A facile three-step synthetic route toward 1,3-diaryl-1H-benzo[g]indazoles 1a–1n starting with 3,4-dimethoxy-2-allylbenzaldehyde (6) in modest total yield is described. The facile route was carried by aldol condensation of aldehyde 6 with aryl methyl ketones 5a–5d in alkaline MeOH at reflux, K...

Indoleamine 2,3-dioxygenase 1 (IDO1)-mediated kynurenine pathway of tryptophan degradation is identified as an important immune effector pathway in the tumor cells to escape a potentially effective immune response. IDO1 is an attractive target for anticancer therapy and the discovery of IDO1 inh...

Indoleamine 2,3-dioxygenase 1 (IDO1) and tryptophan 2,3-dioxygenase (TDO) are constitutively overexpressed in many types of cancer cells and exert important immunosuppressive functions. In this article, a series of 4,6-substituted-1H-indazole derivatives were synthesized and evaluated the inhibi...

Sodium-glucose cotransporter 1 (SGLT1) is the primary transporter for glucose absorption from digested nutrients in the gastrointestinal tract. Intestinal SGLT1 inhibition reduces post-prandial hyperglycemia and enhances the increase of plasma glucagon-like peptide-1 (GLP-1) levels. SGL5213 is a...

SummaryA set of sixteen para-substituted N,N-[(dimethylamino)ethyl] benzoate hydrochlorides structurally related to procaine was synthesized. The apparent partition coefficients were determined by either shake-flask or HPLC methods and were taken as hydrophobic parameters. The IR stretching freq...

BRS-3 has an important role in glucose homeostasis. Its expression was reduced in skeletal muscle from obese and/or diabetic patients, and BRS-3 KO-mice developed obesity. In this work, focused on rat/human adipose tissue, BRS-3 gene-expression was lower than normal-levels in hyperlipidemic, typ...

The reductive aminolysis of glucose with dimethylamine (DMA) as aminating agent has been investigated experimentally as well as via kinetic model construction. A fed-batch reactor configuration was used at following conditions: temperatures ranging between 383 K–398 K, total pressures from 6.0 ...

The main aim of this work was to synthesise a novel 1-(3-(N,N-dimethylamino)-1-(5-substituted thiophene-2-yl)propylidene semicarbazone Mannich base derivatives and examine the anti-diabetic and anti-inflammatory activities using alloxan-induced diabetic and carrageenan-induced paw oedema methods...

Glycogen synthase kinase 3β (GSK-3β) is a widely investigated molecular target for numerous diseases including Alzheimer’s disease, cancer, and diabetes mellitus. Inhibition of GSK-3β activity has become an attractive approach for treatment of diabetes and cancer. We report the discovery of ...

Taking advantage of microwave-assisted synthesis, efficient and expedite procedures for preparation of a library of fusaric acid and 39 analogues are reported. The fusaric acid analogues were tested in cell-based screening assays for inhibition of the las and rhl quorum sensing system in Pseudom...

In this communication, we account the synthesis, spectroscopic, crystal structure, and photophysical and DFT studies of N-phenylthiazole-5-carboxamide derivatives. Synthesis of N-arylthiazole-5-carboxamideswas obtained using eco-friendly conditions. Two compounds were synthesized with high yield...

A palladium-catalyzed N-arylation of 1-substituted-1H-tetrazol-5-amines has been described for the first time. The reaction provides good yields of desired products with broad substrate scope and good functional group tolerance.

A Cu-mediated ligand-free arylation of NH-sulfoximines and sulfonamides by arylhydrazine hydrochlorides was herein demonstrated. The oxidative transformation provided an easy access towards N-aryl sulfoximines and sulfonamides in high yields (up to 93% yields) with broad functional groups tolera...

ObjectiveInvasive microorganisms and free radicals are responsible for the delayed healing of various infections. It is necessary to discovery of novel molecules that are effective against invasive microorganisms and inhibit free radicals. Therefore, a series of metal complexes of 2-amino-4-subs...

Novel [n]benzofuranophanes (n = 8 & 10) 2a–b have been prepared by successive intramolecular cyclization from 5,19-di-tert-butyl-8,22-dimethoxy[n]metacyclophane-1-yne (syn-1a–b) by treatment with BBr3 in CH2Cl2 at room temperature for 8h. [2.n]Benzofuranophanes 2a–b were also obtained by trea...

A highly reactive intermediate N-sulfonyl acetylketenimine was generated from an ynone-participated CuAAC/ring-opening method. Its unique structure allowed it to react with aryl carboxylic acids to give N-aroylsulfonamides via a novel Mumm-type rearrangement.

Anodic methoxylation and acetoxylation reactions of five membered cyclic sulfides such as thiazolidines, 1,3-oxathiolanes and 1,3-dithiolanes, which have been reported to not always undergo the Pummerer reaction, were successfully carried out by using a fluoride ion mediator.

Recently,ionic liquids (ILs) functionalized cyclodextrins (CDs) have attracted more and more attention in the fields of enantioseparation. In this study, a novel IL amino triazolium functionalized β-CD derivative, mono-6-deoxy-6-(4-amino-1,2,4-triazolium)-β-cyclodextrin chloride (4-ATMCDCl), w...

RNA interference (RNAi) is an evolutionarily conserved gene-silencing phenomenon that shows great promise for developing new therapies. However, the development of small interfering RNA (siRNA)-based therapies need to establish efficient delivery system that silences target genes with siRNA dose...

Aromatic nucleophilic substitution reactions in 1-halo-3,5-dinitrobenzenes (where the halogen is bromine or chlorine) can occur with replacement of either a nitro group or a halogen atom, depending on the nature of anionic nucleophile Nu– as a Lewis base (hard, soft or intermediate), as well as...