Aim To investigate more efficient synthetic method of the nitrogen analogue 4 of salacinol (1) for searching new antidiabetic agents. Methods The synthesis of the key intermediate 2,4-O-isopropylidene-L-erythritol 1,3-cyclic sulfate (2a) was accomplished by modification of reports from Dglucose via seven steps in much more less expensive. Using this method, an efficient synthesis of 4 was carried out. The glycosidase inhibitory activity of 4 was tested for the intestinal α-glucosidase in vitro and compared with that of salacinol. Results A nitrogen analogue 4 of salacinol (1) was synthesized by the coupling reaction between the cyclic sulfate 2a and an azasugar 3b. Conclusion Substitution of the sulfur atom in 1 with a nitrogen reduced the activity considerably.

We have established NICU (Neonatal Intensive Care Unit) in our hospital and have made efforts to improve the contents of medical treatment since 1976 in order to establish a regionalization of neonatal medical treatment.
Thus are main items of the improvement:
1. Completed the apparatuses and equipments needed in Intensive Care.
2. Promoted the communication with regional facilities of delivery so as to enable immature or stressed mature babies to be transported to our hospital at all hours.
3. Made Pediatrician attend all the deliveries with high risk factors and treat the asphyxiated newborn right after the delivery.
We have recorded the results of comparison of the death rate of immature babies at different birth weight treated in our hospital, and of the perinatal mortality in our Obstetric Department in the pie-improvement period of 5 years (1971-1975) and in the post-improvement period of 4 years (1976-1979) respectively.
The results are as follows:
1. A comparison of the death rate of immature babies at different birth weight.
In comparison of pre and post improvement, under 1, 000 g we haven't had enough cases to compare, besides most of the babies have died. However, at the weight between 1, 001-1, 500 g, the death rate has decreased from 39.4% down to 14.3%, at between 1, 501-2, 000g it has decreased from 11.4% down to 8.9%, and at between 2, 001-2, 500 g, from 6.9% to 1.1%.
2. A comparison of the perinatal mortality in our Obstetric Department.
The perinatal mortality has decreased from 18.5% down to 11.8% when we compare pre and post improvement. This result of the decrease depends on the decrease of fetal death at delivery and baby's death in the early neonatal period. Items of the causes of early neonatal death reveals that the deaths of immature babies and asphyxiated mature babies have decreased significantly.
From these results, we are fully realized the benefit of the regionalization of the neonatal medical treatment and I think we ought to promote such regionalization especially in rural area.

We have established NICU (Neonatal Intensive Care Unit) in our hospital and concentrated our efforts on improving the contents of medical treatment since 1976 in order to accomplish a regionalization of neonatal medical treatment in our district.
Thereafter, the mortality rate of low birth weight infants at different weight have decreased markedly. During this period, we have gathered information by means of questinnaire concerning the prognosis of low birth weight (below 2, 000 g) infants whowere admitted in our hospital in the preimprovement period of five years (1971 through 1975, Group 1; N =110) and in the post-improvement period of five years (1976 through 1980, Group 2; N = 96).
The results were as follows:
1, In terms of height and weight, both groups revealed to be no less than those of normal infants.
2. The occurrence of cerebral palsy in Group 2 (2.2%) decreased to below one third of Group 1 (7.5%).
3. There were two infants with blindness resulting from retrolental fibloplasia in Group 1 and one in Group 2.
4. As regards the occurrence rate of epilepsy, there were two children with it in Group 1 (1.98%) and one in Group 2 (1.1%), whereas four children in Group 1 had episodes of afebrile convulsion.
5. Five (5.4%) of 92 grade-school pupils in Group 1 were attending a clss for handicapped.
From these results, it may be concluded that the improvement of neonatal medical treatment brought about a decrease of death rate of low birth weight infants and the improvement of theirprognosis as well.

Due to the widespread acceptance of gastric and esophageal endoscopic submucosal dissections (ESDs), the number of medical facilities that perform colorectal ESDs has grown and the effectiveness of colorectal ESD has been increasingly reported in recent years. The clinical indications for colorectal ESD at the National Cancer Center Hospital, Tokyo, Japan include laterally spreading tumor (LST) nongranular type lesions >20 mm and LST granular type lesions >30 mm. In addition, 0-IIc lesions >20 mm, intramucosal tumors with nonlifting signs and large sessile lesions, all of which are difficult to resect en bloc by conventional endoscopic mucosal resection (EMR), represent potential candidates for colorectal ESD. Rectal carcinoid tumors less than 1 cm in diameter can be treated simply, safely, and effectively by endoscopic submucosal resection using a ligation device and are therefore not indications for ESD. The en bloc resection rate was 90%, and the curative resection rate was 87% for 806 ESDs. The median procedure time was 60 minutes, and the mean size for resected specimens was 40 mm (range, 15 to 150 mm). Perforations occurred in 23 (2.8%) cases, and postoperative bleeding occurred in 15 (1.9%) cases, but only two perforation cases required emergency surgery (0.25%). ESD was an effective procedure for treating colorectal tumors that are difficult to resect en bloc by conventional EMR. ESD resulted in a higher en bloc resection rate as well as decreased invasiveness in comparison to surgery. Based on the excellent clinical results of colorectal ESDs in Japan, the Japanese healthcare insurance system has approved colorectal ESD for coverage.
Asian Continental Ancestry Group ; Carcinoid Tumor ; Colorectal Neoplasms ; Delivery of Health Care ; Emergencies ; Hemorrhage ; Humans ; Insurance ; Japan ; Ligation ; Tokyo

AIMTo investigate more efficient synthetic method of the nitrogen analogue 4 of salacinol (1) for searching new antidiabetic agents.

METHODSThe synthesis of the key intermediate 2, 4-O-isopropylidene-L-erythritol 1,3-cyclic sulfate (2a) was accomplished by modification of reports from D-glucose via seven steps in much more less expensive. Using this method, an efficient synthesis of 4 was carried out. The glycosidase inhibitory activity of 4 was tested for the intestinal alpha-glucosidase in vitro and compared with that of salacinol.

RESULTSA nitrogen analogue 4 of salacinol (1) was synthesized by the coupling reaction between the cyclic sulfate 2a and an azasugar 3b.

CONCLUSIONSubstitution of the sulfur atom in 1 with a nitrogen reduced the activity considerably.

Animals ; Enzyme Inhibitors ; chemical synthesis ; chemistry ; pharmacology ; Glycoside Hydrolase Inhibitors ; Intestinal Mucosa ; drug effects ; enzymology ; Molecular Structure ; Nitrogen Compounds ; chemical synthesis ; pharmacology ; Rats ; Structure-Activity Relationship ; Sugar Alcohols ; chemical synthesis ; chemistry ; pharmacology ; Sulfates ; chemical synthesis ; chemistry ; pharmacology ; alpha-Glucosidases ; metabolism