Synthesis and crystal structures of 5'-phenylspiro[indoline-3, 2'-pyrrolidin]-2-one derivatives

<p>Abstract</p> <p>Background</p> <p>The spiro- indole-pyrrolidine ring system is a frequently encountered structural motif in many biologically important and pharmacologically relevant alkaloids. The derivatives of spirooxindole ring systems are used as antimicrobial, antitumour agents and as inhibitors of the human NKI receptor besides being found in a number of alkaloids like horsifiline, spirotryprostatin and (+) elacomine. The recently discovered small-molecule MDM2 inhibitor MI-219 and its analogues are in advanced preclinical development as cancer therapeutics.</p> <p>Results</p> <p>In the crystal structures of the two organic compounds, 4'-Nitro-3',5'-diphenylspiro[indoline-3,2'-pyrrolidin]-2-one and 3'-(4-Methoxyphenyl)- 4'-nitro -5'-phenylspiro[indoline-3,2'-pyrrolidin]-2-one, N-H···O hydrogen bonds make the R²₂(8) ring motif. Further, the structures are stabilized by intermolecular hydrogen bonds.</p> <p>Conclusion</p> <p>The crystal structures of 4'-Nitro-3',5'-diphenylspiro[indoline-3,2'-pyrrolidin]-2-one and 3'-(4-Methoxyphenyl)- 4'-nitro -5'-phenylspiro[indoline-3,2'-pyrrolidin]-2-one have been investigated in detail. In both the compounds, the R²₂(8) motif is present. Due to the substitution of methoxyphenyl instead of phenyl ring, the entire configuration is inverted with respect to the 2-oxyindole ring.</p

Variations in strain affect friction and microstructure evolution in copper under a reciprocating tribological load

The microstructure of the materials constituting a metallic frictional contact strongly influences tribological performance. Being able to tailor friction and wear is challenging due to the complex microstructure evolution associated with tribological loading. Here, we investigate the effect of the strain distribution on these processes. High-purity copper plates were morphologically surface textured with two parallel rectangles—referred to as membranes—over the entire sample length by micro-milling. By keeping the width of these membranes constant and only varying their height, reciprocating tribological loading against sapphire discs resulted in different elastic and plastic strains. Finite element simulations were carried out to evaluate the strain distribution in the membranes. It was found that the maximum elastic strain increases with decreasing membrane stiffness. The coefficient of friction decreases with increasing membrane aspect ratio. By analyzing the microstructure and local crystallographic orientation, we found that both show less change with decreasing membrane stiffness

Spot the Diagnosis

A 24-year-old male presented with hoarseness of voice and asymptomatic papular eruption on the face since infancy. He was the second child in the family, born to consanguineous marriage. His younger sister had similar disease. He had no history of photosensitivity or blistering, seizures. He had multiple yellowish waxy papules on the borders of his eyelids giving it a beaded appearance (Figure 1). Similar lesions were also seen on forehead, arms and upper trunk. The skin over the face and neck was shiny and infiltrated with areas of pock like scarring. He also had vegetating plaques in the intertriginous areas. The lips were thickened, infiltrated and everted. The buccal mucosa had a distinct cobblestone appearance. His tongue was firm and enlarged. Systemic examination did not reveal any abnormalities

Not Available

Not AvailableBackground and Aim: Extended-spectrum β-lactamase (ESBL)-producing Escherichia coli are gradually increasing worldwide and carry a serious public threat. This study aimed to determine the antimicrobial resistance pattern of ESBL-producing E. coli isolated from fecal samples of piglets and pig farm workers. Materials and Methods: Fecal samples from <3-month-old piglets (n=156) and farm workers (n=21) were processed for the isolation of ESBL-producing E. coli in MacConkey agar added with 1 μg/mL of cefotaxime. E. coli (piglets=124; farm workers=21) were tested for ESBL production by combined disk method and ESBL E-strip test. Each of the ESBL-positive isolate was subjected to antibiotic susceptibility testing. The ESBL-producing E. coli were further processed for genotypic confirmation to CTX-M gene. Results: A total of 55 (44.4%, 55/124) and nine (42.9%, 9/21) ESBL-producing E. coli were isolated from piglets and farm workers, respectively. Antibiotic susceptibility testing of the ESBL-positive E. coli isolates from piglets and farm workers showed 100% resistance to ceftazidime, cefotaxime, cefotaxime/clavulanic acid, ceftazidime/clavulanic acid, and cefpodoxime. A proportion of 100% (55/55) and 88.9% (8/9) ESBL-positive E. coli were multidrug resistance (MDR) in piglets and farm workers, respectively. On genotypic screening of the ESBL E. coli isolated from piglets (n=55), 15 were positive for the blaCTX-M gene and of the nine ESBL E. coli from farm workers, none were positive for the blaCTX-M gene. Conclusion: Although there was no significant difference in isolation of ESBL-producing E. coli between piglets and farm workers, the ESBL-positive E. coli from piglets showed relatively higher MDR than farm workers.Not Availabl

Not Available

Not AvailableGlobal status of COVID-19 diagnosis: An overviewNot Availabl

Not Available

Not AvailableThis study analyzed the determinants of morbidity, mortality, and case fatality rate (CFR) of the ongoing pandemic of severe acute respiratory syndrome coronavirus-2 disease 2019 (COVID-19). Data for 210 countries and territories available in public domains were analyzed in relation to mandatory vaccination with Bacille-Calmette-Guérin (BCG), population density, median age of the country population, health care expenditure per capita, life expectancy at birth, healthy life expectancy, literacy rate, per capita gross domestic production adjusted to purchasing power (PPP), burden of tuberculosis (TB), acquired immunodeficiency disease caused by human immunodeficiency virus (HIV-AIDS), malaria, cardiovascular disease (CVD), neoplasm, diabetes, deaths due to energy-protein (food) deficiency (EPD), and per capita government spending on safe water and sanitation. Mandatory BCG vaccination showed a highly significant (p<0.0001) negative correlation with COVID-19 morbidity (r = -0.62) and mortality (r = -0.58) rates, but no significant correlation with CFR. The median age of the nation showed a significant (p<0.0001) positive correlation with COVID-19 morbidity (r= 0.40) and mortality (r = 0.34) rates, but no significant correlation with CFR. The pandemic resulted in higher morbidity (r= 0.47, p<0.0001) and mortality (r= 0.25, p = 0.01) rates in countries with a higher PPP than in those with a lower PPP. COVID-19 CFR and morbidity and mortality rates showed no significant correlation with population density, the burden of malaria or diabetes, or the level of spending on safe water and sanitation. Only the burden of TB showed a positive correlation with CFR (r = 0.17, p = 0.05). However, COVID-19 morbidity showed a significant (p ≤0.05) negative correlation with the burden of TB, HIV-AIDS, CVD, and EPD. Mortality and morbidity in COVID-19 patients showed a positive correlation with per capita health expenditure, life expectancy, the burden of neoplasia, and PPP.Not Availabl