Synthesis and applications of highly functionalized 1-halo-3-substituted bicyclo [1.1. 1] pentanes
DFJ Caputo, C Arroniz, AB Dürr, JJ Mousseau… - Chemical …, 2018 - pubs.rsc.org
Bicyclo [1.1. 1] pentanes (BCPs) are important bioisosteres of 1, 4-disubstituted arenes, tert-
butyl and acetylenic groups that can impart physicochemical benefits on drug candidates …
butyl and acetylenic groups that can impart physicochemical benefits on drug candidates …
NMR quantification of hydrogen-bond-activating effects for organocatalysts including boronic acids
KM Diemoz, AK Franz - The Journal of Organic Chemistry, 2018 - ACS Publications
The hydrogen-bonding activation for 66 organocatalysts has been quantified using a 31P
NMR binding experiment with triethylphosphine oxide (TEPO). Diverse structural classes …
NMR binding experiment with triethylphosphine oxide (TEPO). Diverse structural classes …
Lithium‐Catalyzed Thiol Alkylation with Tertiary and Secondary Alcohols: Synthesis of 3‐Sulfanyl‐Oxetanes as Bioisosteres
RA Croft, JJ Mousseau, C Choi… - Chemistry–A European …, 2018 - Wiley Online Library
Sulfanyl‐oxetanes are presented as promising novel bioisosteric replacements for thioesters
or benzyl sulfides. From oxetan‐3‐ols, a mild and inexpensive Li catalyst enables …
or benzyl sulfides. From oxetan‐3‐ols, a mild and inexpensive Li catalyst enables …
Design, Synthesis, and SAR of C-3 Benzoic Acid, C-17 Triterpenoid Derivatives. Identification of the HIV-1 Maturation Inhibitor 4-((1R,3aS,5aR,5bR,7aR,11aS,11bR,13aR,13bR)-3a …
A Regueiro-Ren, JJ Swidorski, Z Liu… - Journal of Medicinal …, 2018 - ACS Publications
GSK3532795, formerly known as BMS-955176 (1), is a potent, orally active, second-
generation HIV-1 maturation inhibitor (MI) that advanced through phase IIb clinical trials. The …
generation HIV-1 maturation inhibitor (MI) that advanced through phase IIb clinical trials. The …
The design, synthesis and structure-activity relationships associated with C28 amine-based betulinic acid derivatives as inhibitors of HIV-1 maturation
Y Chen, SY Sit, J Chen, JJ Swidorski, Z Liu… - Bioorganic & medicinal …, 2018 - Elsevier
The design and synthesis of a series of C28 amine-based betulinic acid derivatives as HIV-1
maturation inhibitors is described. This series represents a continuation of efforts following …
maturation inhibitors is described. This series represents a continuation of efforts following …
Oxetane ethers are formed reversibly in the lithium-catalyzed Friedel–Crafts alkylation of phenols with oxetanols: Synthesis of dihydrobenzofurans, diaryloxetanes …
Studies on the mechanism and intermediate products in the Friedel–Crafts reaction between
oxetanols and phenols are presented. The formation of O-alkylated intermediates is …
oxetanols and phenols are presented. The formation of O-alkylated intermediates is …
Four-membered ring systems
J Anaya, RM Sánchez - Progress in Heterocyclic Chemistry, 2018 - Elsevier
The review covers work published in the calendar year 2017. The synthesis and reactivity of
four-membered heteroatom-containing cycles are reviewed. New developments in the …
four-membered heteroatom-containing cycles are reviewed. New developments in the …
[PDF][PDF] 基于布洛芬的结构修饰研究进展
罗潇, 朱玉超, 霍童雨, 焦宁 - 中国医药工业杂志, 2018 - cjph.com.cn
布洛芬是临床上广泛应用的一种非甾体抗炎药, 有超过50 年的使用历史. 近年来基于布洛芬的
结构修饰仍在进行, 以求获得活性更高的化合物或解决其存在的不良反应. 本文从对布洛芬进行 …
结构修饰仍在进行, 以求获得活性更高的化合物或解决其存在的不良反应. 本文从对布洛芬进行 …
[PDF][PDF] Modulatoren epigenetischer Regulationsmechanismen: Medizinische Chemie neuer KDM4-Inhibitoren und Methodenentwicklung zur SFC-MS-Analytik von …
GM Fassauer - 2018 - epub.ub.uni-greifswald.de
Die Zusammenhänge zwischen der Aktivität Epigenetik-assoziierter Enzyme und
Krankheitsgeschehen neoplastischer Art konnten nicht nur experimentell bestätigt, sondern …
Krankheitsgeschehen neoplastischer Art konnten nicht nur experimentell bestätigt, sondern …
Oxetane-based peptidomimetics
JD Beadle - 2018 - wrap.warwick.ac.uk
This thesis describes the synthesis, structural preferences and biological properties of
oxetane-containing peptidomimetics in which one of the amide C= O bonds of a peptide …
oxetane-containing peptidomimetics in which one of the amide C= O bonds of a peptide …