The discovery and optimization of a novel class of potent CCR3 antagonists is described. Details of synthesis and SAR are given together with some ADME properties of selected compounds. An optimal balance between activities, physicochemical properties, and in vitro metabolic stability was reached by the proper choice of substituents.
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http://dx.doi.org/10.1016/j.bmcl.2007.05.035 | DOI Listing |
J Endod
December 2024
Tokyo New Drug Research Laboratories, Pharmaceutical Business Unit, Kowa Company, Ltd., 2-17-43 Noguchi-cho, Higashimurayama, Tokyo, Japan.
Introduction: Our previous study showed that transplantation of dental pulp stem cells (DPSCs) in combination with a chemokine receptor 3 (CCR3) antagonist into the root canals of aged dogs promoted dental pulp regeneration. In this study, we attempted to regenerate dental pulp in young dogs using a CCR3 antagonist without DPSC transplantation.
Methods: The teeth of dogs were histologically evaluated 4 weeks after extraction of the pulp and administration of scaffold materials and CCR3 antagonist (KDH-136) into the root canal.
Mol Psychiatry
November 2024
Department of Regulatory Science for Evaluation & Development of Pharmaceuticals & Devices, Fujita Health University Graduate School of Medical Sciences, Toyoake, Aichi, Japan.
Negative experiences during adolescence, such as social isolation (SI), bullying, and abuse, increase the risk of psychiatric diseases in adulthood. However, the pathogenesis of psychiatric diseases induced by these factors remain poorly understood. In adolescents, stress affects the intestinal homeostasis in the gut-brain axis.
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November 2024
Chongqing College of Traditional Chinese Medicine, Chongqing, 402760, China.
J Leukoc Biol
November 2024
Unidad de Investigación en Biomedicina, Facultad de Estudios Superiores Iztacala, UNAM, Tlalneplantla, Estado de México 54090, México.
Neutrophils represent one of the host's first lines of defense against invading pathogens. However, an aberrant activation can cause damage to the host. In the case of respiratory infections with viral or bacterial pathogens, one of the most common complications is the development of acute respiratory distress syndrome, in which neutrophil infiltration into the lung is a hallmark.
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