Design, synthesis and evaluations of spiro-fused benzoxaborin derivatives as novel boron-containing compounds.

07:00 EST 5th February 2019 | BioPortfolio

Summary of "Design, synthesis and evaluations of spiro-fused benzoxaborin derivatives as novel boron-containing compounds."

Drug design using boron-containing heterocycles has attracted a great deal of attention because these compounds are believed to possess high biological activity. However, information on the synthetic methodology and pharmacokinetic profiling of boron-containing compounds is limited. In this study, we provide a new synthetic route for preparation of spiro-fused benzoxaborin derivatives and investigate their in vitro pharmacokinetic properties. Our efforts led to the successful construction of a chemical library of spiro-fused benzoxaborin derivatives with appropriate physicochemical and in vitro pharmacokinetic properties for oral drugs. These results indicate that the synthesized boron-containing compounds are therefore eligible for classification in a novel chemical library. This article is protected by copyright. All rights reserved.


Journal Details

This article was published in the following journal.

Name: Chemical biology & drug design
ISSN: 1747-0285


DeepDyve research library

PubMed Articles [11261 Associated PubMed Articles listed on BioPortfolio]

Synthesis of Spiro- and Fused Heterocycles via (4+4) Annulation of Sulfonylphthalide with o-Hydroxystyrenyl Derivatives.

An expedient one-pot protocol for the synthesis of functionalized benzofuran containing fused and spiro-heterocycles has been accomplished by the modified Hauser-Kraus (HK) annulation of sulfonylphtha...

Total Synthesis of (+)-Pyrenolide D.

An efficient approach to stereoselective construction of an spiro-γ-lactone core structure via BF3-promoted formal [3 + 2] annulation of aldehydo-aldose derivatives with γ-methylene-γ-butyrolactone...

Noncanonical Cation-π Cyclizations of Alkylidene β-Ketoesters: Synthesis of Spiro-fused and Bridged Bicyclic Ring Systems.

Three cation-π cyclization cascades initiated at alkylidene β-ketoesters bearing pendent alkenes are described. Depending upon the alkene substitution pattern and the reaction conditions employed, i...

Design, synthesis and biological evaluation of novel, orally bioavailable pyrimidine-fused heterocycles as influenza PB2 inhibitors.

With the aim to identify novel influenza PB2 inhibitors with high potency and excellent pharmacokinetic parameters, we have designed and synthesized two new series of pyrimidine-fused heterocycle deri...

Synthesis and evaluation of novel fused pyrimidine derivatives as GPR119 agonists.

A novel series of fused pyrimidine derivatives were designed, synthesized and evaluated as GPR119 agonists. Among them, cyclohexene fused compounds (tetrahydroquinazolines) showed greater GPR119 agoni...

Clinical Trials [2267 Associated Clinical Trials listed on BioPortfolio]

Evaluation of a Mobile Application to Facilitate the Interpretation of Spirometry by Family Physicians and Residents

Problematic: Spirometry is used to objectify the obstructive syndrome defining chronic obstructive pulmonary disease (COPD). However, this test remains underused in the primary care. The t...

Derivatives of Omega-3 PUFA as Biomarkers of Traumatic Brain Injury

This is a Phase 2 clinical trial designed to obtain data on relationships between potentially therapeutic doses of n-3 HUFA (highly unsaturated fatty acids) and their bioactive molecular d...

A Study Evaluating the Effects of Lipid Lowering Treatment on Steroid Synthesis

Cholesterol is the precursor of glucocorticoids, mineralocorticoids and sex steroids. Both adrenal and non-adrenal (ovarian + testicular) all steroid hormones are primarily synthesized usi...

The Effect of Enamel Matrix Derivatives on Root Coverage Esthetic Score

Subepithelial connective tissue grafts (SCTG) are accepted as the gold standard in covering denuded root surfaces. Combining enamel matrix derivatives (EMD) with periodontoplasic surgical ...

Effects of Oral Supplementation of Arginine, Zinc and Vitamin C on Collagen Synthesis in Inguinal Hernia Patients

Collagen synthesis is depressed systemically in the immediate postoperative period. Arginine, zinc and vitamin C impact collagen synthesis. The aim of this study is to investigate the eff...

Medical and Biotech [MESH] Definitions

Derivatives of QUINOLINES with fused PYRROLES and a keto group or INDOLEQUINONES with fused PIPERIDINES.

A family of spiro(isobenzofuran-1(3H),9'-(9H)xanthen)-3-one derivatives. These are used as dyes, as indicators for various metals, and as fluorescent labels in immunoassays.

An approach, process, or methodology which emphasizes credible evidence and the best available scientific knowledge, judiciously integrated to achieve the best possible outcomes in structural design. For example, the design of a new OUTPATIENT CLINIC might incorporate a review of published research on outpatient clinic design, decisions on similar past projects, along with interviews with staff and consumers.

A compound composed of a two CYCLIC PEPTIDES attached to a phenoxazine that is derived from STREPTOMYCES parvullus. It binds to DNA and inhibits RNA synthesis (transcription), with chain elongation more sensitive than initiation, termination, or release. As a result of impaired mRNA production, protein synthesis also declines after dactinomycin therapy. (From AMA Drug Evaluations Annual, 1993, p2015)

A trace element with atomic symbol Mn, atomic number 25, and atomic weight 54.94. It is concentrated in cell mitochondria, mostly in the pituitary gland, liver, pancreas, kidney, and bone, influences the synthesis of mucopolysaccharides, stimulates hepatic synthesis of cholesterol and fatty acids, and is a cofactor in many enzymes, including arginase and alkaline phosphatase in the liver. (From AMA Drug Evaluations Annual 1992, p2035)

Quick Search


DeepDyve research library

Relevant Topics

Pharmacy is the science and technique of preparing as well as dispensing drugs and medicines. It is a health profession that links health sciences with chemical sciences and aims to ensure the safe and effective use of pharmaceutical drugs. The scope of...

Biological Therapy
Biological therapy involves the use of living organisms, substances derived from living organisms, or laboratory-produced versions of such substances to treat disease. Some biological therapies for cancer use vaccines or bacteria to stimulate the body&rs...

Searches Linking to this Article