Month: November 2022

Milchev, Boyan published the artcileDiet of Barn Owl Tyto alba in central South Bulgaria as influenced by landscape structure, Category: imidazoles-derivatives, the main research area is diet Barn Owl landscape feeding ecol central South Bulgaria.

This study of the diet of Barn Owl Tyto alba analyzed pellets containing 18,810 prey specimens. Small mammals (98.2% by number, 97.5% by biomass) dominated, while birds, reptiles, amphibians, and insects constituted a negligible portion of the diet (1.8% by number, 2.5% by biomass). Voles (Microtus spp.) were the most numerous prey (35.3 ± 14.4%, range 14.6%-67.1%) in 9 localities (69.2%, n = 13 individually studied localities) and dominated the biomass in all diets (51.4 ± 14.1%, range 27.4%-78.2%). The lesser white-toothed shrew (Crocidura suaveolens) (20.8 ± 7.6%, range 7.3%-32.8%) was the most frequent prey in the other 4 localities (30.8%). The breeding localities with more similar proportions of habitats in their hunting territories had significantly higher diet overlaps (r = 0.336, P < 0.01). The amount of wetlands and the indexes of habitat heterogeneity and topog. relief among the landscape characteristics of the hunting territories significantly influenced diet composition according to redundancy anal. Larger areas of wetlands correlated with higher predation on wetland mammal species, as well as the European pine vole (Microtus subterraneus) and white-toothed shrews, and thus with broader food niche breadth. Turkish Journal of Zoology published new progress about Amphibia. 274-78-2 belongs to class imidazoles-derivatives, name is Imidazo[1,2-c]pyrimidine, and the molecular formula is C6H5N3, Category: imidazoles-derivatives.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Kim, Mi Kyoung published the artcile3D-QSAR of PET agents for imaging β-amyloid in Alzheimer’s disease, SDS of cas: 1023-01-4, the main research area is beta amyloid PET imaging agent QSAR model; thioflavin stilbene derivative amyloid plaque imaging QSAR.

The accumulation of excess senile plaques (β-amyloid, Aβ-plaques) in the brain is strongly associated with the pathogenesis of Alzheimer’s disease (AD). While there are no definitive treatments available to affect a cure of AD, much recent interest has been given to the development of antiamyloid therapies aimed at halting and reversing Aβ-deposition and, thus, monitoring of the therapeutic efficacy would greatly benefit from methods for the in vivo detection and quantification of Aβ-deposits in the brain. A 3D-QSAR model was constructed with several PET ligands such as Thioflavin-T analogs and stilbene derivatives using CoMFA (Comparative Mol. Field Anal.) and CoMSIA (Comparative Mol. Similarity Indexes Anal.). The 3D-QSAR model could be applied to predict binding affinity of the structurally related compounds against Aβ-plaques.

Bulletin of the Korean Chemical Society published new progress about Affinity. 1023-01-4 belongs to class imidazoles-derivatives, name is 2-(4-Bromophenyl)-6-methylimidazo[1,2-a]pyridine, and the molecular formula is C14H11BrN2, SDS of cas: 1023-01-4.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Morita, Kunihiko published the artcileInhibition of testosterone biosynthesis in testicular microsomes by various imidazole drugs. Comparative study with ketoconazole, Recommanded Product: 4-((1H-Imidazol-1-yl)methyl)benzoic acid, the main research area is testosterone formation testis microsome imidazole.

Ketoconazole (KCZ), an imidazole-containing antimycotic, has been demonstrated to inhibit testosterone biosynthesis in man. In this study, the inhibitory activities of various imidazole drugs such as miconazole (MCZ), cimetidine (CIM), ozagrel (OZA) and its metabolites (M-1 and M-2) on the pathway of testosterone biosynthesis in testicular microsomes were compared with that of KCZ in vitro. Addnl., the changes in serum testosterone level in the patients by the treatments with MCZ were followed. KCZ inhibited 17α-hydroxylase and C17,20-lyase activities in a dose-dependent manner, while it did not affect 17β-hydroxysteroid dehydrogenase activity. Although the patterns of the inhibitory actions and the interaction of either imidazole drugs with cyclochrome P 450 as 17α-hydroxylase and C17,20-lyase were similar to those of KCZ, the inhibitory potencies and affinities for the cytochrome P 450 system decreased in the order of KCZ > MCZ > OZA > M-2 > M-1 > CIM. At the end of the i.v. injection of 200 mg MCZ to the patients, the serum testosterone levels decreased by about 16% of the original level and then returned to the original level 5 h after the end of injection. These results indicate that either imidazole drugs tested could inhibit a cytochrome P 450 enzyme C17,20-lyase mainly in testicular microsomes, and suggest that MCZ, a potent inhibitor subsequent to KCZ, induces a slight alteration in the testosterone biosynthesis in its clin. use.

