A REVIEW ON THE SYNTHETIC METHODOLOGIES OF CHROMONES

Chromones group of compounds and their derivatives form the essential component of pharmacophores in many biologically active molecules. They exhibit a wide range of biological activities such as antibiotic, antitumor, antiviral, antioxidant, antipsychotic, and antihypoxic activities. These applications have stimulated a continuous search for the synthesis of new compounds in this field and are being extensively investigated. The various methodologies so far reported for the synthesis of these compounds with the compounds biological applications are discussed in this communicatio

An unusual case of malignant mesothelioma mimicking as Fournier’s gangrene

Fournier gangrene is a rare, life-threatening necrotizing fasciitis that usually involves the perineal or genital areas. Malignant mesothelioma in the inguinal and paratesticular region is a very rare entity and manifesting as Fournier’s gangrene is still rare. Here we present a case of malignant mesothelioma which presented clinically as Fournier’s gangrene.

Synthesis, biological evaluation and docking studies of (4-aryl-3-methyl-4,5-dihydropyrazolo[3,4-c]pyrazol-1(3aH)-yl)(3-hydroxyquinoxalin-2-yl)methanones

862-866An efficient synthesis of (4-aryl-3-methyl-4,5-dihydropyrazolo[3,4-c]pyrazol-1(3aH)-yl)(3-hydroxyquinoxalin-2-yl) methanones is described via reactions of ethyl acetoacetate with 3-hydroxyquinoxaline-2-carbohydrazide. The structures of the compounds prepared have been determined by spectral analyses

Synthesis, biological evaluation and docking studies of (4-aryl-3-methyl-4,5-dihydropyrazolo[3,4-c]pyrazol-1(3aH)-yl)(3-hydroxyquinoxalin-2-yl)methanones

An efficient synthesis of (4-aryl-3-methyl-4,5-dihydropyrazolo[3,4-c]pyrazol-1(3aH)-yl)(3-hydroxyquinoxalin-2-yl) methanones is described via reactions of ethyl acetoacetate with 3-hydroxyquinoxaline-2-carbohydrazide. The structures of the compounds prepared have been determined by spectral analyses

DFT Analysis, ADME, antibacterial activity and molecular docking studies of 2-(3-aryl-1,2,4-oxadiazol-5-yl)-n-phenylacetamide derivatives

Quantum computational study based on density functional theory (DFT/B3LYP) using basis set 6-311G (d,p) a number of global and local reactivity descriptors have been computed to predict the reactivity and the reactive sites on the 2-(3-aryl-1,2,4-oxadiazol-5-yl)-n-phenylacetamideoxadiazole derivatives. The molecular geometry and the electronic properties such as frontier molecular orbital (HOMO and LUMO), ionization potential (I) and electron affinity (A) are investigated to get a better insight of the molecular properties. Molecular electrostatic potential (MEP) for all compounds were determined to check their electrophilic or nucleophilic reactivity. The in silico pharmacokinetics showed that nearly all derivatives obeyed Lipinski rule of 5 with low toxicity and metabolic stability. The antibacterial activity was carried out against B. subtilis, S. aureus, P.aeruginosa and E. coli, displaying considerable inhibition. MurE ligases, (PDB: 7b6k) participating in the intracellular steps of bacterial peptidoglycan biosynthesis, are taken as targets for molecular docking studies using Flare GUI software. The docking outcome revealed that these 1,2,4-oxadiazole analogues have highest LF rank score in the range -12.9 to -6.0 which shows that they act as potent antibacterial agents

RNA editing signature during myeloid leukemia cell differentiation

Adenosine deaminases acting on RNA (ADARs) are key proteins for hematopoietic stem cell self-renewal and for survival of differentiating progenitor cells. However, their specific role in myeloid cell maturation has been poorly investigated. Here we show that ADAR1 is present at basal level in the primary myeloid leukemia cells obtained from patients at diagnosis as well as in myeloid U-937 and THP1 cell lines and its expression correlates with the editing levels. Upon phorbol-myristate acetate or Vitamin D3/granulocyte macrophage colony-stimulating factor (GM-CSF)-driven differentiation, both ADAR1 and ADAR2 enzymes are upregulated, with a concomitant global increase of A-to-I RNA editing. ADAR1 silencing caused an editing decrease at specific ADAR1 target genes, without, however, interfering with cell differentiation or with ADAR2 activity. Remarkably, ADAR2 is absent in the undifferentiated cell stage, due to its elimination through the ubiquitin–proteasome pathway, being strongly upregulated at the end of the differentiation process. Of note, peripheral blood monocytes display editing events at the selected targets similar to those found in differentiated cell lines. Taken together, the data indicate that ADAR enzymes play important and distinct roles in myeloid cells

