Sinteza i biološka evaluacija nekih pirimidina, pirimido[2,1-b][1,3]tiazina i tiazolo[3,2-a]pirimidin derivata

4,6-Diamino-1H-pyrimidine-2-thione (1) was used for the preparation of the pyrimidine derivatives 2-5. Compound 5 was cyclized to produce pyrimido[2,1-b][1,3]thiazine derivatives 6, which was condensed with p-chlorobenzaldehyde to give compound 7. The latter compound was reacted with hydroxylamine to give isoxazolo[4,5-d]thiazino[2,3-a]pyrimidines 8. Compound 8b was treated with 2-chloroethyl methyl ether to afford compound 9. Similarly, compound 3 was reacted with chloroacetic acid to give thiazolo[3,2-a]pyrimidine 10, which was condensed with p-chlorobenzaldehyde to give compound 11. Compound 11 was condensed with hydroxylamine to give isoxazolo[4,5-d]thiazolo[2,3-a]pyrimidine 12. Compound 12b was treated with 2-chloroethyl methyl ether to afford compound 13. The biological evaluation of some prepared products showed that many of them revealed promising antimicrobial activity.4,6-Diamino-1H-pirimidin-2-tion (1) upotrebljen je kao ishodni spoj u sintezi derivata pirimidina 2-5. Spoj 5 je cikliziran u pirimido[2,1-b][1,3]tiazin derivat 6, koji je kondenziran s p-klorbenzaldehidom u spoj 7. Produkt 7 je u reakciji s hidroksilaminom dao izoksazol[4,5-d]tiazino[2,3-a]pirimidin 8. Spoj 8b je u reakciji s 2-kloretil metil eterom dao spoj 9. Slično je spoj 3 reagirao s kloroctenom kiselinom i dao tiazol[3,2-a]pirimidin 10, koji je kondenziran s p-klorbenzaldehidom u produkt 11. Spoj 11 je kondenzacijom s hidroksilaminom dao izoksazol[4,5-d]tiazolo[2,3-a]pirimidin 12. Spoj 12b je s 2-kloretil metil eterom dao produkt 13. Biološka evaluacija pokazuje da neki od sintetiziranih produkata imaju antimikrobno djelovanje

QUERCETIN AND ELLAGIC ACID IN GASTRIC ULCER PREVENTION: AN INTEGRATED SCHEME OF THE POTENTIAL MECHANISMS OF ACTION FROM IN VIVO STUDY

  Objective: The present study was initiated to describe the gastroprotective role of quercetin (Qu) and ellagic acid (EA) on aspirin-induced gastric ulcer (GU) in rats.Methods: Forty adult female albino rats of Wistar strain were distributed into: Control group, GU group, Omeprazole group, Qu group, and EA group. Gross examination, biochemical analyses including serum adrenocorticotropic hormone (ACTH), serotonin (ST), ferritin, heme oxygenase-1 (HO-1), interleukin-2 (IL-2), advanced glycosylation end products (AGEs), and fibronectin (FN) levels were estimated. Moreover, histopathological and histochemical examinations of stomach tissue samples were carried out.Results: Gross examination of gastric mucosa of rats in GU group revealed hyperemia of the stomach mucosa. Furthermore, rats in GU group experienced a significant rise in serum ACTH, ferritin, HO-1, IL-2 and AGEs levels accompanied with significant drop in serum ST and FN levels versus control counterparts. Pre-treatment of GU group with Omeprazole, Qu or EA caused marked improvement in the measured biochemical parameters. Histopathological and histochemical examinations of stomach tissue samples documented the protective action of Omeprazole, Qu and EA with different degrees against GU caused by aspirin.Conclusion: As a conclusion to this study, we can state that both Qu and EA have gastroprotective effect against aspirin-induced GU in rat model. Of note, Qu showed superior impact than EA as an antiulcer agent in this study. The corresponding mechanisms are speculated to be associated with inhibiting stress-induced gastric lesion, attenuating the oxidative stress, iron chelation and blunting ferritin level, modulating inflammatory cascade, and promoting the healing process

