73279-02-4

Upstream product

• 5460-29-7 2-(3-bromopropyl)isoindole-1,3-dione 
• 123-08-0 4-hydroxy-benzaldehyde 
• 136918-14-4 phthalimide 
• 17954-81-3 4-(3-bromopropoxy)benzaldehyde 

Downstream Products

• 244094-34-6 3-Methylene-2-oxo-5-(p-N-phthalimidopropoxyphenyl)-tetrahydrofuran 
• 1417738-47-6 [1N-(oxyproplyamine)-3,6,10,13,16,19-hexaazabicyclo[6.6.6]eicosane-1,8-diamine] 
• 1219094-77-5 C₂₇H₃₂BF₂N₃OS 
• 1219094-76-4 C₂₆H₃₄BF₂N₃O 
• 1219094-78-6 C₃₆H₅₁BF₂N₅O₂S 
• 1240125-33-0 4,4'-{[3-(1,3-dihydro-1,3-dioxo-2H-isoindol-2-yl)propoxy]phenylmethylene}bis(N,N-dimethylbenzeneamine) 
• 754992-79-5 ((3-(4-(((2-(3-(((tert-butoxy)carbonyl)amino)propoxy)benzoyl)(6-phenoxy-2-benzothiazolyl)amino)methyl)phenoxy)propyl)carbonimidoyl)-bis-carbamic acid bis(tert-butyl) ester 
• 754992-76-2 N-(3-(2-(N-(6-phenoxybenzothiazol-2-yl)-N-(4-(3-(1,3-dihydro-1,3-dioxoisoindol-2-yl)propoxy)benzyl)carbamoyl)phenoxy)propyl)carbamic acid tert-butyl ester 
• 754992-83-1 (3-{2-[[4-(3-amino-propoxy)-benzyl]-(6-phenoxy-benzothiazol-2-yl)-carbamoyl]-phenoxy}-propyl)-carbamic acid tert-butyl ester 
• 754992-74-0 2-(3-(4-((6-phenoxybenzothiazol-2-ylamino)methyl)phenoxy)propyl)isoindole-1,3-dione 

Relevant academic research and scientific papers

Design, synthesis and biological evaluation of novel phthalimide-Schiff base-coumarin hybrids as potent α-glucosidase inhibitors

We have designed and synthesized phthalimide-Schiff base-coumarin hybrids 8a–b, 9a–d, 10a–b, and 11a–d and evaluated them for α-glucosidase inhibitory potential against yeast form of this enzyme. For the synthesis of title compounds 4-hydroxybenzaldehyde, 4-hydroxy-3-methoxybenzaldehyde, 2-hydroxybenzaldehyde, 2-hydroxybenzaldehyde derivatives, coumarin-3-carbohydrazide, and coumarin-7-yloxy-acetohydrazide were used. In vitro α-glucosidase inhibition revealed that all the synthesized compounds exhibited outstanding α-glucosidase inhibition with IC50 values ranging between 85.2 ± 1.7 and 577.7 ± 7.5?μM when compared with the standard inhibitor acarbose having IC50 value 750.0 ± 12.0?μM. The most potent compounds were 4-hydroxybenzaldehyde derivative 8a with coumarin-3-carbohydrazide moiety, 2-hydroxy-5-nitrobenzaldehyde derivative 11d with coumarin-7-yloxy-acetohydrazide moiety, and 2-hydroxy-5-nitrobenzaldehyde derivative 9d with coumarin-3-carbohydrazide moiety. Molecular docking studies were carried out to understand the interaction modes and binding energies of the most active compounds and standard drug acarbose. This studies predicted that compounds 8a, 11d, and 9d (respectively with binding energies = ? 10.77, ? 8.65, and ? 8.66?kcal/mol) bind to active site α-glucosidase more easily than acarbose (binding energy = ? 4.04?kcal/mol).

