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21.

Background:

Laparoscopic pyeloplasty is one of the most common reconstructive procedures performed by urologists. Both continuous and interrupted sutures are being practiced for ureteropelvic anastomosis. The success rate and the complications associated with the suturing technique needs evaluation. We analyzed the results from of our patients who underwent laparoscopic pyeloplasty using both techniques.

Objective:

To review the outcome differences among patients undergoing laparoscopic pyeloplasty regarding suturing technique.

Materials and Methods:

All patients who underwent laparoscopic, transperitoneal dismembered pyeloplasty of the primary pelviureteric obstruction were analyzed. The primary outcome was successful pyeloplasty, as assessed by the resolution of symptoms and T½ <10 minutes. The secondary outcomes were the complication rate and the operative parameters. The difference in the parameters was assessed by Student t test analysis.

Results:

Of the 107 patients we studied, 65 had interrupted suturing and 42 had continuous suturing. The success rate was not significantly different among the 2 groups. The mean suturing time, postoperative drainage volume, postoperative hospital stay, and total cost of the procedure were significantly less in the continuous suturing group.

Conclusion:

The continuous suturing technique is preferred over the interrupted suturing technique for laparoscopic pyeloplasty because the success rates are equal and the postoperative stay, suturing time, drain output, and cost of the procedure are better.  相似文献   
22.
A new one pot assembly of highly functionalized benzo[a]phenazinone fused chromene/bicyclic scaffolds via a domino Knoevenagel intramolecular hetero-Diels–Alder (IMHDA) strategy using a solid state melt reaction (SSMR) of 2-hydroxynaphthalene 1,4-dione, o-phenylenediamine, O-allyl salicylaldehyde/O-vinyl salicylaldehyde derivatives is reported. The formation of five new bonds (two C–C bonds and three C–O bonds), three six-membered rings, and three stereogenic centers in a one-pot manner is very attractive. Ease of reaction with short time, good yields with water as the only byproduct and work up free procedure are some of the excellent features of the present protocol.

A new one pot assembly of highly functionalized benzo[a]phenazinone fused chromene/bicyclic scaffolds via a domino Knoevenagel intramolecular hetero-Diels–Alder (IMHDA) strategy using a solid state melt reaction (SSMR) is reported.