Influence of the analysis technique on estimating hepatic iron content using MRI

Peer Reviewedhttp://deepblue.lib.umich.edu/bitstream/2027.42/134998/1/jmri25317.pdfhttp://deepblue.lib.umich.edu/bitstream/2027.42/134998/2/jmri25317_am.pd

Task Scheduling Optimization in Cloud Computing by Jaya Algorithm

Cloud computing provides resources to its consumers as a service. The cloud computing paradigm offers dynamic services by providing virtualized resources via the internet for enabling applications, and these services are provided by large-scale data centers known as clouds. Cloud computing is entirely reliant on the internet to provide its services to consumers. Cloud computing offers several advantages, including the fact that users only pay for what they use weekly, monthly, or yearly, that anybody with an internet connection may use the cloud, and that there is no need to purchase resources, hardware, or software on their own. This paper proposes an efficient task scheduling algorithm based on the Jaya algorithm for the cloud computing environment. We evaluate the performance of our method by applying it to three instances. The recommended technique produced the optimal solution in makespan, speedup, efficiency, and throughput, according to the findings

Radiological evaluation of postoperative complications after non-sleeve gastrectomy bariatric procedures

Background: Obesity is a medical condition, which may lead to serious related diseases, ultimately, resulting in many morbidities and early mortality. Its management involves many approaches of which bariatric surgery is considered nowadays as one of the most effective treatment for it. However, follow up of postoperative complications of this surgery by effective radiological method as computed tomography (CT) is important for assessment of its success.Objective: The aim of this study was to illuminate the radiological signs and features of postoperative complications after non sleeve bariatric procedures and stressing the importance of using multi-slice CT (MSCT), and fluoroscopic study for detection of these complications. Patients and methods: An observational cohort study for 275 patients with suspected complications after non sleeve gastrectomy bariatric procedures, including 195 patients after Roux-en-Y gastric bypass (RYGB), 76 patients after laparoscopic adjustable gastric banding (LAGB) and 4 patients after intragastric balloon placement was done. These patients were subjected to either multi-slice CT and or fluoroscopy. Results: We detected complications in 21 patients out of the 195 patients who underwent RYGB: leakage, abscess, intestinal obstruction, internal hernia, port site ventral hernia, intussusception, fistula between the gastric pouch and the excluded stomach and hiatus hernia. On the other hand, 8 out of 76 patients operated by LAGB developed complications: band slippage, band erosion, pouch dilatation and tubal disconnection. Lastly two out of the 4 patients who placed intra-gastric balloon encountered other complications: gastric outlet obstruction, spontaneous balloon deflation and distal migration with intestinal obstruction.Conclusion: It could be concluded that bariatric procedures may be followed by many complications and accurate diagnosis of these problems by proper radiological procedures as MSCT is imperative

Sexual behaviour of pregnant women attending antenatal care clinic at Assiut Women's Health Hospital, Egypt

Background: The aim of the current study was to describe the knowledge, attitudes, beliefs and behavior of pregnant women regarding sexuality during pregnancy. Study was carried out at Women’s Health Hospital, Assiut University, Egypt.Methods: A cross-sectional study included pregnant women at different gestational ages between December 2016 and Jun 2017 recruited consecutively at the antenatal outpatient clinic of women’s Health Hospital at Assiut University. We used the Arabic version of the Female Sexual Function Index (Ar-FSFI) in the interview to evaluate the sexual functions or problems during the last month. The cut-off score used to indicate sexual dysfunction was 28.1. The obtained data were analyzed by means of SPSS software (version 22.0) and p<0.05 was taken as the significant level.Results: The study included 140 pregnant women at different ages and trimesters and also at different socio-economic states. Concerning the level of knowledge, the classification in recorded a mean score =11.91±4.05 which revealed a level of knowledge below average. Regarding the extent of beliefs in relation to sexuality during pregnancy, the mean score=2.72 of the respondents’ beliefs means that the impact of the beliefs regarding sexuality during pregnancy was weak among respondents. On assessing their perceptions about sexual intercourse during pregnancy, majority of them [130 (93.1%)] felt that sex have no negative impacts on pregnancy while 10 (6.9%) opined that sex during pregnancy had negative effects. Perceived negative effects of sex during pregnancy included vaginal bleeding and miscarriage.Conclusions: The low rate of sexual activity in our study, regardless question about the taboo of sexual intercourse during pregnancy, could be related to a cultural background in which women avoid speaking about their desires and sexual needs

