Generation of Molecular Complexity from Cyclooctatetraene: Preparation of Optically Active Protected Aminocycloheptitols and Bicyclo[4.4.1]undecatriene

The racemic (6-cyclo-heptadienyl)Fe(CO)3+ cation ((±)-7), prepared from cyclooctatetraene, was treated with a variety of carbon and heteroatom nucleophiles. Attack took place at the less hindered C1 dienyl carbon and decomplexation of the (cycloheptadiene)Fe(CO)3 complexes gave products rich in functionality for further synthetic manipulation. In particular, a seven-step route was developed from racemic (6-styryl-2,4-cycloheptadien-1-yl)phthalimide ((±)-9 d) to afford the optically active aminocycloheptitols (−)-20 and (+)-20

Spectral Data for Generation of Molecular Complexity from Cyclooctatetraene: Preparation of Optically Active Protected Aminocycloheptitols and Bicyclo[4.4.1]undecatriene

Spectral data created in the course of the research project. Supports specific findings in Generation of Molecular Complexity from Cyclooctatetraene: Preparation of Optically Active Protected Aminocycloheptitols and Bicyclo[4.4.1]undecatriene . The racemic (6-cyclo-heptadienyl)Fe(CO)3+ cation ((±)-7), prepared from cyclooctatetraene, was treated with a variety of carbon and heteroatom nucleophiles. Attack took place at the less hindered C1 dienyl carbon and decomplexation of the (cycloheptadiene)Fe(CO)3 complexes gave products rich in functionality for further synthetic manipulation. In particular, a seven-step route was developed from racemic (6-styryl-2,4-cycloheptadien-1-yl)phthalimide ((±)-9 d) to afford the optically active aminocycloheptitols (−)-20 and (+)-20

Sprectral data for Generation of Molecular Complexity from Cyclooctatetraene Using Dienyliron and Olefin Metathesis

Spectral data used in the course of researching Generation of molecular complexity from cyclooctatetraene using dienyliron and olefin metathesis methodology . Transformation of the simple hydrocarbon cyclooctatetraene into a variety of polycyclic skeletons was achieved by sequential coordination to iron, reaction with electrophiles followed by allylated nucleophiles, decomplexation and olefin metathesis

Generation of Molecular Complexity from Cyclooctatetraene: Preparation of Aminobicyclo[5.1.0]octitols

A series of eight stereoisomeric N-(tetrahydroxy bicyclo-[5.1.0]oct-2S*-yl)phthalimides were prepared in one to four steps from N-(bicyclo[5.1.0]octa-3,5-dien-2-yl)phthalimide (±)-7, which is readily available from cyclooctatetraene (62 % yield). The structural assignments of the stereoisomers were established by 1H NMR spectral data as well as X-ray crystal structures for certain members. The outcomes of several epoxydiol hydrolyses, particularly ring contraction and enlargement, are of note. The isomeric phthalimides as well as the free amines did not exhibit β-glucosidase inhibitory activity at a concentration of less than 100 μM

Neutrophil-surface antigens CD11b and CD64 expression: a potential predictor of early-onset neonatal sepsis

Background: CD11b, an α subunit of the β2 integrin adhesion molecule, and CD64, the high affinity Fcγ receptor I, are specific neutrophil-surface antigens activated in response to systemic inflammation and, hence, they might potentially help identifying neonatal infections. Objective: We sought to evaluate the time course of expression and diagnostic and prognostic utility of CD11b and CD64 in early-onset sepsis in the suspected newborn. Methods: Sixty newborn infants (28-40 weeks gestation) with antenatal risk factors for sepsis were enrolled and subjected to sepsis work-up including complete blood count, quantification of serum C reactive protein (CRP) and flow cytometric analysis of CD11b and CD64 in cord blood (0 h). These tests were repeated at 8, 24 and 48 h postnatally. Neonates were defined, retrospectively, in two groups: sepsis and no infection, on basis of clinical observation over their first five postnatal days and sepsis work-up results. Results: A significant enhancement of neutrophil CD11b and CD64 expression was demonstrated in the sepsis group as compared to the non-infected group. CD11b over-expression had an onset at 0 h. Its mean value approached two-fold mean level of non-infected neonates by 8-24 h, and declined thereafter. CD64 rising onset was detectable at 8 h and its mean percentage reached four-fold mean value of the non-infected group at 24 h. At 24 h, an optimal cut-off value for CD11b expression of 35% (sensitivity 80%, and specificity 100%), and for CD64 expression of 17% (sensitivity 88%, and specificity 90.3%) had the best performance for prediction of sepsis. Combined use of both markers at 24 h yielded 90% sensitivity and 95% specificity for sepsis prediction. Sepsis survivors showed significantly lower mean expression for CD11b and CD64 as compared to those with fatal outcome. At 24 h, a cut-off value of 88% expression for CD11b and 50% expression for CD64 predicted mortality with sensitivity and specificity of 100%. Conclusion: Enhanced expression of neutrophil-surface antigens CD11b and CD64 could be a promising tool for prediction and therapeutic decision-making in early-onset sepsis indicating the necessity of initiation of antimicrobial therapy and reduction of its unnecessary use in non-infected neonates even before definitive microbiologic identification.Keywords: sepsis, neonate, early-onset, neutrophil activation, surface antigen, CD11b, CD64Egypt J Pediatr Allergy Immunol 2004; 2(2): 90-10

