroline ligand, and K2CO3 base in refluxing DMA. Direct 3-substituted 1H-indazole containing an EWG on the arene ring gave expected products good isolated yields. In addition, a one-pot Suzuki-Miyaura/arylation procedure leading to C3,C7-diarylated has been developed.
3-iodo-1H-pyrrolo[3',2':4,5]imidazo-[1,2-a]pyridines and [1,2-b]pyridazines were prepared following Groebke-Blackburn-Bienaymé MCR combined with I2-promoted electrophilic cyclization. The flexibility of the method enables introduction diversity in 2, 5, 6, 7 positions on resulting scaffold using commercially available starting materials. Furthermore, subsequent palladium-catalyzed reactions successfully achieved our iodinated derivatives.
Substituted 1,4-benzoxazines bearing an amino side chain at the 2-position were prepared and found to have a moderate activity on intracellular calcium. Of compounds studied it was that those which possess homoveratrylamino moiety exhibited superior potency. The length nature of amine (4-fluorophenylpiperazine, 4-fluorobenzhydryloxyethylamine, N-substituted homoveratrylamine) is discussed. 4-benzyl-3, 4-dihydro-2-[3-[[2-(3,4-dimethoxyphenyl)ethyl]amino]propyl]-2H-1, 4-benzoxazine (3c) most...
The palladium-catalyzed coupling reaction of 3-thiomethyl-1,2,4-triazine 1 with different organoboron compounds in the presence copper(I) 3-methylsalicylate proceeds to afford corresponding 3-substituted-1,2,4-triazines good yield. This approach leads very easily a large range C-5 and C-6 unsubstituted as-triazines.
Contrary to the common idea that Fischer indole cyclization often cannot be effectively applied synthesis of corresponding azaindoles, we show this approach can actually very efficient for formation 4- and 6-azaindoles bearing an electron-donating group on starting pyridylhydrazines. Two 4-azaindole natural product analogues were synthesized in a few steps good overall yields.