Directed combinatorial chemistry.

J C Hogan

Home/Archive/PubMed

PubMed · 8895595

Directed combinatorial chemistry.

J C Hogan

View original source ↗Export metadata ↓

Abstract

Combinatorial chemistry has given chemists access to vast numbers of molecules, but selecting the right one has proved more difficult. As chemists have gained experience in the technique, however, it has become possible to use solid- or solution-phase syntheses with different chemistries and scaffolds to produce libraries tailor-made for finding or optimizing a lead directed at almost any class of target.

Explore related subjects

Chemistry, Pharmaceutical Drug Evaluation, Preclinical Forecasting Journal Article

Keep this discovery

Explore connections, maps & timelines

BibTeX RIS

J C Hogan. 1996-11-07. Directed combinatorial chemistry.. https://pubmed.ncbi.nlm.nih.gov/8895595/

Cite the original work for its findings. Save a collection to share your selection of sources.

KEEP EXPLORING

Related citations

PubMed1998

Direct pharmaceutical analysis of bisphosphonates by capillary electrophoresis.

Bisphosphonate compounds have been studied as a class of potential drugs for the treatment of various bone diseases. However, the analyses of these compounds are problematic because most of them do not contain strong chromophores. Based on the unique structures of these compounds, we have employed a capillary electrophoresis (CE) technique for the characterization of these compounds in pharmaceutical dosage formulations. In this study, two CE methods were developed for the determination of a bisphosphonate compound, 2-thioethane-1,1-bisphosphonic acid. The first method involved the use of an uncoated column, a phosphate buffer, and hydrostatic injection with direct UV absorbance detection. The method showed excellent resolution and precision with a reasonable detection limit of 30 microg/ml. Sensitivity was further improved using a glycerol-coated column, together with a phosphate buffer of higher concentration and electrokinetic injection under sample stacking conditions. This modified method revealed a significant improvement in sensitivity with a detection limit of about 50 ng/ml. Both methods demonstrated high simplicity and excellent reproducibility and were successfully applied to the quantitative analyses of pharmaceutical dosing solutions.

Chemistry, Pharmaceutical↗

PubMed1998

Finite element analysis of diffusional drug release from complex matrix systems. II. Factors influencing release kinetics.

This work concentrated on the analysis of several factors influencing the kinetics of diffusional drug release from complex matrix devices, such as convex tablets and rings, into a finite volume. These factors include initial drug concentration distribution, anisotropic matrix, and time- and concentration-dependent diffusion coefficients. The individual and comprehensive effects of these factors on the release kinetics were investigated by the finite element method. Errors introduced by neglecting drug diffusion through the ends of edges of cylindrical devices were estimated by comparison of the 1-D models with the 2-D cylinder model. The influence of side-wall coating on the accuracy of the prediction of release profiles by the 1-D slab model for cylindrical devices was studied using various coating materials of different permeabilities. The analyses carried out in this work could assist the design of the complex matrix systems required for controlled drug release.

Chemistry, Pharmaceutical↗

PubMed1998

Education of medicinal chemists in Departments of Medicinal Chemistry (U.S.A.).

The present state of faculties, student bodies, and curricula in departments of medicinal chemistry have been surveyed by questionnaire and analyzed in the context of perceptions of quality and content. The results reveal a healthy diversity of educational objectives and a broader range of educational objectives than those uncovered in previous surveys of the perceived needs of industrial departments of medicinal chemistry in their search for drug discovery personnel.

Chemistry, Pharmaceutical↗