Multicomponent reactions (MCRs)1 are known to construct complex structures from simple starting materials in a rapid and highly efficient manner where the production of wastes is minimized. Those multicomponent reactions which are carried out in a ‘one-pot’ MC sequential manner provide a high degree of reaction mass efficiency, which is crucial in the development of modern synthetic methodology for drug discovery and pharmaceutical programs.2 Enormous work has been carried out in the field of multicomponent reactions in the past decade where several MCRs have been developed and extensively used in natural product synthesis and drug discovery. The Ugi reaction is a prime example of a four-component reaction that has been found to be a powerful and efficient method for the preparation of α-amino amides both in academia and industry.3 Therefore, the development of new MCRs for the synthesis of biologically active molecules continues to attract considerable attention for their atom- and step economy features.Heterocycles having nitrogen atom are widely available in nature and possess diverse and important biological activities.4 Phenazines are a group of organic compounds known to the mankind since past 150 years and are known to exhibit significant biological activities such as antimalarial, fungicidal, trypanocidal, antiplatelet, etc.5 A large number of drug molecules bearing the phenazine scaffold have been designed and evaluated in the recent years. The phenazines motif possess two dentate N atoms with three fused aromatic rings and an electron deficient conjugated system. The presence of the above features in phenazines give them an ability to form hydrogen bonds, ionic bonds, and π–π interactions with relative ease, and their use has also been demonstrated in supramolecular chemistry for molecular recognition (MR), supramolecular self-assembly (MS-A), and organic optic electronics materials.6 Few representative examples of phenazine and its derivatives are shown in the Fig. 1.Open in a separate windowFig. 1Some of naturally occurring phenazine derivatives.Chromenes and their derivatives are privileged scaffolds due to their ubiquitous presence in many natural products and synthetic molecules.7 Chromenes are also an important class of compounds displaying interesting biological activities against prostate cancer (DU-145) and breast cancer (MCF-7).8 Additionally, they have medicinal qualities such as antiviral and antimicrobial activity.9 Chromenes have also found their use in medicine, health-promoting agents, and photochromic materials.10In recent years, the domino-Knoevenagel-hetero-Diels–Alder reaction (DKHDA) which was extensively studied by Tietze''s group constitutes an important process for the preparation of complex compounds having interesting biological properties.11 The Diels–Alder reaction is important since it allows the formation of functionalized rings where there is complete control on regio-, diastereo-, and enantioselectivity. Moreover, the concerted nature of the Diels–Alder reactions allow the selective formation of up to three stereogenic centers in a single reaction step. Majority of the reactions reported on DKHDA have utilized 1,3-dicarbonyl compounds such as dimethyl barbituric acid, Meldrum''s acid and 1,3-indanedione.12 Additionally, other active methylene compounds like 1-phenyl-3-methyl pyrazolone, 4-hydroxy-coumarin, dihydroindole-2-thione, benzoylacetonitrile, 4-hydroxydithiocoumarin have been also used;13 but phenazinones have never been employed in DKHDA reactions. To the best of our knowledge, there are no reports on intramolecular DKHDA reactions using phenazinone as the coupling partner. Due to our interest in the construction of bioactive fused chromenophenazinone derivatives and since this molecule contains a 1,3-dicarbonyl as well as a 1,3-imine moiety, it would be very challenging to control the regioselectivity of the molecule; therefore phenazinone scaffold can act as a model substrate for an intramolecular DKHDA. We envisaged that a series of angular polycyclic chromeno fused phenazinone derivatives could be obtained and it is possible that the final hybrid compounds will result in being more selective and efficient than chromene and phenazinone compounds in biological assays.In this direction, we have decided to develop a new method for the preparation of novel benzo[a]phenazinone fused chromene/bicyclic scaffolds via a domino Knoevenagel intramolecular hetero-Diels–Alder (IMHDA) strategy using a solid state melt reaction (SSMR). As part of our research program for the development of new synthetic methods in heterocyclic chemistry14 and solid state melt reactions,15,16 we would like to report a simple and a general domino three-component reaction of 2-hydroxynaphthalene-1,4-dione, o-phenylenediamine and O-allylated/vinylated salicylaldehyde for the synthesis of pentacyclic benzo[a]phenazinone fused chromene/bicyclic scaffolds under environmentally benign reaction conditions (Scheme 1).Open in a separate windowScheme 1Synthetic approach to benzo[a]phenazinone fused chromenes.We have started this study by melting 2-hydroxynaphthalene-1,4-dione (2), o-phenylenediamine (1), and (E)-methyl 2-((2-formylphenoxy)methyl)-3-phenylacrylate (3) at 180 °C for 1 h in solvent free condition. Unfortunately, we could not obtain any desired product and the formation of a complex mixture was observed. To minimize the formation of the side products, the 2-hydroxynaphthalene-1,4-dione (2) and o-phenylenediamine (1) were first melted at 180 °C for 10 minutes to form the intermediate benzo[a]phenazin-5-ol. Subsequently, (E)-methyl 2-((2-formylphenoxy)methyl)-3-phenylacrylate 3a was added and the mixture was melted under the same temperature for 1 h which afforded the desired hybrid product chromene fused benzo[a]phenazinone 4a (ester moiety in ring junction) in 78% yield as shown in
Open in a separate windowaAll reactions were carried out on 1 mmol scale of o-phenylenediamine (1a–c) 2-hydroxynaphthalene-1,4-dione (2), and O-allylated salicylaldehyde derivatives (3a–o) at 180 °C for 1 h.bIsolated yield of the pure products (4a–q).cAll compounds were fully characterized (see ESI).This two-step procedure allows the one-pot three-component reaction to be controlled, avoiding the separation of intermediates, as well as time-consuming and costly purification processes. It is also important to mention here that the reaction is not only diastereoselective, but also chemoselective. Among the two possible hetero diene such as C Created by potrace 1.16, written by Peter Selinger 2001-2019 O and C Created by potrace 1.16, written by Peter Selinger 2001-2019 N from phenazine ring, only the C Created by potrace 1.16, written by Peter Selinger 2001-2019 N diene is involved in the reaction which clearly shows the chemo-selective nature of the reaction (Fig. 2).Open in a separate windowFig. 2Competitive two different heterodienes present in the intermediate.To expand the scope of this one pot reaction, by following the aforementioned procedure, we treated a variety of O-allylated salicylaldehyde derivatives (3b–o) and melted with o-phenylenediamine (1a–c), 2-hydroxynaphthalene-1,4-dione (2), which successfully yielded the desired fused novel benzo[a]phenazinone fused chromene derivatives 4b–q in 71–80% yields. The isolated yields of the pure products (4b–q) are summarized in Open in a separate windowaAll reactions were carried out on 1 mmol scale of o-phenylenediamine (1a–b), 2-hydroxynaphthalene-1,4-dione (2), and O-allylated salicylaldehyde derivatives (5a–e) at 180 °C for 1 h.bIsolated yield of the pure products (6a–f).cAll compounds were fully characterized (see ESI).Further, to explore this methodology, we have prepared a variety of vinylogous carbonate derivatives (7a–d) and treated with o-phenylenediamine (1) and 2-hydroxynaphthalene-1,4-dione (2) for 1 h at 180 °C which successfully provided the novel benzo[a]phenazinones fused bicyclic scaffolds compounds (8a–d) in 94–96% yields ( Open in a separate windowaAll reactions were carried out on 1 mmol scale of o-phenylenediamine (1a), 2-hydroxynaphthalene-1,4-dione (2), and vinylogous carbonate derivatives (7a–d) at 180 °C for 1 h.bIsolated yield of the pure products (8a–d).cAll compounds were fully characterized (see ESI).This one pot domino reaction is highly stereoselective in nature and was evidenced by single crystal X-ray analyses.17 The stereochemistry of the compounds 4l and 8b is confirmed by X-ray crystallographic analysis (Fig. 3). It can be seen from the crystal structure that the phenyl group and the adjacent ester moiety are in the anti-orientation in benzo[a]phenazinone-fused chromene (4l) which is due to the initial trans geometry of the phenyl group and ester moiety present in the double bond at vicinal position of the compound 4l. Similarly, the ORTEP diagram of compound 8b (Fig. 3) clearly demonstrates that the relative stereochemistry of the ester at the ring junction and the ring junction hydrogen are in syn-orientation with each other.Open in a separate windowFig. 3X-ray crystal structure of 4l and 8b.17  相似文献   
23.
Experimental and DFT studies on the ultrasonic energy-assisted extraction of the phytochemicals of Catharanthus roseus as green corrosion inhibitors for mild steel in NaCl medium     
N. Palaniappan  I. Cole  F. Caballero-Briones  S. Manickam  K. R. Justin Thomas  D. Santos 《RSC advances》2020,10(9):5399
Catharanthus roseus (Apocynaceae family) extract is rich in organic phytochemicals such as alkaloids, polyphenolic compounds, and flavonoids. It contains several functional entities such as fused heterocycles, and hydroxyl and carbonyl groups, which could be useful for corrosion inhibition of mild steel in NaCl environments. In the present work, ultrasonic energy was used to obtain the ethanolic extracts of root and stem which were then tested as corrosion inhibitors for mild steel in the presence of 3.5% NaCl. The corrosion inhibition process was studied by UV-visible spectroscopy, Fourier transform infrared spectroscopy, atomic force microscopy, weight loss, and electrochemical methods. After immersing in the corrosive medium, the microstructures of mild steel were investigated by scanning electron microscopy, X-ray diffraction, and ellipsometry. The extract of C. roseus showed excellent adsorption on mild steel surface as confirmed by DFT calculations. The results indicate that the extract of C. roseus acts as a mixed type corrosion inhibitor, where the stem extract is the most efficient inhibitor in 3.5% NaCl solution possibly due to the higher active area of stem phytochemicals.