Design, synthesis, in silico analysis with PPAR-γ receptor and study of non-covalent interactions in unsymmetrical heterocyclic/phenyl fleximer

This work deals with the design, synthesis, in silico analysis, crystallization, and the interpretation 2-cyano-3-{4-[2-(phthalimid-nyl)-propoxy]-phenyl}-acrylic acid ethyl ester (7). Analog 7 is designed based on rosiglitazone. The quantitative analysis

Synthesis and Characterization of Novel Phthalimide-pyrano[3,2-c]chromene and Phthalimide-pyrano-2-one Hybrids

Coumarin skelton holds substantial promise for further exploration because of its immense pharmacological potential. In this pursuit, a series of phthalimide-chromen and phthalimide-pyran-2-one hybrids were synthesized in efficient yields via one-pot multicomponent reaction of aldehyde linked to phthalimide moiety, 4-hydroxy coumarin/4-hydroxy-6-methyl-2H-pyran-2-one, and malanonitrile by Knoevenagel reaction at room temperature in the presence of DABCO as catalyst. The compounds were characterized by 1H NMR and 13C NMR, MS, and FTIR. All the compounds consisting of phthalimide-chromen/pyrano-2-one moieties tethered by spacers of varying lengths were evaluated for their biological activity in Ellman's assay. Most of the compounds feebly inhibited Acetylcholinesterase Enzyme and were inactive toward Butyrylcholinesterase Enzyme.

Discovery of imidazopyridines containing isoindoline-1,3-dione framework as a new class of BACE1 inhibitors: Design, synthesis and SAR analysis

Alzheimer's disease is characterized by chronic neurodegeneration leading to dementia. The main cause of neurodegeneration is considered to be the accumulation of amyloid-β. Inhibiting BACE1 is a well-studied approach to lower the burden of amyloid-β aggregates. We designed a series of imidazopyridines-based compounds bearing phthalimide moieties as inhibitors of BACE1. The compounds 8a-o were synthesized by the Groebke–Blackburn–Bienaymé three-component reaction of heteroaromatic amidines, aldehydes and isocyanides. Evaluating the BACE1 inhibitory effects of the synthesized compounds revealed that introducing an aminocyclohexyl moiety in the imidazopyridine core resulted in a significant improvement in its BACE1 inhibitory potential. In this regard, compound 8e was the most potent against BACE1 with an IC50 value of 2.84 (±0.95) μM. Molecular docking revealed that the nitrogen atom of imidazopyridines and the oxygen atom of the phenoxypropyl linker were involved in hydrogen bound interactions with Asp228 and Asp32 of BACE1 active site, respectively. The phthalimide moiety oriented toward the flap pocket and interacted with phe108, lle110, Trp115, Ile118 through van der Waal's and hydrophobic interactions. These findings demonstrate that imidazopyridines-based compounds bearing phthalimide moiety have the potential to decrease amyloid-β levels and ameliorate the symptoms of Alzheimer's disease.

Sol-gel reaction of porphyrin-based superstructures in the organogel phase: Creation of mechanically reinforced porphyrin hybrids

We have demonstrated that a one-dimensional molecular assembly created by an H-aggregated porphyrin·Cu(II) stack can be immobilized, without a morphological change, by sol-gel polycondensation of the peripheral triethoxysilyl groups. The resultant gel pre

Synthesis and biological evaluation of nonpeptide mimetics of ω-conotoxin GVIA

A benzothiazole-derived compound (4a) designed to mimic the C α-Cβ bond vectors and terminal functionalities of Lys2, Tyr13 and Arg17 in ω-conotoxin GVIA was synthesised, together with analogues (4b-d), which had each side-chain mimi

Antineoplastic α-methylene-γ-butyrolactones

The present invention provides antineoplastic α-methylene-γ-butyrolactones represented by the general formula ?I! wherein R1 is a phenyl group optionally substituted with one or two groups selected from the group consisting of halide, (C1

Molecular encapsulation: Cyclodextrin-based analogues of heme-containing proteins

The active site heme prosthetic group of such species as hemoglobin, the cytochrome P-450s, and the peroxidases is enveloped within a protective hydrophobic environment located adjacent to a binding site for exogeneous compounds. In addition to providing

1,2,4-TRIAZOLE-3,5-DIAMINE DERIVATIVES

The invention relates to compounds of the formula (I) STR1 and physiologically acceptable salts, hydrates and bioprecursors thereof, in whichR 1 and R 2 represent hydrogen, an aliphatic or cycloaliphatic group, or R 1 and R 2 together with the nitrogen atom form a 5 to 10 membered heterocyclic ring:Alk represents a straight or branched alkylene chain;Q represents furan, thiophen or benzene ring which is incorporated into the rest of the molecule; X represents--CH 2--, STR2--O--or--S--where R 6 represents hydrogen or methyl;n represents zero, 1 or 2; m represents 2, 3 or 4;R 3 represents hydrogen, a substituted or unsubstituted aliphatic or aryl group and;R 4 and R 5, which may be the same or different, each represent hydrogen, a substituted or unsubstituted aliphatic, aryl, or together with the nitrogen atom form a heterocyclic group.