Synthesis of 3-acylindoles by oxidative rearrangement of 2-aminochalcones using a hypervalent iodine reagent and cyclization sequence.

An efficient one-pot method was developed for the construction of 3-acylindoles via oxidative rearrangement of 2-aminochalcones followed by intramolecular cyclization. The reaction was used to convert a variety of 2-aminochalcones into 3-acylindoles in moderate to high yields.

Biotin levels in blood and follicular fluid and their associations with pregnancy outcomes in IVF/ICSI patients.

It has been shown that biotin, a water-soluble vitamin (B7), plays roles in reproductive functions, such as oocyte maturation and embryo development, in experimental animals. On the other hand, little is known about the clinical effects of biotin on human reproduction. In this study, serum and follicular fluid biotin levels were measured in patients who underwent in vitro fertilization/intracytoplasmic sperm injection (IVF/ICSI), and their associations with reproductive outcomes were evaluated. As a result, biotin was detected in follicular fluid, as well as serum, and the biotin levels of follicular fluid were found to be positively correlated with those of serum. The biotin levels of serum were higher than those of follicular fluid, suggesting that biotin may be taken up into the follicular fluid from the blood. Although serum and follicular fluid biotin levels tended to be higher in pregnant patients than in non-pregnant patients, these data did not show the significant statistical difference. These findings indicate that biotin does not contribute to the maintenance of oocyte quality, and hence, it does not increase fertilization and pregnancy rates. J. Med. Invest. 69 : 65-69, February, 2022.

[Antifungal susceptibility among the isolates of yeast from the University Hospital of the Ryukyus].

During the period from 1999 to 2003, A total of 2,255 isolates of yeast from the patients of the University Hospital of the Ryukyus were determined for their antifungal susceptibilities by the ASTY (Kyokuto Pharmaceutical Industrial Co., Ltd., Tokyo) colorimetric microdilution testing. The isolates included 1,576 strains of Candida albicans, 409 of C. glabrata, 69 of C. tropicalis, 60 of C. parapsilosis and 141 of other Candida species. A high and uniform antifungal activity of amphotericin B against all the members of Candida was demonstrated with the most minimum inhibitory concentrations (MICs) ranging between 0.25 to 2.0 microg/ml. The MICs obtained from a nearly half of the isolates included against flucytosine distributed < or = 0.125 microg/ml, but 65 (2.9%) and 43 (1.9%) isolates were interpreted as being resistant and intermediate, respectively. The activity of fluconazole markedly varied by species. The resistant ratios of C. albicans and C. parapsilosis were 0.9% and 1.7%, whereas those of C. tropicalis and C. glabrata were estimated as being 40.6% and 13.7%, respectively. The activities of miconazole and micafungin were the most potent with MICs50, 0.125 and 0.06 microg/ml. However, the MICs of C. parapsilosis against miconazole and those of C. glabrata against micafungin were significantly higher when compared to those of C. albicans. By this study, it became apparent that the activities of the presently available antifungal agents were mostly similar for the time and place, but the susceptibilities of the agents among Candida species were markedly different, particularly against azole derivatives. With this, it is necessary for clinical microbiology laboratories to determine antifungal susceptibility for the isolates of yeast and to continuously monitor the effectiveness of each antifungal agent.