C. roseus phytochemicals are physisorbed on the 111 Fe surface, and the oxygen non-bonding electron chemisorbed on the polarized state 111 Fe surface.  相似文献   
24.
PhageLeads: Rapid Assessment of Phage Therapeutic Suitability Using an Ensemble Machine Learning Approach     
Kumarasan Yukgehnaish  Heera Rajandas  Sivachandran Parimannan  Ravichandran Manickam  Kasi Marimuthu  Bent Petersen  Martha R. J. Clokie  Andrew Millard  Thomas Sicheritz-Pontn 《Viruses》2022,14(2)
The characterization of therapeutic phage genomes plays a crucial role in the success rate of phage therapies. There are three checkpoints that need to be examined for the selection of phage candidates, namely, the presence of temperate markers, antimicrobial resistance (AMR) genes, and virulence genes. However, currently, no single-step tools are available for this purpose. Hence, we have developed a tool capable of checking all three conditions required for the selection of suitable therapeutic phage candidates. This tool consists of an ensemble of machine-learning-based predictors for determining the presence of temperate markers (integrase, Cro/CI repressor, immunity repressor, DNA partitioning protein A, and antirepressor) along with the integration of the ABRicate tool to determine the presence of antibiotic resistance genes and virulence genes. Using the biological features of the temperate markers, we were able to predict the presence of the temperate markers with high MCC scores (>0.70), corresponding to the lifestyle of the phages with an accuracy of 96.5%. Additionally, the screening of 183 lytic phage genomes revealed that six phages were found to contain AMR or virulence genes, showing that not all lytic phages are suitable to be used for therapy. The suite of predictors, PhageLeads, along with the integrated ABRicate tool, can be accessed online for in silico selection of suitable therapeutic phage candidates from single genome or metagenomic contigs.  相似文献   
25.
Prognostic stratification of oestrogen receptor‐positive HER2‐negative lymph node‐negative class of breast cancer          下载免费PDF全文
Emad A Rakha  Devika Agarwal  Andrew R Green  Ibraheem Ashankyty  Ian O Ellis  Graham Ball  Mohammed A Alaskandarany 《Histopathology》2017,70(4):622-631
  相似文献   
26.
Specific detection of fungal pathogens by 18S rRNA gene PCR in microbial keratitis   总被引:1,自引:0,他引:1  
Zunaina Embong  Wan Hazabbah Wan Hitam  Chan Yean Yean  Nur Haslindawaty Abdul Rashid  Balqis Kamarudin  Siti Khaironi Zainal Abidin  Sabariah Osman  Zainul F Zainuddin  Manickam Ravichandran 《BMC ophthalmology》2008,8(1):7

