Synthesis of Dynamic 2-Ethoxycarbonyl-4H-3, 1-Benzoxazin-4-one and its Behavior Towards Nitrogen Nucleophiles

The behavior of  2-ethoxycarbonyl-4H-3,1-benzoxazin-4-one and its behavior towards nitrogen nucleophiles namely, hydrazine hydrate, formamide, benzylamine, ethylamine, piperidine, ethanol amine, o-phenylenediamine, and glucosamine hydrochloride has been investigated. Also the reaction of 3-[aminoquinazolin-4(3H)-one-2-yl]formic acid hydrazide with aromatic aldehydes and phenylisothiocyanate has been discussed. The structure of the prepared compounds are elucidated using physical and spectral data like, FT-IR, 1HNMR, and mass spectroscopy

Synthesis of bioactive quinazolin-4(3H)-one derivatives via microwave activation tailored by phase-transfer catalysis

A series of nine new 2,3-disubstituted 4(3H)-quinazolin-4-one derivatives was furnished starting from the 2-propyl-4(3H)-quinazoline-4-one (2). The reinvestigation of the key starting quinazolinone 2 was performed under microwave irradiation (MW) and solvent-free conditions. Combination of MW and phase-transfer catalysis using tetrabutylammonium benzoate (TBAB) as a novel neutral ionic catalyst was used for carrying out N-alkylation and condensation reactions of compound 2 as a simple, efficient and eco-friendly technique. The structure of the synthesized compounds was elucidated using different spectral and chemical analyses. In vitro antimicrobial activity of the compounds was investigated against four bacterial and two fungal strains; very modest activity was achieved. Some of the synthesized compounds were screened for their antitumor activity against different human tumor cell lines. The screened compounds exhibited a significant antitumor activity on some of the cancer cell lines, melanoma (SK-MEL-2), ovarian cancer (IGROV1), renal cancer (TK-10), prostate cancer (PC-3), breast cancer (MCF7) and colon cancer (HT29). The most active, even more active than the reference 5-fluorouracil, were found to be ethyl 4-[(4-oxo-2-propylquinazolin-3(4H)-yl)methyl]benzoate (3c), 3-{2-[6-(pyrrolidin-1-yl-sulfonyl)-1,2,3,4-tetrahydroquinoline]-2-oxoethyl}-2-propylquinazolin-4(3H)-one (3e), N’-[(E)-(2H-1,3-benzodioxo-5-yl)methylidene]-2-(4-oxo-2-propylquinazolin-3(4H)-yl)acetohydrazide (10a), N’-[(E)-(4-hydroxyphenyl)methylidene]-2-(4-oxo-2-propylquinazo-lin-3(4H)-yl)acetohydrazide (10b) and N’-[(E)-(4-nitrophenyl)methylidene]-2-(4-oxo-2-propylquinazolin-3(4H)-yl)acetohydrazide (10c)

Self-Emulsifying Drug Delivery Systems: Easy to Prepare Multifunctional Vectors for Efficient Oral Delivery

Self-emulsifying drug delivery systems (SEDDS) have been mainly investigated to enhance the oral bioavailability of drugs belonging to class II of the Biopharmaceutics Classification System. However, in the past few years, they have shown promising outcomes in the oral delivery of various types of therapeutic agents. In this chapter, we discuss the recent progress in the application of SEDDS for oral delivery of protein therapeutics and genetic materials. The role of SEDDS in enhancing the oral bioavailability of P-glycoprotein and cytochrome P450 3A4 substrate drugs is also highlighted. Also, we discuss the most critical evaluation criteria of SEDDS. Additionally, we summarize various solidification techniques employed to transform liquid SEDDS to the more stable solid self-emulsifying drug delivery systems (s-SEDDS) that are associated with high patient compliance. This chapter provides a comprehensive approach to develop high utility SEDDS and their further transformation into s-SEDDS

AGN All the Way Down? AGN-like Line Ratios are Common In the Lowest-Mass Isolated Quiescent Galaxies

We investigate the lowest-mass quiescent galaxies known to exist in isolated environments ($\mathrm{M^* = 10^{9.0-9.5} \ M_\odot}$; 1.5 Mpc from a more massive galaxy). This population may represent the lowest stellar mass galaxies in which internal feedback quenches galaxy-wide star formation. We present Keck/ESI long-slit spectroscopy for 27 isolated galaxies in this regime: 20 quiescent galaxies and 7 star-forming galaxies. We measure emission line strengths as a function of radius and place galaxies on the Baldwin Phillips Terlevich (BPT) diagram. Remarkably, 16 of 20 quiescent galaxies in our sample host central AGN-like line ratios. Only 5 of these quiescent galaxies were identified as AGN-like in SDSS due to lower spatial resolution and signal-to-noise. We find that many of the quiescent galaxies in our sample have spatially-extended emission across the non-SF regions of BPT-space. When considering only the central 1$^{\prime\prime}$, we identify a tight relationship between distance from the BPT star-forming sequence and host galaxy stellar age as traced by $\mathrm{D_n4000}$, such that older stellar ages are associated with larger distances from the star-forming locus. Our results suggest that the presence of hard ionizing radiation (AGN-like line ratios) is intrinsically tied to the quenching of what may be the lowest-mass self-quenched galaxies.Comment: 16 pages, 9 figures, submitted to Ap

The origin of ultra diffuse galaxies: stellar feedback and quenching

We test if the cosmological zoom-in simulations of isolated galaxies from the FIRE project reproduce the properties of ultra diffuse galaxies. We show that stellar feedback-generated outflows that dynamically heat galactic stars, together with a passively aging stellar population after imposed quenching (from e.g. infall into a galaxy cluster), naturally reproduce the observed population of red UDGs, without the need for high spin halos or dynamical influence from their host cluster. We reproduce the range of surface brightness, radius and absolute magnitude of the observed z=0 red UDGs by quenching simulated galaxies at a range of different times. They represent a mostly uniform population of dark matter-dominated galaxies with M_star ~1e8 Msun, low metallicity and a broad range of ages. The most massive simulated UDGs require earliest quenching and are therefore the oldest. Our simulations provide a good match to the central enclosed masses and the velocity dispersions of the observed UDGs (20-50 km/s). The enclosed masses of the simulated UDGs remain largely fixed across a broad range of quenching times because the central regions of their dark matter halos complete their growth early. A typical UDG forms in a dwarf halo mass range of Mh~4e10-1e11 Msun. The most massive red UDG in our sample requires quenching at z~3 when its halo reached Mh ~ 1e11 Msun. If it, instead, continues growing in the field, by z=0 its halo mass reaches > 5e11 Msun, comparable to the halo of an L* galaxy. If our simulated dwarfs are not quenched, they evolve into bluer low-surface brightness galaxies with mass-to-light ratios similar to observed field dwarfs. While our simulation sample covers a limited range of formation histories and halo masses, we predict that UDG is a common, and perhaps even dominant, galaxy type around Ms~1e8 Msun, both in the field and in clusters.Comment: 20 pages, 13 figures; match the MNRAS accepted versio

Giardia intestinalis assemblages among Egyptian symptomatic/asymptomatic cases in Cairo

Giardia intestinalis is frequent enteric protozoa, affecting humans worldwide. Human infections aremainly caused by two genetically different assemblages call A & B. This cross-sectional study characterizedthe Giardia genotypes isolated from the stool of symptomatic and asymptomatic Egyptians inCairo and correlated these genotypes with the demographic and clinical data of the cases. Stool sampleswere collected from 389 individuals (245 complaining of gastrointestinal (GIT) symptoms and144 apparently healthy asymptomatic individuals), and microscopically examined. Positive Samplesfor G. intestinalis were molecularly characterized by Copro-nPCR targeting beta-giardin gene, andthen analyzed by RFLP for assemblage identification. Giardia was detected in 62 samples (15.9%); 53samples in symptomatic cases (21.6%) and 9 samples in asymptomatic individuals (6.25%). DNA ofpositive samples was amplified by nPCR-RFLP assays. There was a significant predominance of assemblageB among symptomatic (82.7%) and asymptomatic (77.8%) groups, while the rest of sampleshad assemblage A. Among the clinical data, only flatulence was significantly associated with Giardiainfection with assemblage B. Assemblage B is the predominant genotype found in Egypt in symptomaticand asymptomatic patients suggesting an anthropologic transmission cycle.Key Words: Giardia; genotyping; Assemblage; nPCR-RFLP; beta-giardin

Dark and luminous satellites of LMC-mass galaxies in the FIRE simulations

Within lambda cold dark matter (CDM), dwarf galaxies like the Large Magellanic Cloud (LMC) are expected to host numerous dark matter subhaloes, several of which should host faint dwarf companions. Recent Gaia proper motions confirm new members of the LMC system in addition to the previously known SMC, including two classical dwarf galaxies (M∗ > 105 M; Carina and Fornax) as well as several ultrafaint dwarfs (Car2, Car3, Hor1, and Hyd1). We use the Feedback In Realistic Environments (FIRE) simulations to study the dark and luminous (down to ultrafaint masses, M∗ ∼6×103 M) substructure population of isolated LMC-mass hosts (M200m = 1–3×1011 M) and place the Gaia + DES results in a cosmological context. By comparing number counts of subhaloes in simulations with and without baryons, we find that, within 0.2 r200m, LMC-mass hosts deplete ∼30 per cent of their substructure, significantly lower than the ∼70 per cent of substructure depleted by Milky Way (MW) mass hosts. For our highest resolution runs (mbary = 880 M), ∼ 5–10 subhaloes form galaxies with M∗ ≥ 104 M , in agreement with the seven observationally inferred pre-infall LMC companions. However, we find steeper simulated luminosity functions than observed, hinting at observation incompleteness at the faint end. The predicted DM content for classical satellites in FIRE agrees with observed estimates for Carina and Fornax, supporting the case for an LMC association. We predict that tidal stripping within the LMC potential lowers the inner dark matter density of ultrafaint companions of the LMC. Thus, in addition to their orbital consistency, the low densities of dwarfs Car2, Hyd1, and Hyd2 reinforce their likelihood of Magellanic association

Utility of arylhydrazidoyl aryl ethers in heterocycles: A novel synthesis of aryloxypyridazines, phthalazines and thieno-[3,4-d]pyridazine derivatives

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