Generation of Molecular Complexity from Cyclooctatetraene: Preparation of Optically Active Protected Aminocycloheptitols and Bicyclo[4.4.1]undecatriene

The racemic (6-cyclo-heptadienyl)Fe(CO)3+ cation ((±)-7), prepared from cyclooctatetraene, was treated with a variety of carbon and heteroatom nucleophiles. Attack took place at the less hindered C1 dienyl carbon and decomplexation of the (cycloheptadiene)Fe(CO)3 complexes gave products rich in functionality for further synthetic manipulation. In particular, a seven-step route was developed from racemic (6-styryl-2,4-cycloheptadien-1-yl)phthalimide ((±)-9 d) to afford the optically active aminocycloheptitols (−)-20 and (+)-20

Generation of Molecular Complexity from Cyclooctatetraene Using Dienyliron and Olefin Metathesis Methodology

Transformation of the simple hydrocarbon cyclooctatetraene into a variety of polycyclic skeletons was achieved by sequential coordination to iron, reaction with electrophiles followed by allylated nucleophiles, decomplexation and olefin metathesis

Chemical Proteomics-Based Analysis of Off-target Binding Profiles for Rosiglitazone and Pioglitazone: Clues for Assessing Potential for Cardiotoxicity

Drugs exert desired and undesired effects based on their binding interactions with protein target(s) and off-target(s), providing evidence for drug efficacy and toxicity. Pioglitazone and rosiglitazone possess a common functional core, glitazone, which is considered a privileged scaffold upon which to build a drug selective for a given target—in this case, PPARγ. Herein, we report a retrospective analysis of two variants of the glitazone scaffold, pioglitazone and rosiglitazone, in an effort to identify off-target binding events in the rat heart to explain recently reported cardiovascular risk associated with these drugs. Our results suggest that glitazone has affinity for dehydrogenases, consistent with known binding preferences for related rhodanine cores. Both drugs bound ion channels and modulators, with implications in congestive heart failure, arrhythmia, and peripheral edema. Additional proteins involved in glucose homeostasis, synaptic transduction, and mitochondrial energy production were detected and potentially contribute to drug efficacy and cardiotoxicity

Barriers to breast cancer screening among a sample of Egyptian females

Background: Breast cancer (BC) is usually diagnosed in late stages in countries with limited resources. Early detection of BC is likely to improve the outcome of the disease for women in these areas. Objective: The aim of this study was to understand the possible personal, economic, and systems barriers to BC screening in a sample of Egyptian women. Materials and Methods: A cross-sectional study was conducted in family health centers representing the seven districts of Alexandria governorate, Egypt. A total of 612 women were randomly selected from the chosen centers. Results: In this sample of Egyptian women, the most frequently identified potential barriers to BC screening were the following: 81.8% would not seek care until they were ill, 77% were unwilling to have a mammogram until it was recommended by the doctor, 71.4% blamed the, lack of privacy, 69.2% thought that medical checkups were not worthwhile, and 64.6% blamed the cost of services. The study further revealed that women of lower education, women in the lower income category, women who did not do paid work, those who had poor knowledge of the risks of BC, and women with no family history of BC were more likely to perceive different screening barriers compared with their counterparts. Conclusion: Many potential personal, economic, and health system barriers were identified. Addressing these barriers by increasing the awareness of BC and dealing with the misconceptions that the women have can help the policy makers to design more culturally relevant strategies to motivate women to utilize screening services