Synthesis, anti-Infammatory, Analgesic, Molecular Modeling and ADMET Studies of Novel Diclofenac Derivatives Containing Alanyl Moiety

The present work aims to synthesize novel diclofenac derivatives containing L-alanine moiety. The synthesized compounds docked into the active site to discover validated inhibitors of cyclooxygenases (COX-1 and COX-2). The calculations in-silico were predicted that, the compound with lowest energy of docked poses was interacted with residues of active site, perhaps could be making them possible selective inhibitors against (COX-2) and physiologically  active. The binding score of compound compared with reference drug, and show extensive interactions with the targets, which may consider it a suitable selective inhibitor against   (COX-2). Keywords: Alanine, Diclofenac, COX, DOCKING, ADMET

An Examination of the Determinants and Contents of Corporate Voluntary Disclosure of Management\u27s Responsibilities For Financial Reporting

The Sarbanes-Oxley Act (S-O Act) of 2002 requires principal officers to certify under oath to the veracity of information contained in SEC filings and opine on the effectiveness of the internal control system. This study examines the determinants and contents of corporate voluntary disclosure of management\u27s responsibilities during the five-year period preceding the S-O Act. We predict that the voluntary disclosure of management\u27s responsibilities for financial information signals certain incentives and characteristics of the reporting firm that are relevant to financial statement users and regulators. Consistent with our predictions, our findings reveal significant differences between issuing and non-issuing firms as to the effectiveness of an individual firm\u27s internal control system, access to capital markets, audit committee characteristics, and ownership structure. An empirical analysis of the contents of these assertions also reveals different areas of emphasis and selectivity by management, which represents an informative link to existing disclosure mandates. The results of this study contribute to our knowledge of management\u27s motivations for voluntary disclosure and lend credence to the mandatory certification requirements and related disclosure reforms established in the post-Enron era

Market Revaluations of Foreign Listings’ Reconciliations to U.S. Financial Reporting GAAP

The Securities and Exchange Commission (SEC) requires foreign firms wishing to list their securities on the U.S. exchanges to convert their financial statements to U.S.-based generally accepted accounting principles (GAAP) in a reconciliation filing known as Form 20-F. This paper extends prior research analyzing the importance of the SEC requirement by examining the value relevance to U.S. capital markets of Form 20-F reconciliation information under two additional hypotheses related to: i) investors\u27 anticipation of the reconciliation, and ii) investors\u27 perception of foreign countries\u27 enforcement and reliability in applying local accounting rules. We argue that the information content of the Form 20-F reconciliation data is preempted (at least partially) on the date of foreign earnings announcements because of investor anticipation of these reconciliations. Therefore, only significant unanticipated reconciliations exhibit value relevance on the date of filing. In addition, investor perception of the reliability of the reconciliations and the degree of confidence in foreign authorities enforcing local GAAP also affect the value relevance of the reconciliation data. We hypothesize that reconciliations made by firms from countries with mature and developed capital markets should be more value relevant to U.S. investors. Our results show that both unexpected foreign earnings and anticipated reconciliations to U.S. GAAP are significantly associated with unexpected market returns during the week of earnings announcements. The region of the foreign country is also significantly associated with market returns. However, unexpected reconciliations are not significantly associated with unexpected market returns during the week of Form 20-F filing

Dizajniranje i sinteza novih derivata tiofenkarbohidrazida, tienopirazola i tienopirimidina s antioksidativnim i antitumorskim djelovanjem

