Analytical methods for disease diagnosis require high sensitivity and specific methods. For neonatal mass screening of congenital metabolic disorders, a 3 mm diameter disc of dried filter paper blood obtained from one drop of newborn blood is used, and one disc contains about 4 μL of blood. Diagnosis is performed by measuring hormones and genes in this disc. In hormone analysis, chemiluminescent enzyme immunoassay was developed. In genetic analysis, pyrophosphate generated by PCR amplification reaction or DNA fragment as amplification product was analyzed by luciferase bioluminescence method and capillary electrophoresis, respectively. In addition, identification of reactive oxygen species generated from natural medicines and antianginal drugs and their physiological action mechanism are described.
This paper describes the development of a synthetic method for tetrahydrobiphenylenes and derivatives based on a palladium(0)-catalyzed C(sp2)−H functionalization. This is a new direct method for accessing partially hydrogenated biphenylenes. The derivatization of a tetrahydrobiphenylene is also reported.
A novel series of benzoylsulfonamide derivatives were synthesized and biologically evaluated. Among them, compound 18K was shown to inhibit protein tyrosine phosphatase 1B (PTP1B) activity potently and non-competitively (IC50=0.25 μM). Molecular dynamics simulation demonstrated that 18K binds to the allosteric site of PTP1B. Compound 18K showed high oral absorption in mice, rats, and beagles, and markedly reduced plasma glucose levels, TG levels, and HOMA values with no side effects at 30 mg/kg (p.o.) for one week in db/db mice. In conclusion, the substituted benzoylsulfonamide is a novel scaffold of non-competitive allosteric PTP1B inhibitors, and compound 18K is a promising candidate for an efficacious and safe anti-diabetic drug with anti-obesity effects.
Chemistry and Pharmacology of Analgesic Indole Alkaloids from the Rubiaceous Plant, Mitragyna speciosa
August 10, 2004 | Volume 52 Issue 8 Pages 916-928
Preparation of Methacrylic Acid Copolymer S Nano-fibers Using a Solvent-Based Electrospinning Method and Their Application in Pharmaceutical Formulations
February 01, 2015 | Volume 63 Issue 2 Pages 81-87
Mami Hamori, Yuki Shimizu, Kaori Yoshida, Keizo Fukushima, Nobuyuki Sugioka, Asako Nishimura, Kazumasa Naruhashi, Nobuhito Shibata
Studies on Ketene and Its Derivatives. CXII. Reaction of Ketene with Schiff Bases to give α-Unsubstituted β-Lactams
March 31, 2008 | Volume 31 Issue 2 Pages 538-544
NOBUYA KATAGIRI, YUTAKA MIURA, RYUJI NIWA, TETSUZO KATO
Structural Requirements of Flavonoids and Related Compounds for Aldose Reductase Inhibitory Activity
June 01, 2002 | Volume 50 Issue 6 Pages 788-795
Hisashi Matsuda, Toshio Morikawa, Iwao Toguchida, Masayuki Yoshikawa