Journal of Pharmacobio-Dynamics published new progress about Microsome. 94084-75-0 belongs to class imidazoles-derivatives, name is 4-((1H-Imidazol-1-yl)methyl)benzoic acid, and the molecular formula is C11H10N2O2, Recommanded Product: 4-((1H-Imidazol-1-yl)methyl)benzoic acid.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Ogiso, Taro published the artcilePharmacokinetics of ozagrel and its metabolites after intravenous and oral administrations, Application In Synthesis of 94084-75-0, the main research area is ozagrel metabolism pharmacokinetics liver intestine.

The pharmacokinetics of ozagrel, a selective thromboxane A2 synthetase inhibitor, and its metabolites M1 [p-(1H-imidazol-1-ylmethyl)benzoic acid] and M2 [3-[p-(1H-imidazol-1-ylmethyl)phenyl]-2-propionic acid] were investigated in rats. The plasma concentration-time profile of ozagrel was biexponential, with a rapid terminal decay (t1/2b = 0.173 and 0.160 h after doses of 15 and 45 mg/kg, resp.). Metabolites M1 and M2 appeared in plasma immediately after i.v. administration of the parent drug. Similar patterns of metabolites were observed in plasma after oral administration, although concentrations of M2 were higher than those of M1, indicating the metabolic conversion of ozagrel to M2 and M1. However, a saturable 1st-pass clearance was seen after a high oral dose (60 mg/kg) of ozagrel. When M2 was administered i.v., M1 appeared in the circulation at appreciable levels, providing evidence of metabolic conversion of M2 to M1 in the systemic circulation. Ozagrel was partly metabolized to M2 and M1 in rat intestinal mucosa, although the main metabolic site might be in the liver. The results indicate that the metabolic pathway of ozagrel in rats is the conversion of the parent drug to M2 and M1 and the conversion of M2 to M1.

Journal of Pharmaceutical Sciences published new progress about Intestine. 94084-75-0 belongs to class imidazoles-derivatives, name is 4-((1H-Imidazol-1-yl)methyl)benzoic acid, and the molecular formula is C11H10N2O2, Application In Synthesis of 94084-75-0.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Fichert, Thomas published the artcileA structure-Permeability study of small drug-like molecules, Application In Synthesis of 94084-75-0, the main research area is tetrazole permeability MSPR.

A systematic structure-permeability relationship study on a set of small drug-like mols. with log D values in the range -2.5 to 3 and carrying a diverse array of functionality reveals that the compounds with log D>0 and <3 are highly permeable. Surprisingly, several tetrazole derivatives were found to be substrates for efflux pump(s). Bioorganic & Medicinal Chemistry Letters published new progress about Diffusion. 94084-75-0 belongs to class imidazoles-derivatives, name is 4-((1H-Imidazol-1-yl)methyl)benzoic acid, and the molecular formula is C11H10N2O2, Application In Synthesis of 94084-75-0.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Zhao, Yaohong published the artcileApplication of molecular probe to investigate surface structure of metal passivator on copper, Recommanded Product: Methyl 1H-benzo[d]imidazole-2-carboxylate, the main research area is copper sulfide surface structure metal passivator investigative.

Copper sulfide (Cu2S) contaminant is semi-conductive. Its formation and migration to insulating paper and oil caused insulation breakdown. Addition of benzotriazole derivatives as metal passivator slows down the corrosion process, as the metal passivator produces a protective layer on the copper surface, which prevents the reaction between corrosive sulfur and copper. But the surface structure of this impermeable film is still unknown. Herein we reported our investigation on the orientation of metal-passivator complex on copper surface by means of mol. probe. Ageing exptl. study with different steric and electronic groups in benzotriazole skeleton indicated that the second position of the mol. was sensitive to steric effect, suggesting end-on orientation preferable. Subsequently, SEM-EDX revealed the relative amount of copper sulfide on copper surface. Moreover, FTIR represented the characteristic wavenumber of C=O, C=N moiety and benzene skeleton of passivator-copper complex. XPS anal. delivered the organic elemental composition of the protective layer.

IEEE Transactions on Dielectrics and Electrical Insulation published new progress about Corrosion. 5805-53-8 belongs to class imidazoles-derivatives, name is Methyl 1H-benzo[d]imidazole-2-carboxylate, and the molecular formula is C9H8N2O2, Recommanded Product: Methyl 1H-benzo[d]imidazole-2-carboxylate.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Wu, Qiongyou published the artcileSynthesis and characterization of potential photolabeling probes for studying the antiviral mechanisms of EICAR, Recommanded Product: 5-Amino-1-methyl-1H-imidazole-4-carboxamide, the main research area is diazoniumribofuranosylimidazole azidoribofuranosylimidazole carboxamide nucleoside preparation azidolysis nucleophilic substitution photolysis.

The designed photo-labeling probes: 5-diazonium-1-β-D-ribofuranosyl-1H-imidazole-4-carboxamide (I) and 5-azido-1-β-D-ribofuranosyl-1H-imidazole-4-carboxamide (II) were synthesized via a short and convenient synthetic route, namely by diazotizing AICAR and subsequently performing substitution with NaN3. Although I was not stable even at low temperatures, II showed a rapid and clean photochem. reaction, which suggests that it may be a valuable tool for use in photo-labeling studies.

