(123)I-labeled 2β-carbomethoxy-3β-(4-iodophenyl)-N-(3-fluoropropyl)nortropane ((123)I-FP-CIT) was approved for clinical use in 2011 by the Food and Drug Administration. (123)I-FP-CIT is a radioligand for brain dopamine transporter (DAT) imaging that is useful for the differential diagnosis of Parkinson disease (PD) and other diseases that mimic PD. The sensitivity and specificity of (123)I-FP-C...

This study reported methylene blue (MB) dye decolorization by using mixed consortium culture, brown-rot fungus (BRF) Gloeophyllum trabeum which is known as degradative with bacterium Bacillus subtilis addition. B. were added into G. cultures at variation 2, 4, 6, 8, and 10 mL incubated statically (1 = 9.47 × 108 CFU). All of had ability to decolorize MB (100 mg/L) in potato dextrose broth (PDB)...

[3H]MK-801 binding in rat brain was characterized using a quantitative autoradiographic binding assay. [3H]MK-801 binding (5 nM) reached equilibrium by 120 min at 23 degrees C. [3H]MK-801 appeared to label a single high affinity site with an affinity constant of approximately 11 nM. [3H]MK-801 binding was heterogeneously distributed throughout the brain with the following order of binding densi...

The anti-apoptotic protein Bcl-2 is a well-known and attractive therapeutic target for cancer. In the present study the solution-phase T3P-DMSO mediated efficient synthesis of 2-amino-chromene-3-carbonitriles from alcohols, malanonitrile and phenols is reported. These novel 2-amino-chromene-3-carbonitriles showed cytotoxicity in human acute myeloid leukemia (AML) cell lines. Compound 4 g was fo...

Starting from N-substituted indole-3-carboxaldehydes (1a-g) a series of new 3-[(N-substituted indol-3-yl)methyleneamino]-6-amino-4-aryl-pyrano(2,3-c)pyrazole-5-carbonitriles (3a-g and 4a-g) have been synthesized via the acid catalyzed condensation reaction of 1a-g with 3-amino-5-pyrazolone, followed by the reaction with arylidene malononitriles. A series of new 3,6-diamino-4-(N-substituted indo...

3-Acetyl-4-hydroxycoumarin (2) was reacted with some aldehydes (4-chlorobenzaldehyde, 4-bromobenzaldehyde, 5-methylfurfural) to afford the chalcones (3a-c). Cyclization of these chalcones with malononitrile in the presence of ammonium acetate afforded pyridine carbonitriles (4a-c), while the cyclization reaction of chalcones (3a-c) with ethyl cyanoacetate afforded the oxopyridine carbonitriles ...

for the first time, a spectrum of morphological abnormalities have been produced in developingmouse embryos (n=50), by injecting (ip) 75 and 100 mg/kg of maternal body weight of a new quinazolinonederivative, 4(3h)quinazolinone-2-propyl-2-phenylethyl(qppe), on days 9, 10 and 11 of gestation.measurements of the length of the crown-rump (cr), weight of body of the embryos and placenta on day 17sh...

The expansion and differentiation of oval cells in the acetylaminofluorene (AAF)/partial hepatectomy (PH) model was studied utilizing pulse-chase labeling with both tritiated thymidine ([3H]TdR) and bromodeoxyuridine (BUdR). Animals in which a significant decrease in serum albumin and increase in alanine aminotransferase and bilirubin were observed demonstrated the most prominent differentiatio...

4(3H)-Quinazolinones 1 are known for more than a century [1]. Molecules based on quinazoline and quinazolinone exhibit a multitude of interesting pharmacological activities [2], including anticonvulsant, antibacterial and antidiabetic activity [3,4]. The important natural and synthetic 4(3H)-quinazolinones include l-vasicinone 2 [5], chrysogine 3 [6], methaquinalon 4 [7] – a sedative, piriqualo...

The binding characteristics of conotoxin GIIIA purified from the venom of a marine snail, Conus geographus, with regard to electroplax membranes from Electrophorus electricus were studied using a radiolabeled monopropionyl derivative of the toxin (3H-Pr-CGIIIA). 3H-Pr-CGIIIA bound specifically to a single class of saturable binding sites in electroplax membranes with a dissociation constant of ...