A series of novel organic ligands, 5-(4-oxo-4H-chromen-3-yl)-4,5-dihydro-1,3,4-thiadiazole-2-carboxamide, which are the tautomeric forms of 2-oxo-2-(arylamino)-(2E)-2- [(4-hydroxy-2-oxo-2H-1-benzopyran-3-yl)-methyledene]ethanethioic acid hydrazides, have been synthesized from 3-formylchromone an...

The synthesis of 6-aryl, 8- aryl, and 8-aryl-6-chloro-2-morpholino-1,3-benzoxazines with potent activity against PI3K and DNA-PK is described. Synthesis of thirty one analogues was facilitated by an improved synthesis of 3-bromo-2-hydroxybenzoic acid 13 by de-sulphonation of 3-bromo-2-hydroxy-5-...

Novel pyrazolo[1,5-a]pyridine derivatives were designed, synthesized and evaluated as orally active EP1 antagonists for the treatment of overactive bladder. Matched molecular pair analysis (MMPA) allowed the design of a new series of pyrazolo[1,5-a]pyridine derivatives 4–6. Structure-activity r...

A novel pyridine based polymer (PAPY) bearing typical bis(2-pyridylmethyl)amine and additional amino groups was newly prepared with much lower cost (46.5 USD/kg) than commercial resins with bis(2-pyridylmethyl)amine functional groups such as M4195 and TP220 (134.6 USD/kg). PAPY is a weakly basic...

In the present work, structural studies on 2-chloromethyl-1H-benzimidazole hydrochloride have been performed extensively by X-ray crystallography, 1H NMR, FT-IR, UV/vis, and elemental analysis. The title compound crystallizes in a monoclinic space group P21/c with a = 7.1982 (3) Å, b = 9.4513 (5...

BackgroundVarious cytochrome P450 isoforms modulate sibutramine activity and influence sibutramine plasma levels and pharmacokinetics. However, there are no available data to demonstrate the association of these polymorphisms with the clinical outcomes of sibutramine administration.

β-Cyclodextrin (β-CD) is widely used to increase the stability, solubility, and bioavailability of poorly soluble drugs because of the appropriate size of its cavity. Sibutramine is a neurotransmitter reuptake inhibitor that has been investigated as an oral anorexiant. Here we report the compl...

The effects of acute treatment with sibutramine on the peripheral sympathetic neurotransmission in vas deferens of young rats were still not evaluated. Therefore, we carried out this study in order to verify the effects of acute sibutramine treatment on the neuronal- and exogenous agonist-induce...

Sibutramine is one of the most occurring adulterants encountered in dietary supplements with slimming as indication. These adulterated dietary supplements often contain a herbal matrix.When customs intercept these kind of supplements it is almost impossible to discriminate between the legal prod...

Solubility data from sibutramine (SBA) in a family of alcohols were obtained at different temperatures. Sibutramine was characterized by using thermal analysis and X-ray diffraction technique. Solubility data were obtained by the saturation method. The van’t Hoff equation was used to obtain the...

Sibutramine is one of the most widespread adulterants encountered in herbal formulations or dietary supplements used for weight-loss purposes. In this work, a simple and portable square-wave voltammetric (SWV) method was proposed for fast screening and quantification of sibutramine in herbal for...

Overdose administration of sibutramine, a serotonin-noradrenalin reuptake inhibitor, is considered to elicit severe side effects including hypertension, whose pathogenic mechanism remains unclear. Here, we found that 48-h incubation with > 10 μM sibutramine provokes apoptosis of human aortic en...

Sibutramine hydrochloride monohydrate is a weight loss agent indicated for the treatment of obesity. Although it has been banned from most markets, studies are still relevant as it is often a hidden ingredient in herbal and over the counter slimming products. Sibutramine induces liver fibrosis w...

Sibutramine may be illicitly included in herbal slimming foods and supplements marketed as “100% natural” to enhance weight loss. Considering public health and legal regulations, there is an urgent need for effective, rapid and reliable techniques to detect sibutramine in dietetic herbal foods...

Sibutramine had been prescribed as an oral anorexiant that reduces dietary intake, but was withdrawn from the market due to frequent occurrence of severe cardiovascular events including hypertension. To elucidate the pathogenic mechanism of hypertension, we here investigated whether sibutramine ...

Novel vitamin D3 derivatives, 26 − homo − Δ22 − 1α25(S)-dihydroxyvitamin D3 and 26-homo-Δ22-1α25(R)-dihydroxyvitamin D3 were compared with the native hormone, 1,25-dihydroxyvitamin D3, and with other vitamin D3 derivatives, in inhibition of cell growth, induction of phenotypic differentiatio...

1,25-Dihydroxyvitamin D3 (1,25-(OH)2D3) greatly enhances sodium butyrate (NaB)-induced enterocyte differentiation of HT-29 human colonic carcinoma cells while 1,25-(OH)2D3 alone induces growth restriction without associated differentiation. In the present study, the efficacies of various analogs...

We synthesized 25-hydroxy-26,27-dimethylvitamin D3, 9, and 1,25-dihydroxy-26,27-dimethylvitamin D3,14, from chol-5-enic acid-3β-ol and tested their biological activity in vivo and in vitro. 9 was found to be a highly potent vitamin D analog with bioactivity similar to that of 25-hydroxyvitamin ...

HPLC analysis of the roots of Cynanchum otophyllum Scheind (Asclepiadaceae) led to the isolation of six new pregnane glycosides, specifically otophyllosides N-P (2–4) and otophyllosides Q-S (7–9), in addition to the identification of three known C-21 steroidal glycosides, otophylloside A (1), ...

The orf virus is the type species of the Parapoxvirus genus and is the causative agent of contagious echtyma, a debilitating skin disease of sheep and goats, which can also affect man. The virus exhibits a restricted host range, even if it has been shown to bind to a wide range of tissues of non...