Enantioselective total synthesis of (+)-Panepophenanthrin, a novel inhibitor of the Ubiquitin-activating enzyme

An enantioselective total synthesis of the novel natural product (+)-panepophenanthrin has been accomplished in which a biomimetic Diels-Alder dimerisation is a key step. The monomeric precursor 2 was assembled from the readily available Diels-Alder adduct of cyclopentadiene and p-benzoquinone through a short, simple sequence employing chemo- and stereoselective operations

Polycyclitols: novel conduritol and carbasugar hybrids as a new class of potent glycosidase inhibitors

We have conceptualized new molecular entities (bicyclitols) in which two conduritol and two carbasugar moieties are embedded in a polyhydroxylated decahydronaphthalene framework and achieved their syntheses in a stereo- and regioselective manner. One of the bicyclitols was found to be a potent and selective α -glucosidase inhibitor

Novel conformationally locked inositols: from aromatics to annulated cyclitols

A new family of ring-annulated inositols with "locked" conformations has been designed to deliver a range of these biologically important entities in "unnatural conformations" while retaining their "natural configurations". The simple "tool" of trans ring fusion has been used to "lock" the conformation of the annulated inositols. Short, simple syntheses of a range of these novel cyclitols have been achieved from readily available aromatic precursors such as tetralin and indane. Along the way, annulated C2-symmetric cyclohexadiene-trans-diol (trans-CHD) derivatives have been prepared for the first time and serve as the pivotal building blocks for generating the oxy-functionalization pattern of inositols. The presence of chemo-differentiated hydroxyl groups in our novel inositols is expected to facilitate the installation of phosphate diversity to harness the biological potential of these entities

Fatal pulmonary embolism after middle ear surgery: a case report

Pulmonary thromboembolism is a complication of underlying venous thrombosis. Factors contributing to thrombus formation include venous stasis, hypercoagulable state, immobilisation, surgery and pregnancy. Authors present the challenges authors faced in diagnosing pulmonary embolism in a post-operative patient. 35-year-old female with complaint of decreased hearing for 2 years along with tinnitus and giddiness was admitted for stapedectomy. She also gave history of dyspnoea and pedal oedema one month back for which she was hospitalized and underwent investigations which were normal. Patient was discharged as her clinical symptoms improved. On postoperative day 5, she developed sudden dyspnoea after getting up and walking a few steps. Dyspnoea along with falling saturation and bradycardia progressed to cardiopulmonary arrest. Intensive care was started. Bilateral lower limb venous doppler showed deep venous thrombosis. Clinical diagnosis of pulmonary embolism was made, and patient was lysed with Tenecteplase 30 mg. Echocardiography showed signs of resolution of embolism after lysis, but gradually patient deteriorated and developed cardiogenic shock. Intra-aortic balloon pump was inserted via right femoral artery and inotropic support was continued. However, patient’s condition worsened, and she developed cardiopulmonary arrest the next day and could not be revived. Prevention of pulmonary embolism is a major clinical problem for which prophylactic measures like early ambulation in post-operative periods, elastic stockings, graduated compressive stockings for bed ridden patients and preventive anticoagulation therapy in high risk patients should be considered

Flavour Enhanced Food Recommendation

We propose a mechanism to use the features of flavour to enhance the quality of food recommendations. An empirical method to determine the flavour of food is incorporated into a recommendation engine based on major gustatory nerves. Such a system has advantages of suggesting food items that the user is more likely to enjoy based upon matching with their flavour profile through use of the taste biological domain knowledge. This preliminary intends to spark more robust mechanisms by which flavour of food is taken into consideration as a major feature set into food recommendation systems. Our long term vision is to integrate this with health factors to recommend healthy and tasty food to users to enhance quality of life.Comment: In Proceedings of 5th International Workshop on Multimedia Assisted Dietary Management, Nice, France, October 21, 2019, MADiMa 2019, 6 page

Effect of Loading Densities in Closed Vessel Tests on the Burning Rate of a Propelling Charge

Closed vessel firing of gun propellant at different loading densities is conducted for evaluation of its ballistic parameters. Although in actual gun applications, loading densities are higher, but for closed vessel evaluation standard loading density is taken as 0.2 g/cc for interior ballistic calculations of guns. Closed vessel evaluation of standard triple-base propellant in hepta-tubular configuration with loading density varying in the range of 0.2 g/cc to 0.3 g/cc is conducted for the evaluation of salient ballistic parameters. It is observed that maximum pressure increases with increase in loading density of propellants. As loading density increases, rate of rise of pressure also increases. Accordingly, a rise in burning rate is also observed. However, the burning rate index (α) and coefficient (β) of the power law of burning (r = βPα) is found independent of loading density. The average values of these burning rate parameters are calculated as (α =) 0.78 and (β =) 0.45 for the studied propellant.Defence Science Journal, Vol. 65, No. 2, March 2015, pp.126-130, DOI:http://dx.doi.org/10.14429/dsj.65.815

Enantioselective total synthesis of polyoxygenated cyclohexanoids: (+)-streptol, ent-RKTS-33 and putative '(+)-parasitenone'. identity of parasitenone with (+)-epoxydon