Hatchery production of penaeid prawn seed: Penaeus indicus

The different techniques of hatchery production of penaeid prawn seed that have been developed in different countries of the world are generally capital intensive, involving high technology. A developing country such as India with limited resources needs a low-cost technology which is simple enough to be used by semiskilled workers. The technology presented here is based on a multi-disciplinary research experience from experimental to pilot stage, on induced breeding of marine prawns and hatchery production of penaeid prawn seed during the past decade. It is developed by utilising the locally available resources and materials and is appropriate to the socio-economic conditions prevailing along our coast

Isoform-specific targeting of PKA to multivesicular bodies

PKA RIα subunit is localized to MVBs by the A-kinase–anchoring protein AKAP11 when disassociated from the PKA catalytic subunit

‘What’s in the NIDDK CDR?’—public query tools for the NIDDK central data repository

The National Institute of Diabetes and Digestive Disease (NIDDK) Central Data Repository (CDR) is a web-enabled resource available to researchers and the general public. The CDR warehouses clinical data and study documentation from NIDDK funded research, including such landmark studies as The Diabetes Control and Complications Trial (DCCT, 1983–93) and the Epidemiology of Diabetes Interventions and Complications (EDIC, 1994–present) follow-up study which has been ongoing for more than 20 years. The CDR also houses data from over 7 million biospecimens representing 2 million subjects. To help users explore the vast amount of data stored in the NIDDK CDR, we developed a suite of search mechanisms called the public query tools (PQTs). Five individual tools are available to search data from multiple perspectives: study search, basic search, ontology search, variable summary and sample by condition. PQT enables users to search for information across studies. Users can search for data such as number of subjects, types of biospecimens and disease outcome variables without prior knowledge of the individual studies. This suite of tools will increase the use and maximize the value of the NIDDK data and biospecimen repositories as important resources for the research community

Global, regional, and national sex-specific burden and control of the HIV epidemic, 1990–2019, for 204 countries and territories: the Global Burden of Diseases Study 2019

Background: The sustainable development goals (SDGs) aim to end HIV/AIDS as a public health threat by 2030. Understanding the current state of the HIV epidemic and its change over time is essential to this effort. This study assesses the current sex-specific HIV burden in 204 countries and territories and measures progress in the control of the epidemic. Methods: To estimate age-specific and sex-specific trends in 48 of 204 countries, we extended the Estimation and Projection Package Age-Sex Model to also implement the spectrum paediatric model. We used this model in cases where age and sex specific HIV-seroprevalence surveys and antenatal care-clinic sentinel surveillance data were available. For the remaining 156 of 204 locations, we developed a cohort-incidence bias adjustment to derive incidence as a function of cause-of-death data from vital registration systems. The incidence was input to a custom Spectrum model. To assess progress, we measured the percentage change in incident cases and deaths between 2010 and 2019 (threshold >75% decline), the ratio of incident cases to number of people living with HIV (incidence-to-prevalence ratio threshold <0·03), and the ratio of incident cases to deaths (incidence-to-mortality ratio threshold <1·0). Findings: In 2019, there were 36·8 million (95% uncertainty interval [UI] 35·1–38·9) people living with HIV worldwide. There were 0·84 males (95% UI 0·78–0·91) per female living with HIV in 2019, 0·99 male infections (0·91–1·10) for every female infection, and 1·02 male deaths (0·95–1·10) per female death. Global progress in incident cases and deaths between 2010 and 2019 was driven by sub-Saharan Africa (with a 28·52% decrease in incident cases, 95% UI 19·58–35·43, and a 39·66% decrease in deaths, 36·49–42·36). Elsewhere, the incidence remained stable or increased, whereas deaths generally decreased. In 2019, the global incidence-to-prevalence ratio was 0·05 (95% UI 0·05–0·06) and the global incidence-to-mortality ratio was 1·94 (1·76–2·12). No regions met suggested thresholds for progress. Interpretation: Sub-Saharan Africa had both the highest HIV burden and the greatest progress between 1990 and 2019. The number of incident cases and deaths in males and females approached parity in 2019, although there remained more females with HIV than males with HIV. Globally, the HIV epidemic is far from the UNAIDS benchmarks on progress metrics. Funding: The Bill & Melinda Gates Foundation, the National Institute of Mental Health of the US National Institutes of Health (NIH), and the National Institute on Aging of the NIH