2-Amino-5-acetyl-4-methyl-thiophene-3-carboxylic acid ethyl ester (1) and 5-acetyl-2-amino-4-methylthiophene-3-carbohydrazide (2) were synthesized and used as starting materials for the synthesis of new series of 1-(5-amino-4-(3,5-dimethyl-1H-pyrazole-1-carbonyl)-3-methylthiophen-2-yl) ethanone (3a), 1-(5-amino-4-(4-chloro-3,5-dimethyl-1H-pyrazole-1-carbonyl)-3-methylthiophen-2-yl) ethanone (3b), 1-(4-methyl-2-amino-5-acetylthiophene-3-carbonyl) pyrazolidine-3,5-dione (4), (Z)-N\u27-(4-methyl-2-amino-5-acetylthiophene-3-carbonyl) formohydrazonic acid (5a), (Z)-ethyl-N\u27-(4-methyl-2-amino-5-acetylthiophene-3-carbonylformo hydrazonate (5b), 6-acetyl-3-amino-2,5-dimethylthieno2,3-dpyrimidin-4(3H)-one (8), 5-methyl-3-amino-2-mercapto-6-acetylthieno2,3-dpyrimidin-4(3H)-one (10) and 5-methyl-6-acetyl-2-thioxo-2,3-dihydrothieno2,3-dpyrimidin-4(1H)-one (12) as potential antioxidant and antitumor agents. Pharmacological results showed that compounds 6a, 6b, 8, 10 and 12 exhibited promising antitumor and antioxidant activity.Etilni ester 2-amino-5-acetil-4-metil-tiofen-3-karboksilne kiseline (1) i 5-acetil-2-amino-4-metiltiofen-3-karbohidrazid (2) sintetizirani su i upotrebljeni kao reaktanti u sintezi novih spojeva 1-(5-amino-4-(3,5-dimetil-1H-pirazol-1-karbonil)-3-metiltiofen-2-il) etanona (3a), 1-(5-amino-4-(4-klor-3,5-dimetil-1H-pirazol-1-karbonil)-3-metiltiofen-2-il) etanona (3b), 1-(4-metil-2-amino-5-acetiltiofen-3-karbonil) pirazolidin-3,5-diona (4), (Z)-N\u27-(4-metil-2-amino-5-acetiltiofen-3-karbonil) formohidrazonske kiseline (5a), (Z)-etil-N\u27-(4-metil-2-amino-5-acetiltiofen-3-karbonilformo hidrazonata (5b), 6-acetil-3-amino-2,5-dimetiltieno2,3-dpirimidin-4(3H)-one (8), 5-metil-3-amino-2-merkapto-6-acetiltieno2,3-dpirimidin-4(3H)-ona (10) i 5-metil-6-acetil-2-tiokso-2,3-dihidrotieno2,3-dpirimidin-4(1H)-ona (12) kao potencijalnih antioksidansa i citostatika. Farmakološka ispitivanja ukazuju na to da spojevi 6a, 6b, 8, 10 i 12 imaju značajno antitumorsko i antioksidativno djelovanje

The Information Content of Earnings Announcements in Regulated and Deregulated Markets: The Case of the Airline Industry

Most of the accounting research examining the information content of earnings assumes a competitive market framework. Little research has been devoted to the value relevance of earnings announcements in regulated markets. This paper examines the information content of earnings releases under two economic conditions facing the airline industry: regulation and deregulation (i.e., competition). We hypothesize that in a deregulated (competitive) environment, there is greater competition, causing more risk and uncertainty for the investor in setting security prices. Therefore, earnings\u27 releases provide more useful information in resolving uncertainties and in formulating and revising the investor\u27s beliefs regarding future earnings and prices in deregulated than for regulated markets. Three critical event periods are examined: the regulation period (1973 - 1975), the transition period (1976 - 1978), and the deregulation period (1979 - 1981). A revaluation index (RI) and a standardized revaluation index (SRI) are used to examine the extent of airline stock price revaluation in response to quarterly accounting earnings releases during the three critical event periods. The results indicate that earnings announcements have value relevance in setting security prices in both regulated and deregulated market conditions. However, the level of the market revaluation to earnings releases is dependent on market structure. The market revaluation to earnings releases is greater in a deregulated (competitive) period than in a regulated one. This result confirms the hypothesis that earnings have more value relevance in competitive markets than in regulated ones. The findings of this research have direct implications for the level of accounting disclosure and the extent of financial reporting in a given market structure. Since financial reporting is a costly process, it becomes important to identify the circumstances under which the level of financial disclosure should be expanded or reduce

Sinteza, in vitro antitumorsko ispitivanje i radiosenzitirajuće vrednovanje novih derivata 4-[3-(supstituiranih)tioureido]-N-(kinoksalin-2-il)benzensulfonamida

