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Biomedical subjects

Yoshio Ogino

Publications and source records attributed to Yoshio Ogino.

6 recordsLinked to original sources

Pituitary abscess in a patient with painless thyroiditis.

The preoperative diagnosis of pituitary abscess is difficult. The case of a 56-year-old man with a pituitary abscess and painless thyroiditis is presented. There has been no previous such report. The differential diagnosis includes pituitary abscess, lymphocytic adenohypophysitis or infundibuloneurohypophysitis, share clinical symptoms of panhypopituitarism and diabetes insipidus, and is of critical importance as the treatment of these conditions differ. The association with painless thyroiditis suggests a diagnosis of lymphocytic adenohypophysitis or infundibuloneurohypophysitis. However, the coincidence of pituitary abscess and painless thyroiditis was observed in our patient, and thus though rare, should be considered. Surgical exploration and histopathological examination are essential for the differential diagnosis of these diseases.

Brain Abscess↗

Discovery of 2-aminothiazole-4-carboxamides, a novel class of muscarinic M(3) selective antagonists, through solution-phase parallel synthesis.

Synthesis and structure-activity relationship of a new class of muscarinic M(3) selective antagonists were described. In the course of searching for a muscarinic M(3) antagonist with a structure distinct from those of the 2-(4,4-difluorocyclopentyl)-2-phenylacetamide derivatives, we identified a thiazole-4-carboxamide derivative (1) as a lead compound in our in-house chemical collection. Since this compound (1) showed relatively low binding affinity (K(i)=140 nM) for M(3) receptors in the human binding assays, we tried to improve its potency and selectivity for M(3) over M(1) and M(2) receptors by derivatization of 1 through a combinatorial approach. A solution-phase parallel synthesis effectively contributed to the optimization of each segment of 1. Thus, we have identified a cyclooctenylmethyl derivative (3e) and a cyclononenylmethyl derivative (3f) as representative M(3) selective antagonists in this class.

Amides↗

[Chloride].

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Acid-Base Imbalance↗

Muscarinic M(3) receptor antagonists with (2R)-2-[(1R)-3,3-difluorocyclopentyl]-2-hydroxyphenylacetamide Structures. Part 2.

Optimization of the amine part of our original muscarinic M(3) receptor antagonist 1 was performed to identify M(3) receptor antagonists that are superior to 1. Compounds carrying a variety of diamine moieties without hydrophobic substituent on the nitrogen atom were screened against the binding affinity for the M(3) receptor and the selectivity for M(3) over the M(1) and M(2) receptors. This process led to a 4-aminopiperidinamide (2l) with a K(i) value of 5.1 nM and with a selectivity of the M(3) receptor that was 46-fold greater than that of the M(2) receptor. Further derivatization of 2l by inserting a spacer group or by incorporating alkyl group(s) into the amine part resulted in the identification of an 4-(aminoethyl)piperidinamide 2l-b with a K(i) value of 3.7 nM for the M(3) receptor and a selectivity for the M(3) receptor that was 170-fold greater than that of the M(2) receptor.

Acetamides↗