Heterocycles published new progress about Azidation. 21343-04-4 belongs to class imidazoles-derivatives, name is 5-Amino-1-methyl-1H-imidazole-4-carboxamide, and the molecular formula is C5H8N4O, Recommanded Product: 5-Amino-1-methyl-1H-imidazole-4-carboxamide.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Robinson, Henry published the artcileLate-Stage Functionalization by Chan-Lam Amination: Rapid Access to Potent and Selective Integrin Inhibitors, Synthetic Route of 30086-17-0, the main research area is naphthyridinylpentanamide arylpropanoic acid boronate Chan Lam amination; aminophenylpropanoic tetrahydro naphthyridinylpentanamide preparation integrin inhibitor idiopathic pulmonary fibrosis; C−N coupling; integrin antagonists; late-stage functionalization; medicinal chemistry; β-amino acids.

A late-stage functionalization of the aromatic ring in amino acid derivatives was described. The key step was a copper-catalyzed diversification of a boronate ester I (X = 4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl; R1 = Boc; R2 = t-Bu) by amination (Chan-Lam reaction) that can be carried out on a complex β-aryl-β-amino acid scaffold. This not only considerably extended the substrate scope of amination partners, but also delivered an array of potent and selective integrin inhibitors I (X = 1-pyrazolyl, 4-chloro-1-imidazolyl, 1-piperidinyl, 1,4-oxazepan-4-yl, etc.; R1 = R2 = H) as potential treatment agents of idiopathic pulmonary fibrosis (IPF). This versatile chem. strategy, which was amenable to high-throughput-array protocols, allows the installation of pharmaceutically valuable heteroaromatic fragments at a late stage by direct coupling to NH heterocycles, leading to compounds with drug-like attributed.

Chemistry – A European Journal published new progress about Amination. 30086-17-0 belongs to class imidazoles-derivatives, name is 5-Fluoro-1H-imidazole, and the molecular formula is C3H3FN2, Synthetic Route of 30086-17-0.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Melo, M. J. published the artcilePhotochemistry of 2-(2-furyl)benzimidazole (Fuberidazole), COA of Formula: C9H8N2O2, the main research area is photolysis furylbenzimidazole; benzimidazole furyl photolysis; Fuberidazole photolysis.

The photodegradation of 2-(2-furyl)benzimidazole (Fuberidazole) has been reinvestigated employing advanced HPLC-UV/VIS technique and fluorescence emission and excitation spectroscopy in methanol at natural pH, in acidic medium and in aqueous solutions at pH 7 and 3; four main products, benzimidazole-2-carboxylic acid, its Me ester, 1-methoxybenzimidazole, and Me 4-oxo-2-benzimidazolecrotonate (cis and trans isomers), besides benzimidazole and 2,2′-bibenzimidazole and other side products, have been isolated and characterized. The kinetics of the photodegradation process were followed independently by HPLC-UV and fluorescence emission and showed significant similarity; this allowed monitoring of a photodegradation at very low concentrations (5 × 10-5-5 × 10-6 M). The quantum yield of disappearance of Fuberidazole has been determined

Zeitschrift fuer Naturforschung, B: Chemical Sciences published new progress about Photolysis. 5805-53-8 belongs to class imidazoles-derivatives, name is Methyl 1H-benzo[d]imidazole-2-carboxylate, and the molecular formula is C9H8N2O2, COA of Formula: C9H8N2O2.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Yeh, Herman J. C. published the artcileFluorine-19 and proton nuclear magnetic resonance studies of ring-fluorinated imidazoles and histidines, Safety of 5-Fluoro-1H-imidazole, the main research area is imidazole fluoro NMR ionization; histidine fluoro NMR ionization; NMR fluoroimidazole fluorohistidine ionization.

1H and 19F titration curves in D2O and H2O, resp., were obtained for 2- and 4-fluoroimidazole and -histidine. Dissociation pK values were determined by computer-assisted curve fitting. Fluoroimidazoles are weaker bases and stronger acids than bromoimidazoles showing that the inductive effect of the halogen overshadows its resonance effect. Introduction of an alkyl group at C-5 displaces the F-4 and F-2 signals upfield and downfield, resp., indicating C-4 and C-5 are coupled by induction and resonance whereas C-2 and C-5 are coupled by induction only. Introduction of F displaces the H-2 and H-4 signals upfield. The shielding effect of the magnetic anisotropy of 19F counteracts the deshielding effect of its electronegativity. Protonation of the imidazole ring displaces the F-2 and F-4 signals downfield and upfield, resp., the same effect was observed in the imidazole anion. The amino acid side chain charge caused field perturbation of the 19F signal in fluorohistidines.

Journal of the Chemical Society, Perkin Transactions 4: Physical Organic Chemistry published new progress about Ionization. 30086-17-0 belongs to class imidazoles-derivatives, name is 5-Fluoro-1H-imidazole, and the molecular formula is C3H3FN2, Safety of 5-Fluoro-1H-imidazole.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem