Coenzyme CoQ10 (CoQ10), a ubiquinone compound, has been reported to inhibit tyrosinase activity and melanin production in melanoma B16F10 cells. However, the molecular mechanism underlying this inhibitory effect is poorly understood. In this paper we aimed to investigate the molecular mechanisms...

The adrenocorticotropic hormone (ACTH) receptor, known as the melanocortin-2 receptor (MC2R), plays a key role in regulating adrenocortical function. MC2R is a subtype of the melanocortin receptor family and ACTH is only agonist for MC2R. Our previous result indicates that ACTH1-17 is the minima...

α-melanocyte stimulating hormone (α-MSH) is a member of the melanocortin family, that has displayed important biological functions in diverse cells and tissues. The purpose of this study is to test the effect of α-MSH on the differentiation and mineralization of osteoblast cells. The expressi...

GPR139 is an orphan G protein-coupled receptor that is expressed primarily in the brain. Not much is known regarding the function of GPR139. Recently we have shown that GPR139 is activated by the amino acids l-tryptophan and l-phenylalanine (EC50 values of 220 μM and 320 μM, respectively), as ...

The central melanocortin system is composed of neurons that express either the proopiomelanocortin (POMC) or the agouti-related protein (AgRP). POMC is cleaved in bioactive peptides, including the α-melanocyte-stimulating hormone (α-MSH). α-MSH activates the melanocortin-4 receptor (MC4R) ind...

ObjectiveThe lack of pro-opiomelanocortin (POMC)-derived melanocortin peptides results in hypoadrenalism and severe obesity in both humans and rodents that is treatable with synthetic melanocortins. However, there are significant differences in POMC processing between humans and rodents, and lit...

Quinazoline-containing derivatives are an important class of synthetic products and represent an attractive scaffold for EGFR inhibitors. A series of oxazolo[4,5-g]quinazolin-2(1H)-one derivatives were synthesized and the EGFR and Src inhibition activities were evaluated using Gefitinib as lead ...

In this study, a series of novel 7 or 8-substituted 4-morpholine-quinazoline derivatives was designed and synthesized. Their PI3Kα inhibitory activities, antiproliferative activities against seven cancer cell lines, namely, PC-3, DU145, MCF-7, BT474, SK-BR-3, U937 and A431, were evaluated in vi...

During random screening of a small in-house library of compounds, certain substituted imidazo[1,2-a]pyridines were found to be weak allosteric inhibitors of HIV-1 reverse transcriptase (RT). A library of these compounds was prepared using the Groebke reaction and a subset of compounds prepared f...

A one-pot multigram synthesis of 3-(trifluoromethyl)-1H-pyrazolo[3,4-b]pyridine starting from 2-fluoropyridine using directed ortho metallation (DoM) technique is described. The compound contains an anionically activatable trifluoromethyl group and is a versatile building block for the microwave...

Publisher SummaryThis chapter discusses the description, methods of preparation, physical properties, solution-phase stability, and methods of analysis of procaine hydrochloride. Procaine is a derivative of p-aminobenzoic acid, and is a one of the oldest used ester-type local anesthetic agents. ...

The densities and viscosities of tri-n-propylamine hydrochloride, tri-n-butylamine hydrochloride, tri-n-pentylamine hydrochloride, tri-n-hexylamine hydrochloride, tri-n-heptylamine hydrochloride, tri-n-octylamine hydrochloride, tri-n-decylamine hydrochloride and tri-n-dodecylamine hydrochloride ...

Adduct formation of Cu(chelate)2 (chelate = anion of thenoyltrifluoroacetone, TTA, and trifluoroacetylacetone, TFA) with alkylamines and alkylamine hydrochlorides, S (S = tri-n-butylamine, TBA, tri-n-hexylamine, THA, tri-n-octylamine, TOA, tri-n-laurylamine, TLA, tri-n-hexylamine hydrochloride, ...

Formation of Schiff bases of n-hexylamine with 5'-deoxypyridoxal in water-dioxan mixtures (0, 50, 70 and 100% dioxane vv) have been studied by kinetic methods. The formation and the hydrolysis rate constants, the equilibrium constants and the pK values have been measured at 25 ° and 0.1 M ...

Assay and electrochemical behaviour of betahistine hydrochloride in Britton–Robinsons (BR) buffer of pH range 2.5–12.0 at a glassy carbon electrode have been investigated. Addition of anionic surfactant (sodium lauryl sulphate) to the betahistine hydrochloride solution containing electrolyte e...

A series of novel terminal trimethylsilylacetylene benzoate derivatives with various linking groups were synthesized using Friedel-Craft's O-acylation reaction. The chemical structures of the novel 4-[2-(trimethylsilyl)ethynyl]benzoates were confirmed by standard spectroscopic techniques. T...

Protein translocation is essential for bacterial survival and the most important translocation mechanism is the secretion (Sec) pathway in which SecA is a central core driving force. Thus targeting SecA is a promising strategy for developing novel antibacterial therapeutics. Herein, we report th...

Bcl-2 family proteins play a vital role for cancer cell in escaping apoptosis, and small-molecule anti-apoptotic Bcl-2 protein inhibitors have been developed as new anticancer therapies. In current study, a series of substituted 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid derivatives were d...

A number of new nitric oxide (NO)-precursors were synthesized by grafting nitrate-containing moieties on the structures of the benzyloxy isonipecotanilide derivatives 1 and 2 already reported as moderately potent antiplatelet agents. Various nitrooxy (ONO2)-alkyl side chains were covalently link...

A new series of N-[5-(4-(alkyl/aryl)-3-nitro-phenyl)-[1,3,4-thiadiazol-2-yl]-2,2-dimethyl-propionamide 4 (a–l) and 6-(4-Methoxy-phenyl)-2-(4-alkyl/aryl)-3-nitro-phenyl)-Imidazo [2,1-b] [1,3,4] thiadiazole 6 (a–l) were synthesized starting from 5-(4-Fluoro-3-nitro-phenyl)-[1,3,4] thiadiazole-2-...