Convenient Synthesis of Some New Bi-heterocycles conataining 3-Aminoquinazolin-4(3H)-one and 1,2,4-Triazole moieties

Dicarboxylic acids, thiosemicarbazides and methylanthranilate reacted to give methyl-2-(3-(5-mercapto-4-s-1,2,4-triazol-3-yl)-3-oxoalkylamino)benzoates 4. The laters, cyclized with hydrazine hydrate to give 3-amino-2-((5-mercapto-4 substitued-1,2,4-triazol-3-yl)alkyl)quinazolin-4(3H)-ones 5 which expected to have biological effects

New Benzoxazole Derivatives as Antiprotozoal Agents: In Silico Studies, Synthesis, and Biological Evaluation

Background. Benzoxazole derivatives have different biological activities. In pursuit of designing novel chemical entities with antiprotozoal and antimicrobial activities, benzoxazolyl aniline was utilized as a privileged scaffold of a series of (3-benzoxazole-2-yl) phenylamine derivatives, 3-benzoxazoloyl acetamide, and butyramide derivatives. Methods. These novel analogs were synthesized in straightforward simple chemistry without any quantitative chromatographic separations in reasonable yields. The biological evaluation of all target compounds as potential antimalarial, antileishmanial, antitrypanosomal, and antimicrobial agents was performed by various well-established cell-based methods. Results. Compounds 6d and 5a showed promising biological screening data. The amidation of 3-benzoxazolyl aniline 1 with the chloroacetyl functional group resulted in a good antimalarial activity and showed moderate inhibitory activities against leishmanial and trypanosomal spp. Moreover, chloroacetyl functionalization of benzoxazolyl aniline serves as a good early goal for constructing and synthesizing new antimicrobial and antiprotozoal agents. The molecular docking study rationalizes the relative inhibitory activity of compound 5a as an antimalarial agent with the deregulation of PfPNP activity which has emerged as a major mechanism of these targets

Characterization of Protein Complexes and Subcomplexes in Protein-Protein Interaction Databases

The identification and characterization of protein complexes implicated in protein-protein interaction data are crucial to the understanding of the molecular events under normal and abnormal physiological conditions. This paper provides a novel characterization of subcomplexes in protein interaction databases, stressing definition and representation issues, quantification, biological validation, network metrics, motifs, modularity, and gene ontology (GO) terms. The paper introduces the concept of “nested group” as a way to represent subcomplexes and estimates that around 15% of those nested group with the higher Jaccard index may be a result of data artifacts in protein interaction databases, while a number of them can be found in biologically important modular structures or dynamic structures. We also found that network centralities, enrichment in essential proteins, GO terms related to regulation, imperfect 5-clique motifs, and higher GO homogeneity can be used to identify proteins in nested complexes

Sacrococcygeal teratoma excision: a vertical rather than transverse wound closure

Background: The chevron incision has been the standard approach for sacrococcygeal teratoma (SCT) excision. Here, we are reporting our experience of shifting to the vertical posterior sagittal approach.Patients and methods: During the period 2011 through 2016, we operated on 17 (16 female and one male) cases of SCT. Their age at presentation ranged from day 1 to 26 months (mean=4.8 months, median=2 months). The chevron incision was used in five, whereas the vertical posterior sagittal approach was used in 12 patients.Results: In this series, we had one case of perioperative mortality, in addition to another case of perineal wound disruption (in the group of vertical wound closure), which was managed conservatively (to heal by secondary intention) with a very satisfactory hidden scar at 6-month follow-up. Overall, we did not find the vertical approach to add any extra limitations to the surgical exposure or dissection; meanwhile, it provided a well-recognized cosmetic advantage.Conclusion: The vertical posterior sagittal approach for excision of SCT is both feasible and advantageous in terms of the cosmetic outcome. It provides a well-hidden scar in the natal cleft and preserves normal contouring of the buttocks.Keywords: buttock, cosmesis, posterior sagittal, reconstruction, sacrococcygeal teratom

Use of bioresorbable vascular scaffold : a meta-analysis of patients with coronary artery disease

BACKGROUND: Differences in outcomes between bioresorbable vascular scaffold (BVS) systems and drug-eluting metal stents (DES) have not been fully evaluated. We aimed to compare clinical and angiographic outcomes in randomised studies of patients with coronary artery disease (CAD), with a secondary analysis performed among registry studies. METHODS: A meta-analysis comparing outcomes between BVS and DES in patients with CAD. Overall estimates of treatment effect were calculated with random-effects model and fixed-effects model. RESULTS: In 6 randomised trials (3818 patients), BVS increased the risk of subacute stent thrombosis (ST) over and above DES (OR 2.14; CI 1.01 to 4.53; p=0.05), with a trend towards an increase in the risk of myocardial infarction (MI) (125 events in those assigned to BVS and 50 to DES; OR 1.36; CI 0.97 to 1.91; p=0.07). The risk of in-device late lumen loss (LLL) was higher with BVS than DES (mean difference 0.08 mm; CI 0.03 to 0.13; p=0.004). There was no difference in the risk of death or target vessel revascularisation (TVR) between the two devices. In 6 registry studies (1845 patients), there was no difference in the risk of death, MI, TVR or subacute ST between the two stents. Final BVS dilation pressures were higher in registry than in randomised studies (18.7±4.6 vs 15.2±3.3 atm; p<0.001). CONCLUSIONS: Patients treated with BVS had an increased risk of subacute ST and slightly higher LLL compared with those with DES, but this might be related to inadequate implantation techniques, in particular device underexpansion.Peer reviewedFinal Published versio

EXTRACTION, FRACTIONATION AND CHARACTERIZATION OF COWPEA (VIGNA UNGUICULATA) GLOBULINS

The proteins were extracted from cowpea seeds by buffered saline solution and the globulins were separated by dialyzing the protein extract against distilled water. Fractionation of the total globulins on Sephacryl S-200 column produced two major and one minor components. The molecular weight of the major globulin components were estimated to be greater than 250000 and 178 000 for the globulin component (a) and (b) respectively and the latter component was the predominant globulin. The two major globulin components were free from contamination of other proteins as shown by polyacrylamide gel electrophoresis. Spectrophotometry and amino acid analyses were used as tools for characterizing the globulin components