In organic synthesis and polymer materials chemistry, a tert-butoxycarbonyl (BOC) group is often used as one of tools for the protection of functional groups. In this study, we carried out radical polymerization of 2-(tert-butoxycarbonyloxy)ethyl methacrylate (BHEMA) and copolymerizations of BHE...

Reaction of Mn(NCS)2 and Cd(NCS)2 with 4-(Boc-amino)pyridine leads to the formation of compounds of composition M(NCS)2(4-(Boc-amino)pyridine)4 (M = Mn, 1-Mn; Cd, 1-Cd) and (M(NCS)2(4-(Boc-amino)pyridine)2 (M = Mn, 2-Mn; Cd, 2-Cd). 1-Cd and 1-Mn, respectively 2-Cd and 2-Mn are isotypic and their...

The asymmetric syntheses of methyl N-Boc-2-deoxy-2-amino-l-erythroside and methyl N-Boc-2-deoxy-2-amino-d-threoside have been achieved from sorbic acid, in six and eight steps, and in 35 and 13% overall yield, respectively. Diastereoselective aminohydroxylation of tert-butyl sorbate gives access...

A simple and efficient synthetic strategy to all four enantiomerically pure diethyl 1,2-di(N-Boc-amino)propylphosphonates has been elaborated starting from the corresponding N-[(R)-(1-phenylethyl)]aziridine-(2S)- and N-[(S)-(1-phenylethyl)]aziridine-(2R)-carboxaldehydes, employing a one-pot thre...

The Ysc–Yop type III secretion (TTS) system allows extracellular Yersinia bacteria, adhering to eukaryotic target cells, to inject Yop effector proteins in the cytosol of these cells. The secretion apparatus, called the injectisome, ends up with a needle-like structure made of YscF. YopN, one o...

.Liposome-encapsulated hemoglobin (LEH) has been developed as a blood substitute. In spite of its size (1/30 – 1/40 of erythrocytes), LEH has an oxygen-carrying capacity comparable to erythrocytes. Thus, LEH is expected to carry oxygen into vital organs via collateral routes during ischemia ind...

We performed this study to elucidate whether a newly developed liposome-encapsulated hemoglobin, TRM-645 (TRM), can prevent cerebral dysfunction resulting from acute ischemic stroke when used as an oxygen carrier. Hippocampal long-term potentiation (LTP) in the perforant path–dentate gyrus syna...

ObjectiveTo examine the relationship between the increase of glycated haemoglobin A1c (HbA1c) levels and the risk of preeclampsia in pregnant with type 1 diabetes mellitus; and to determine from which trimester the increase of HbA1c levels better predicts the risk of suffering preeclampsia in ty...

Oxazoline-amino acids (Xaa-Ozn) occur in natural peptides of potentially important bioactivity. The conformations of the model compounds: Ac-(S)-Ala-Ozn(4R-Me), Ac-(S)-Ala-Ozn(4S–Me), and (gauche+, gauche−, anti) Ac-(S)-Val-Ozn(4R-Me) were studied at meta-hybrid M06-2X/6–311++G(d,p) method inc...

Safe and inexpensive methods for synthesis of a series of four substituted 2,4,6-triphenylyrylium tosylate salts with different substituents are reported. The synthesis methods use p-toluenesulfonic acid monohydrate instead of conventional acid catalysts including perchloric acid or boron triflu...

Homogeneous catalytic dehydration of sorbitol to isosorbide has been performed with a series of metal tosylates as catalysts. Conversions up to 100 % and selectivities into isosorbide up to 67% were obtained with Bi(OTs)3. The metals were exchanged with acidic sites of sulfonic resins and the re...

We evaluated the long-term effects of withdrawal of a newer third-generation bisphosphonate, incadronate disodium (YM175), on both cancellous and cortical bone mass and strength in ovariectomized (OVX) rats. One hundred and sixty female SD rats at 13 weeks of age were randomized into four groups...

Purpose. Total gastrectomy (GX) leads to osteopenia. We examined the effects of bisphosphonate incadronate (INC), a potent inhibitor of bone resorption, on bone characteristics in rats that underwent total GX. Experimental design. Male Wistar rats were divided into four groups: (1) sham-operatio...

Mineral density of trabecular bone at the metaphyses of right tibiae was measured by peripheral quantitative computed tomography (pQCT) in ovariectomized rats. Bone mineral density (BMD) decreased dramatically in the 4 weeks following ovariectomy, suggesting that the method is sensitive enough t...

ObjectivesTo evaluate prophylactic effects of bisphosphonate (BP) on skeletal lesions induced by prostate cancer (CaP).

Incadronate is a highly effective inhibitor of stimulated bone resorption as demonstrated in a hypercalcemia model in rats, bone metastasis models in mice and rats, and an osteoporosis model in dogs. In this study, the effect of incadronate on osteoporosis in ovariectomized rats was examined. In...

Bone metastasis is an important cause of morbidity in advanced prostate cancer. Bisphosphonates are widely used for the treatment and prevention of osteoporosis, but recently have been observed to be effective in controlling prostate cancer metastasis. Since aminopeptidase N (AP-N) is known to b...

We have previously shown that advanced glycation end products (AGE), senescent macroprotein derivatives formed at an accelerated rate in diabetes, induced angiogenesis through overgeneration of autocrine vascular endothelial growth factor (VEGF). In the present study, effects of incadronate diso...

A novel one-pot synthesis of sydnones appended to coumarins (4a–r) via thiazole in presence of silica sulfuric acid as a heterogeneous catalyst is discussed. The use of low cost and reusable silica sulfuric acid as catalyst makes this process feasible and convenient. Further, the title compound...

A novel series of cholecystokinin-2 receptor (CCK-2R) antagonists has been identified, as exemplified by anthranilic sulfonamide 1 (pKi = 7.6). Pharmacokinetic and stability studies indicated that this series of compounds suffered from metabolic degradation, and that both the benzothiadiazole an...