Discovery of novel glitazones incorporated with phenylalanine and tyrosine: synthesis, antidiabetic activity and structure-activity relationships.

We report a series of new glitazones incorporated with phenylalanine and tyrosine. All the compounds were tested for their in vitro glucose uptake activity using rat-hemidiaphragm, both in presence and absence of insulin. Six of the most active compounds from the in vitro screening were taken forward for their in vivo triglyceride and glucose lowering activity against dexamethazone induced hyperlipidemia and insulin resistance in Wistar rats. The liver samples of rats that received the most active compounds, 23 and 24, in the in vivo studies, were subjected to histopathological examination to assess their short term hepatotoxicity. The investigations on the in vitro glucose uptake, in vivo triglyceride and glucose lowering activity are described here along with the quantitative structure-activity relationships.

Efficacy of intra-alveolar chlorhexidine gel in reducing frequency of alveolar osteitis in mandibular third molar surgery.

OBJECTIVE: To determine the efficacy of intra-alveolar administration of chlorhexidine (CHX) gel in reducing the frequency of alveolar osteitis (AO) after impacted mandibular third molar surgery. STUDY DESIGN: A randomized control trial study. PLACE AND DURATION OF STUDY: Department of Oral and Maxillofacial Surgery, Armed Forces Institute of Dentistry, Rawalpindi, Pakistan, from January to December 2007. METHODOLOGY: One hundred patients including 65 males and 35 females with the age range 18-40 years were divided in two equal groups (50 each in the CHX and the control groups). Surgical removal of impacted mandibular third molar was carried out and after surgery CHX gel was placed into the alveolus of CHX group. Patients were followed at the first, second and third postoperative days. A proforma indicating presence or absence of pain, blood clot disintegration, halitosis and AO was filled for each patient. Frequencies and percentages were calculated for qualitative data. Chi-square test was applied to compare both subgroups. RESULTS: Eighteen patients (18%) were diagnosed with AO (11 males and 7 females). Out of these 18 cases, 14 (28%) were found in control group (9 males and 5 females), while 4 cases (8%) in the CHX group (2 males and 2 females). This was statistically significant p=0.017. CONCLUSION: Single application of CHX gel was effective in reducing frequency of AO following mandibular third molar surgery.

Synthesis of unnatural selenocystines and beta-aminodiselenides via regioselective ring-opening of sulfamidates using a sequential, one-pot, multistep strategy.

A variety of N-alkyl-beta-aminodiselenides have been synthesized in high yield from sulfamidates under mild reaction conditions using potassium selenocyanate and benzyltriethylammonium tetrathiomolybdate ([BnNEt(3)](2)MoS(4)) in a sequential, one-pot, multistep reaction. The tolerance of multifarious protecting groups under the reaction conditions is discussed. The methodology was successfully extended to the synthesis of selenocystine, 3,3'-dialkylselenocystine, and 3,3'-diphenylisoselenocystine and their direct incorporation into peptides.

One-pot protection and activation of amino acids using pentafluorophenyl carbonates.

Protection of the amino group and activation of the carboxylic acid groups are the most important steps associated with any peptide synthesis protocol; hence, a one-pot process to achieve these is highly desirable. A possible strategy is to use pentafluorophenyl carbonates to simultaneously protect the amino group as a carbamate derivative and activate the carboxylic acid group as a pentafluorophenyl ester. A detailed study is carried out to understand the scope and limitations of this method using five different pentaflurophenyl carbonates. The efficiency of these one-pot reactions depends largely on the nature of the pentafluorophenyl carbonates and also on the nature of the amino acids. Electron deficient and sterically less demanding carbonates reacted faster than the others, whereas amino acids with longer aliphatic side chains gave better yields than more polar amino acids.

Tuberculous mastitis.

OBJECTIVE: To find out the different clinical presentations of breast tuberculosis and its treatment outcome. DESIGN: An observational study. PLACE AND DURATION OF STUDY: Surgical ward 3 of Jinnah Postgraduate Medical Centre, Karachi from June 2001 to November 2003. SUBJECTS AND METHODS: Fifty consecutive female patients above 13 years presenting with breast lump, multiple sinuses, axillary lymphadenopathy, and cold abscess were included in the study. Medical records of the patients presented were reviewed and analyzed. Data was collected regarding the patient's name, age and marital and lactational status. Clinical Examinations and investigations were carried out by triple assessment i.e. clinical, radiological and histological / cytological evaluation. RESULTS: The commonest presentation was a solitary breast lump in 30 (60%) patients, breast lump with axillary lymphadenopathy in 13 (26%). Four (8%) patients presented with generalized breast swelling (edema) with ipsilateral axillary lymphadenopathy. Two (4%) presented with breast abscess and axillary lymphadenopathy and one (2%) with axillary sinus and breast lump. Upper outer quadrant was most frequently involved in 29 (58%) of patients. Thirty-two (64%) cases were secondary to tuberculosis in other sites, mostly (40%) from tuberculous axillary lymphadenitis. Forty-eight (96%) patients responded well to one year antituberculous treatment with complete disappearance of the lumps except 2 patients who had shrinkage of lump size only, underwent excision of lump. CONCLUSION: Solitary lump and enlarged lymph nodes are the commonest presentation of mammary tuberculosis. Early diagnosis and treatment is necessary to prevent disfigurement of breast. Antituberculous therapy is the treatment of choice. Surgery should be reserved for unresponsive lumps.