Discovery and development of novel pyrimidine and pyrazolo/thieno-fused pyrimidine derivatives as potent and orally active inducible Nitric Oxide Synthase dimerization inhibitor with efficacy for arthritis

Discovery and Optimization of Glucose Uptake Inhibitors

(2020) Kevin G. Liu et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of Novel Transient Receptor Potential Vanilloid 4 (TRPV4) Agonists as Regulators of Chondrogenic Differentiation: Identification of Quinazolin-4(3H)-ones and in vivo Studies on a Surgically Induced Rat Model of Osteoarthritis

(2019) Masakazu Atobe et al.   JOURNAL OF MEDICINAL CHEMISTRY

Novel Pyrazolo[4,3-d]pyrimidine as Potent and Orally Active Inducible Nitric Oxide Synthase (iNOS) Dimerization Inhibitor with Efficacy in Rheumatoid Arthritis Mouse Model

(2019) Jing Bo Shi et al.   JOURNAL OF MEDICINAL CHEMISTRY

Exploiting the Tolerant Region I of the Non-Nucleoside Reverse Transcriptase Inhibitor (NNRTI) Binding Pocket: Discovery of Potent Diarylpyrimidine-Typed HIV-1 NNRTIs against Wild-Type and E138K Mutant Virus with Significantly Improved Water Solubility and Favorable Safety Profiles

(2019) Boshi Huang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Thieno[2,3-d]pyrimidine as a promising scaffold in medicinal chemistry: Recent advances

(2019) Eslam M.H. Ali et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Pyrazoles containing thiophene, thienopyrimidine and thienotriazolopyrimidine as COX-2 selective inhibitors: Design, synthesis, in vivo anti-inflammatory activity, docking and in silico chemo-informatic studies

(2019) Mai S. El-Shoukrofy et al.   BIOORGANIC CHEMISTRY

Linear and Rationally Designed Stapled Peptides Abrogate TLR4 Pathway and Relieve Inflammatory Symptoms in Rheumatoid Arthritis Rat Model

(2019) Asma Achek et al.   JOURNAL OF MEDICINAL CHEMISTRY

Inducible nitric oxide synthase: Regulation, structure, and inhibition

(2019) Maris A. Cinelli et al.   MEDICINAL RESEARCH REVIEWS

Novel resveratrol-based flavonol derivatives: Synthesis and anti-inflammatory activity in vitro and in vivo

(2019) Liu Zeng Chen et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Inducible nitric oxide synthase inhibitors: A comprehensive update

(2019) Richa Minhas et al.   MEDICINAL RESEARCH REVIEWS

Design, synthesis and bio-evaluation of novel 2-aryl-4-(3,4,5-trimethoxy-benzoyl)-5-substituted-1,2,3-triazoles as the tubulin polymerization inhibitors

(2019) Liancheng Huang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

A Thieno[2,3-d]pyrimidine Scaffold Is a Novel Negative Allosteric Modulator of the Dopamine D2 Receptor

(2018) Tim J. Fyfe et al.   JOURNAL OF MEDICINAL CHEMISTRY

Marbostat-100 Defines a New Class of Potent and Selective Antiinflammatory and Antirheumatic Histone Deacetylase 6 Inhibitors

(2018) Andreas Sellmer et al.   JOURNAL OF MEDICINAL CHEMISTRY

Inducible nitric oxide synthase during the late phase of sepsis is associated with hypothermia and immune cell migration

(2018) Yudai Takatani et al.   LABORATORY INVESTIGATION

Nitric oxide signalling in cardiovascular health and disease

(2018) Charlotte Farah et al.   Nature Reviews Cardiology

Targeted Nitric Oxide Synthase Inhibitors for Migraine

(2018) Amynah A. Pradhan et al.   Neurotherapeutics

Nitric oxide synthase enzymology in the 20 years after the Nobel Prize

(2018) Dennis J Stuehr et al.   BRITISH JOURNAL OF PHARMACOLOGY

Acute and sub-acute toxicity study of hydro-alcoholic leaves extract of Reinwardtia indica in rats

(2018) Prabhat Upadhyay et al.   BIOMEDICINE & PHARMACOTHERAPY

Nitric oxide synthase and structure-based inhibitor design

(2017) Thomas L. Poulos et al.   NITRIC OXIDE-BIOLOGY AND CHEMISTRY

The Chemistry and Bio-Medicinal Significance of Pyrimidines & Condensed Pyrimidines

(2016) K. S. Jain et al.   CURRENT TOPICS IN MEDICINAL CHEMISTRY

Novel pyrazole-5-carboxamide and pyrazole–pyrimidine derivatives: Synthesis and anticancer activity

(2015) Jing Bo Shi et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 3: Optimization of [1,2,4]triazolo[1,5-a]pyrimidine core via structure-based and physicochemical property-driven approaches

(2015) Boshi Huang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Privileged s-triazines: structure and pharmacological applications

(2014) Dhruvin R Shah et al.   Future Medicinal Chemistry

Design, Synthesis, and Structure–Activity Relationship Studies of Novel Fused Heterocycles-Linked Triazoles with Good Activity and Water Solubility

(2014) Xufeng Cao et al.   JOURNAL OF MEDICINAL CHEMISTRY

Bioisosteres and Scaffold Hopping in Medicinal Chemistry

(2014) Nathan Brown   Molecular Informatics

Dioxirane-Mediated Heterogeneous Epoxidations with Potassium Caroate: A Solid Catalyst Bearing Anchored Ketone Moieties

(2012) Lucia D'Accolti et al.   EUROPEAN JOURNAL OF ORGANIC CHEMISTRY

Synopsis of Some Recent Tactical Application of Bioisosteres in Drug Design

(2011) Nicholas A. Meanwell   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of Dual Inducible/Neuronal Nitric Oxide Synthase (iNOS/nNOS) Inhibitor Development Candidate 4-((2-Cyclobutyl-1H-imidazo[4,5-b]pyrazin-1-yl)methyl)-7,8-difluoroquinolin-2(1H)-one (KD7332) Part 2: Identification of a Novel, Potent, and Selective Series of Benzimidazole-Quinolinone iNOS/nNOS Dimerization Inhibitors That Are Orally Active in Pain Models

(2010) Joseph E. Payne et al.   JOURNAL OF MEDICINAL CHEMISTRY

Pharmacological Characterization of KLYP961, a Dual Inhibitor of Inducible and Neuronal Nitric-Oxide Synthases

(2010) K. T. Symons et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Design, synthesis, and biological evaluation of novel diarylalkyl amides as TRPV1 antagonists

(2009) Fu-Nan Li et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Discovery of Inducible Nitric Oxide Synthase (iNOS) Inhibitor Development Candidate KD7332, Part 1: Identification of a Novel, Potent, and Selective Series of Quinolinone iNOS Dimerization Inhibitors that are Orally Active in Rodent Pain Models

(2009) Céline Bonnefous et al.   JOURNAL OF MEDICINAL CHEMISTRY

KLYP956 Is a Non-Imidazole-Based Orally Active Inhibitor of Nitric-Oxide Synthase Dimerization

(2009) K. T. Symons et al.   MOLECULAR PHARMACOLOGY