Honeypot Allocation for Cyber Deception in Dynamic Tactical Networks: A Game Theoretic Approach

Honeypots play a crucial role in implementing various cyber deception techniques as they possess the capability to divert attackers away from valuable assets. Careful strategic placement of honeypots in networks should consider not only network aspects but also attackers' preferences. The allocation of honeypots in tactical networks under network mobility is of great interest. To achieve this objective, we present a game-theoretic approach that generates optimal honeypot allocation strategies within an attack/defense scenario. Our proposed approach takes into consideration the changes in network connectivity. In particular, we introduce a two-player dynamic game model that explicitly incorporates the future state evolution resulting from changes in network connectivity. The defender's objective is twofold: to maximize the likelihood of the attacker hitting a honeypot and to minimize the cost associated with deception and reconfiguration due to changes in network topology. We present an iterative algorithm to find Nash equilibrium strategies and analyze the scalability of the algorithm. Finally, we validate our approach and present numerical results based on simulations, demonstrating that our game model successfully enhances network security. Additionally, we have proposed additional enhancements to improve the scalability of the proposed approach.Comment: This paper accepted in 14th International Conference on Decision and Game Theory for Security, GameSec 202

Novel synthesis, ring transformation and anticancer activity of 1,3-thiazine, pyrimidine and triazolo[1,5-a]pyrimidine derivatives

Synthesis, heterocyclization and anticancer activity of a new series of heterocyclic compounds are described. Aminothiazine 1 was obtained from the base induced condensation of thiourea, benzaldehyde and ethyl cyanoacetate. The synthesis of N-phenyl amino pyrimidine derivative 2 was obtained as a result of reaction of aniline with compound 1. Compound 2 underwent ring opening and recyclization upon reaction with HCl or H2O2/ NaOH to afford the acid derivative 3 or oxazine 4, respectively. Thiazine 1 undergoes ring transformation upon the effect of NH2OH.HCl to produce pyrimidine derivative 5. Heterocyclization of compound 1 with thiosemicarbazide followed by oxidation with I2/AcOH afforded triazolopyrimidine 6 and 7, respectively. Alkylation of compound 1 was promoted by reaction of 1 with ethyl iodide to give alkylated thiazine 8 which in turn undergo ring transformation when subjected to reaction with hydrazine hydrate to give pyrazole derivative 9. Refluxing of amino-1,3-thiazine derivative 1 with ethyl bromoacetate in the presence of Et3N produce the alkylated pyrimidine product 10. Hydrazonolysis of 1,3-thiazine 1 with hydrazine or phenyhydrazine gave pyrimidine derivatives 11a,b, respectively. Compound 11b was cyclized with carbon disulfide or formaldehyde to produce triazolopyrimidines 12 and 13, respectively. Some of the new compounds were screened for anticancer activity and significant results were found for some compounds.               KEY WORDS: 1,3-Thiazine, Pyrimidine, Triazole, Pyrazole, Anticancer activity Bull. Chem. Soc. Ethiop. 2018, 32(3), 513-522.DOI: https://dx.doi.org/10.4314/bcse.v32i3.1