Recent development of pyrimidine‐containing antimicrobial agents

J Zhuang, S Ma - ChemMedChem, 2020 - Wiley Online Library
Multidrug‐resistant bacterial infections have become an important cause of clinical death in
the twenty‐first century. Much effort has been made to overcome this challenge. The …

Small molecule ghrelin receptor inverse agonists and antagonists

KO Cameron, SK Bhattacharya… - Journal of medicinal …, 2014 - ACS Publications
Ghrelin is an endogenous peptide hormone secreted primarily by the stomach and is
involved in a number of physiological processes including growth hormone secretion, food …

Discovery of PF-5190457, a potent, selective, and orally bioavailable ghrelin receptor inverse agonist clinical candidate

SK Bhattacharya, K Andrews, R Beveridge… - ACS medicinal …, 2014 - ACS Publications
The identification of potent, highly selective orally bioavailable ghrelin receptor inverse
agonists from a spiro-azetidino-piperidine series is described. Examples from this series …

[HTML][HTML] Enhanced pyrazolopyrimidinones cytotoxicity against glioblastoma cells activated by ROS-Generating cold atmospheric plasma

Z He, C Charleton, RW Devine, M Kelada… - European Journal of …, 2021 - Elsevier
Pyrazolopyrimidinones are fused nitrogen-containing heterocyclic systems, which act as a
core scaffold in many pharmaceutically relevant compounds. Pyrazolopyrimidinones have …

Synthesis of 5-substituted-1H-pyrazolo [4, 3-d] pyrimidin-7 (6H)-one analogs and their biological evaluation as anticancer agents: mTOR inhibitors

GL Reddy, SK Guru, M Srinivas, AS Pathania… - European Journal of …, 2014 - Elsevier
A microwave assisted strategy for synthesis of series of 1H-pyrazolo [4, 3-d] pyrimidin-7 (6H)-
ones has been developed and their biological evaluation as anticancer agents is described …

Identification, optimization, and pharmacology of acylurea GHS-R1a inverse agonists

W McCoull, P Barton, AJH Brown… - Journal of medicinal …, 2014 - ACS Publications
Ghrelin plays a major physiological role in the control of food intake, and inverse agonists of
the ghrelin receptor (GHS-R1a) are widely considered to offer utility as antiobesity agents by …

Bridging computational modeling with amino acid replacements to investigate GHS-R1a-peptidomimetic recognition

J Hou, CL Charron, MM Fowkes, LG Luyt - European Journal of Medicinal …, 2016 - Elsevier
The ghrelin receptor, also referred to as the growth hormone secretagogue receptor 1a
(GHS-R1a), is a G protein-coupled receptor (GPCR) primarily expressed in the brain and …

Rational design, synthesis, and pharmacological characterization of novel ghrelin receptor inverse agonists as potential treatment against obesity-related metabolic …

A Daina, C Giuliano, C Pietra, J Wang… - Journal of medicinal …, 2018 - ACS Publications
A new chemotype of ghrelin inverse agonists was discovered through chimeric design
based on molecular scaffolds known as growth-hormone secretagogue receptor (GHSR) …

Identification of potent, selective, CNS-targeted inverse agonists of the ghrelin receptor

KF McClure, M Jackson, KO Cameron, DW Kung… - Bioorganic & medicinal …, 2013 - Elsevier
The optimization for selectivity and central receptor occupancy for a series of spirocyclic
azetidine–piperidine inverse agonists of the ghrelin receptor is described. Decreased …

Transition Metal–free Single Step Approach for Arylated Pyrazolopyrimidinones and Quinazolinones Using Benzylamines/Benzylalcohols/Benzaldehydes

AD Hudwekar, GL Reddy, PK Verma, S Gupta… - …, 2017 - Wiley Online Library
A transition metal‐free, one step approach has been developed for the synthesis of
pyrazolopyrimidinones using in‐situ condensation of benzylamines, benzylalcohol and …