Short, simple and enantioselective syntheses of the natural product (+)-streptol, the non-peptide apoptosis inhibitor ent-RKTS-33 and the putative structure of 'parasitenone' have been accomplished from the readily available chiral building block. 'Parasitenone' has been shown to be identical with the known natural product epoxydon

Comparative efficacy of agomelatine versus sertraline in major depressive disorder in Himalayan region of India

Background: Depression, a major common affective disorder which carries excess mortality through suicide. Among various drug classes available SSRI’s are usually a choice, but many patients show inadequate response, residual symptoms or discontinue medication due to intolerable side effects. Disturbances of circadian rhythm function are an etiopathogenic hallmark of depression. The degree of circadian misalignment correlates with the severity of depression and circadian abnormalities may partially be a consequence of alterations in behavior and sleep patterns that accompany depression. Agomelatine an agonist acts on MT1 and MT2 receptors and antagonist of 5HT2c receptors contributes to its resynchronization of circadian rhythms, enhancement of dopaminergic and adrenergic input to the frontal cortex, induction of hippocampal neurogenesis, and ultimately, to its antidepressant effect.Methods: The study was randomized, prospective, comparative and interventional regarding the efficacy of therapy. Hundred consenting patients of MDD attending psychiatry OPD were screened for possible enrollment into group A(Agomelatine) and group B(Sertraline). Patients were assessed by semi-structured case recording form, DSM-IV- TR Criteria for major depressive episode, Hamilton Rating Scale for Depression (HAM-D) and Clinical Global Impressions for severity (CGI-S) at baseline and CGI for improvement (CGI-I), every two weeks interval and final assessment at 8 weeks.Results: Socio-demographic parameters like age and sex distribution, marital status, locality, family type, educational status, occupation and socio-economic class were comparable between two groups. Similarly baseline HAM-D and CGI-S values between the two groups were statistically non-significant. HAM-D, CGI-S and CGI-I values at eight weeks among the two groups were also statistically non-significant but in all three sertraline had decreased the values to a greater extent and showed a trend towards improvement.Conclusions: Both groups had shown significant decrease in scores of all scales i.e. HAM-D, CGI-S, and CGI-I at the end of 8th week as compared to baseline scores, indicating that the uses of agomelatine and sertraline have resulted in significant improvement in symptoms of patients of MDD and reinforcing there efficacy in treatment of MDD. No statistical difference was observed between two groups.

Development and testing of a quantitative food frequency questionnaire for use in Gujarat, India

Objective: To develop and test a quantitative, interviewer-administered food frequency questionnaire (FFQ) to ascertain nutrient intakes of individuals in northern India. Design: A 92-item FFQ was developed based on food use and market surveys of the study area. A validation study was conducted consisting of 24-h diet recalls (24HR) administered on 6 randomly selected days over 1 year. Two FFQs were administered, one each at the beginning and end of the 1-year period. FFQ and 24HR-derived nutrient scores were compared using correlation and regression analyses and by computing differences between nutrient intakes estimated by the two methods. Setting: Rural villages in Bhavnagar District, Gujarat, North India. Subjects: 60 individuals who agreed to provide all necessary data. Results: Pearson (parametric) correlation coefficients averaged 0.69 in comparing nutrient scores derived from the 24HR with those from the first FFQ and 0.72 in comparing the second FFQ (P \u3c 0.0001). Spearman correlation coefficients were virtually identical to the Pearson correlations, averaging 0.68 and 0.72, respectively. In regression analyses, most coefficients were close to 1.0 (perfect linear association). Nutrient scores were significantly and consistently higher on both FFQs relative to the 24HR. Conclusions: This FFQ produces results broadly comparable, and superior in some respects, to those commonly used in the West. Higher than average measures of association indicate its suitability for comparing exposures within this study population in reference to health-related endpoints

Psychometric Properties of the Hindi Version of the Disabilities of Arm, Shoulder, and Hand: A Pilot Study

Objectives. To culturally adapt and translate the Disabilities of Arm, Shoulder, and Hand questionnaire into Hindi (DASH-H) and assess its reliability, validity, and responsiveness in adult patients with shoulder tendonitis. Study Design. Descriptive methodological research, using longitudinal design. Setting. Outpatient clinic. Participants. 30 adult patients aged 53.3 ± 6.9 y with shoulder tendonitis. Data Analyses. DASH-H, visual analogue scales for pain (VAS-P) and disability (VAS-D), and shoulder active range of motion (AROM) were assessed at baseline, 2-3 days later, and 4-5 weeks after baseline. Intraclass correlation coefficients (ICC) assessed test-retest reliability of these scales and responsiveness was examined by calculating effect sizes (ES) and standardized response means (SRM). Cronbach’s alpha (CA) was used to examine internal consistency of DASH-H. Convergent construct validity of DASH-H with VAS scales and shoulder AROM was determined using Pearson’s Correlation Coefficients (). Results. DASH-H demonstrated good test-retest reliability and internal consistency (ICC and CA both \u3e 0.75) and excellent responsiveness (ES = 2.2, SRM = 6.1). DASH-H showed high concordance (, ) with AROM-flexion and moderate concordance (, ) with VAS scales and AROM-external rotation. Conclusion. Analyses indicate that DASH-H demonstrates good test-retest reliability, validity, and responsiveness in patients with shoulder tendonitis