Microwave-assisted synthesis of novel 2H-chromene derivatives bearing phenylthiazolidinones and their biological activity assessment.

6-Hydroxy-2-oxo-2H-chromene-4-carbaldehyde (2), 6-chloro-2-oxo-2H-chromene-4-carbaldehyde (3) and 6-hydrazinyl-4-methyl-2H-chromen-2-one (5) were prepared as single-pharmacophore motif key intermediates. Compounds 2, 3 and 5 were incorporated in a series of multicomponent reactions (MCRs), under microwave assistance as well as conventional chemical synthesis processes, to afford a series of three and/or four-pharmacophoric-motif conjugates 8a,b, 11, 13, 16, 17, 19 and 20 in good yields. The newly synthesized compounds were characterized by IR, NMR, 13C-NMR, MS and elemental analyses. Finally the synthesized compounds have been screened for their biological activity whereupon they exhibited remarkable antimicrobial activity on different classes of bacteria and the fungus.

Microwave assisted synthesis of some new thiazolopyrimidine, thiazolodipyrimidine and thiazolopyrimidothiazolopyrimidine derivatives with potential antioxidant and antimicrobial activity.

Biginelli reaction of ethyl acetoacetate, thiourea and the appropriate aromatic aldehyde was used to produce ethyl 4-aryl-6-methyl-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carboxylates, that reacted with bromomalononitrile to give ethyl 3-amino-5-aryl-2-cyano-7-methyl-5H-thiazolo[3,2-a]pyrimidine-6-carboxylates rather than the isomeric 7H-thiazolo[3,2-a]pyrimidines. Thiazolopyrimidine derivatives reacted with carbon disulphide to yield ethyl 9-aryl-7-methyl-2,4-dithioxo-2,3,4,9-tetrahydro-1H-thiazolo[3,2-a:4,5-d']dipyrimidine-8-carboxylates, that reacted with phenacyl bromide to produce ethyl 8-methyl-10-(4-methoxyphenyl)-3-substituted-5-thioxo-2(un)subatituted-10H-thiazolo[3'',2'':1',2']pyrimido[4',5':4,5]thiazolo[3,2-a]pyrimidine-9-carboxylates. The aforementioned reactions were carried out using both conventional chemical methods and with the assistance of microwave irradaition. Comparison between both methods showed that the microwave assisted method is preferable because of the time reduction and yield improvements achieved. The new compounds were tested for their biological activity as antioxidants, antibacterial or antifungal agents. Some of the new compounds were found to have moderate to good antioxidant and antimicrobial activities.

Partial splenic embolization versus splenectomy for the management of hypersplenism in cirrhotic patients.

BACKGROUND: Hypersplenism occurs in patients with chronic liver disease, and splenectomy is the definitive treatment. However, the operation may be hazardous in patients with poor liver function. In recent years, partial splenic embolization (PSE) has been widely used in patients with hypersplenism and cirrhosis. This study was conducted to assess the safety and efficacy of PSE compared to splenectomy in the management of hypersplenism in cirrhotic patients. METHODS: This study comprised 40 patients with hypersplenism secondary to cirrhosis. They were divided into two groups, each including 20 patients. The first group of patients were treated by PSE using polyvinyl alcohol particles to achieve embolization of at least 50% of the distal branches of the splenic artery. Postembolization arteriography and computed tomography were performed to document the extent of devascularization. Patients in the second group were treated by splenectomy with or without devascularization and left gastric ligation according to the presence or absence of esophageal varices. RESULTS: There was marked improvement in platelet and leukocytic counts in both groups, and the counts remained at appropriate levels during the follow-up period. All patients in the first group had problems related to postembolization syndrome that abated by the first week. One patient in the first group died from myocardial infarction. No deaths occurred in the second group. Asymptomatic portal vein thrombosis developed in one patient in the first group that was treated with anticoagulation, and another patient developed splenic abscess treated by splenectomy with a good outcome. In the second group, three patients developed portal vein thrombosis, one of them being readmitted 4 months postoperatively with mesenteric vascular occlusion; that patient underwent a resection anastomosis with good outcome. CONCLUSIONS: Partial splenic embolization is an effective therapeutic modality for the treatment of hypersplenism secondary to chronic liver disease. It is a simple, rapid procedure that is easily performed under local anesthesia; and it allows preservation of adequate splenic tissue to safeguard against overwhelming infection.

Minimally invasive video-assisted thyroidectomy for small follicular thyroid nodules.

Minimal access surgery in the thyroid compartment has evolved considerably over the past 10 years and now takes many forms. This study examined the feasibility and reliability of minimally invasive thyroid surgery for the management of small benign thyroid lesions. A total of 68 patients with small thyroid nodules admitted to the Oncology Center of Mansoura University, Egypt, were enrolled in this prospective randomized trial. Patients were allotted to one of two procedures: minimally invasive video-assisted thyroidectomy (MIVAT) or minimally invasive open thyroidectomy using the Sofferman technique of strap muscle transection. Exclusion criteria were nodules > 4 cm, presence of thyroiditis, and thyroid gland volume > 20 ml. Preoperative diagnosis, operating time, blood loss, postoperative pain, complications, and cosmetic outcome were all evaluated. The MIVAT group included 35 patients, and the Sofferman group included 33 patients. The main preoperative pathology was a benign follicular lesion (70.5%), and the main postoperative final pathology was follicular adenoma (54.4%). The two groups were comparable regarding age, sex, and extent of thyroid surgery. Operating time was significantly longer in the MIVAT group (115.4 +/- 33.5 minutes) compared to the Sofferman group (65.6 +/- 23.7 minutes). The postoperative course was significantly less painful in the MIVAT group (p < 0.05). Although patients in the MIVAT group had smaller incisions (p < 0.05), the cosmetic outcome in the two groups was comparable. No long-term complication was encountered in either group. Two distinct approaches of minimally invasive thyroidectomy are now available and can be performed safely in selected patients. Despite some MIVAT advantages of less postoperative pain and slightly better cosmesis, minimally invasive open thyroidectomy offers an advantage of less operating time with comparable cosmetic results.