Fluorine in pharmaceutical industry: fluorine-containing drugs introduced to the market in the last decade (2001–2011)

J Wang, M Sánchez-Roselló, JL Aceña… - Chemical …, 2014 - ACS Publications
1.1. Brief Historical Overview As expected from the fluorine position on the periodic table of
elements, it possesses some extreme properties, in particular, ultimate electronegativity and …

Transition metal-mediated synthesis of monocyclic aromatic heterocycles

AV Gulevich, AS Dudnik, N Chernyak… - Chemical …, 2013 - ACS Publications
Transition Metal-Mediated Synthesis of Monocyclic Aromatic Heterocycles | Chemical Reviews
ACS ACS Publications C&EN CAS Find my institution Log In Chemical Reviews ACS …

Recent advances in isoxazole chemistry

AV Galenko, AF Khlebnikov, MS Novikov… - Russian Chemical …, 2015 - iopscience.iop.org
The preparation methods and reactions of isoxazoles are described and systematized on
the basis of analysis of the literature published from 2005 to present. In the discussion of …

Transition metal-mediated synthesis of oxazoles

S Bresciani, NCO Tomkinson - Heterocycles, 2014 - pureportal.strath.ac.uk
Among the synthetic methods for the formation of the oxazole ring, transition metal-mediated
protocols are the most attractive in terms of selectivity, efficiency and mildness of reaction …

Sketching the historical development of pyrimidones as the inhibitors of the HIV integrase

RV Patel, YS Keum, SW Park - European Journal of Medicinal Chemistry, 2015 - Elsevier
Heterocyclic substances perform a very unique role in drug design and discovery. This
article provides the primary objectives of the analysis within pyrimidine centered new …

Homology model-guided 3D-QSAR studies of HIV-1 integrase inhibitors

H Sharma, X Cheng, JK Buolamwini - Journal of chemical …, 2012 - ACS Publications
In the present study, we report the exploration of binding modes of potent HIV-1 integrase
(IN) inhibitors MK-0518 (raltegravir) and GS-9137 (elvitegravir) as well as chalcone and …

Synthesis of Novel Pyrazino[2,1‐a]isoindolediones via Intramolecular Hydroamination of 2,3‐Dihydro‐3‐oxo‐2‐(prop‐2‐yn‐1‐yl)‐1H‐isoindole‐1‐carboxamides

F Esmaeili‐Marandi, I Yavari, M Saeedi… - Helvetica Chimica …, 2016 - Wiley Online Library
Novel derivatives of pyrazino [2, 1‐a] isoindolediones were synthesized through 6‐exo‐dig
intramolecular hydroamination of 2, 3‐dihydro‐3‐oxo‐2‐(prop‐2‐yn‐1‐yl)‐1H‐isoindole‐1 …

A QSAR study of integrase strand transfer inhibitors based on a large set of pyrimidine, pyrimidone, and pyridopyrazine carboxamide derivatives

LJ de Campos, EB de Melo - Journal of Molecular Structure, 2017 - Elsevier
In the present study, 199 compounds derived from pyrimidine, pyrimidone and
pyridopyrazine carboxamides with inhibitory activity against HIV-1 integrase were modeled …

Structural modifications of 5, 6-dihydroxypyrimidines with anti-HIV activity

DL Guo, XJ Zhang, RR Wang, Y Zhou, Z Li… - Bioorganic & medicinal …, 2012 - Elsevier
A series of 5, 6-dihydroxypyrimidine analogs were synthesized and evaluated for their anti-
HIV activity in vitro. Among all of the analogs, several compounds exhibited significant anti …

Quantitative structure-activity relationship of anti-HIV integrase and reverse transcriptase inhibitors using norm indexes

Y Wang, F Yan, Q Jia, Y Dai, Q Wang - SAR and QSAR in …, 2017 - Taylor & Francis
The development of new and safe anti-human immunodeficiency virus (anti-HIV) drugs has
been an urgent task for medical research recently. Herein, based on the norm-index …