Sulfonamides and quinoxaline derivatives possess many types of biological activities and have been recently reported to show substantial antitumor activity. This paper reports the synthesis of novel thioureidosulfaquinoxaline derivatives. All the newly synthesized compounds were evaluated for their in vitro anticancer activity against a human liver cell line (HEPG2) and showed higher activity than the reference drug doxorubicin. 4-(3-(4-Ethylbenzoate)thioureido)-N-(quinoxalin-2-yl)benzenesulfonamide (9) (IC50 = 15.6 µmol L1), N-(pyridin-2-yl)-4-(3-(4-(N-quinoxalin-2-yl-sulfamoyl)phenyl)thioureido)benzene-sulfonamide (10) (IC50 = 26.8 µmol L1) and N-(quinoxalin-2-yl)-4-(3-(4-(N-thiazol-2-ylsulfamoyl)phenyl)thioureido)benzenesulfonamide (11) (IC50 = 24.4 µmol L1) were the most potent compared to doxorubicin (IC50 = 71.8 µmol L1). The most potent compounds 9, 10 and 11 were evaluated as radiosensitizing agents by subjecting the compounds to γ-irradiation (8 kGy).Derivati sulfonamida i kinoksalina imaju raznoliko biološko djelovanje, između ostalog i antitumorsko djelovanje. U radu je opisana sinteza novih derivata tioureido sulfakinoksalina. Svim novim spojevima ispitano je antitumorsko djelovanje in vitro na humanoj staničnoj liniji jetre (HEPG 2). Svi ispitani spojevi pokazuju jači učinak nego referentni lijek doksorubicin. Najjači učinak imali su 4-(3-(4-etilbenzoat)tioureido)-N-(kinoksalin-2-il)benzen-sulfonamid (9) (IC50 = 15,6 µmol L1), N-(piridin-2-il)-4-(3-(4-(N-kinoksalin-2-il-sulfamoil)fenil)tioureido)-benzen-sulfonamid (10) (IC50 = 26,8 µmol L1) i N-(kinoksalin-2-il)-4-(3-(4-(N-tiazol-2-ilsulfamoil)fenil)tioureido)benzen-sulfonamid (11) (IC50 = 24,4 µmol L1), dok je IC50 vrijednost bila 71,8 µmol L1. Najaktivniji spojevi 9, 10 i 11 evaluirani su kao radziosenzitirajuća sredstva nakon izlaganja spojeva γ-zračenju (8 kGy)

EFFECT OF SPRAYING WASHINGTON NAVEL ORANGE TREES WITH SELENIUM ON VEGETATIVE GROWTH, PRODUCTIVITY AND FRUIT QUALITY

ve seasons, 2012 and 2013 in a private orchard in Barshom vallage located at El-Kalubia Governorate Egypt. Washington Navel Orange trees (Citrus Sinensis) budded on sour orange rootstock (Citrus aurantium, L.) were 7- years- old and planted at 5 x 5 meters under basin irrigation system. This investigation aimed to study the effect of selenium (Se) levels (0, 20, 40, 80 and 160 ppm)  as foliar spray on growth, yield, fruit quality, leaf mineral content and enzymes activity of Washington Navel orange trees. The obtained data showed that, selenium had a significant promotive effect on growth, yield, fruit quality, leaf mineral content and enzymes activity of Washington Navel orange trees. Results indicated that treatment of Se at 40 ppm gave the highest significant results, whereas, treatment 160 ppm gave the highest fruit selenium content

Fusing Structural and Functional MRIs using Graph Convolutional Networks for Autism Classification

Geometric deep learning methods such as graph convolutional networks have recently proven to deliver generalized solutions in disease prediction using medical imaging. In this paper, we focus particularly on their use in autism classification. Most of the recent methods use graphs to leverage phenotypic information about subjects (patients or healthy controls) as additional contextual information. To do so, metadata such as age, gender and acquisition sites are utilized to define intricate relations (edges) between the subjects. We alleviate the use of such non-imaging metadata and propose a fully imaging-based approach where information from structural and functional Magnetic Resonance Imaging (MRI) data are fused to construct the edges and nodes of the graph. To characterize each subject, we employ brain summaries. These are 3D images obtained from the 4D spatiotemporal resting-state fMRI data through summarization of the temporal activity of each voxel using neuroscientifically informed temporal measures such as amplitude low frequency fluctuations and entropy. Further, to extract features from these 3D brain summaries, we propose a 3D CNN model. We perform analysis on the open dataset for autism research (full ABIDE I-II) and show that by using simple brain summary measures and incorporating sMRI information, there is a noticeable increase in the generalizability and performance values of the framework as compared to state-of-the-art graph-based models

Sinteza i protuupalno, analgetsko i ulcerogeno djelovanje derivata tieno[2,3-d]pirimidina

5-Methyl-6-phenyl-2-thioxothieno[2,3-d]pyrimidone derivative (2) reacted with hydrazonoyl chloride derivatives to afford triazolothienopyrimidones 4a-f. Also, acetone-1-(2-amino-5-isopropyl-thiophene-3-carbonitrile) (3) reacted with functional and bifunctional groups to yield the corresponding compounds 5-11. The new products showed anti-inflammatory, analgesic, and ulcerogenic activities comparable to that of indomethacin and acetylsalicylic acid, respectively.Reakcijom derivata 5-metil-6-fenil-2-tioksotieno[2,3-d]pirimidona (2) s hidrazonoil kloridima dobiveni su triazolotienopirimidoni 4a-f, a reakcijom aceton-1-(2-amino-5-izopropil-tiopen-3-karbonitrila (3) s funkcionalnim i bifunkcionalnim spojevima dobiveni su produkti 511. Novi spojevi imaju slično protuupalno, analgetsko i ulcerogeno djelovanje kao i indometacin, odnosno acetilsalicilna kiselina