Background  

The sensitivity and specificity of 18S rRNA polymerase chain reaction (PCR) in the detection of fungal aetiology of microbial keratitis was determined in thirty patients with clinical diagnosis of microbial keratitis.  相似文献   
27.
Strong association between house characteristics and malaria vectors in Sri Lanka     
Konradsen F  Amerasinghe P  van der Hoek W  Amerasinghe F  Perera D  Piyaratne M 《The American journal of tropical medicine and hygiene》2003,68(2):177-181
The objective of this study was to determine whether house characteristics could be used to further refine the residual insecticide-spraying program in Sri Lanka. Indoor-resting mosquito densities were estimated in 473 houses based on fortnightly collections over a two-and-a-half-year period. The type of house construction and the exact location of all houses were determined. In a multivariate analysis, distance of less than 750 meters between a house and the main vector-breeding site was strongly associated with the presence of Anopheles culicifacies in the house (odds ratio [OR] 4.8, 95% confidence interval [CI] 3.4-6.8) and to a lesser extent with the presence of An. subpictus (OR 1.4, 95% CI 1.1-1.7). Poor housing construction also was an independent risk factor (OR for An. culicifacies 1.3, 95% CI 1.0-1.9; OR for An. subpictus 1.3, 95% CI 1.0-1.6). It is recommended that a malaria control strategy focus on residential areas within 750 meters of streams and rivers, with special attention given to areas with the poorest type of house construction.  相似文献   
28.
A seroepidemiological study of toxocariasis and risk factors for infection in children in Sri Lanka     
Iddawela DR  Kumarasiri PV  de Wijesundera MS 《The Southeast Asian journal of tropical medicine and public health》2003,34(1):7-15
A seroepidemiology study using TES-ELISA was carried out in 1,020 children aged 1-12 years in the Hindagala Community Health Project, Sri Lanka. Toxocariasis seroprevalence was 43% with 16.6% showing high antibody levels. Unconditional logistic regression analysis showed 7-9 year olds to be at the highest risk (OR 3.0820; CI = 1.95-4.87). Dog ownership, especially puppies (OR 29.28; CI = 7.40-116.0), and geophagia-pica (OR 6.3732; CI = 3.87-10.50), were significant risk factors. Family clustering of toxocariasis was significant (chi2 = 88.000; p = 0.0001). Abdominal pain (45%), cough (30%), limb pain (23%) and skin rashes (20%) were significantly associated with seropositivity indicating that toxocariasis causes covert morbidity. These findings are, overall, applicable to other areas in Sri Lanka. However, in the dry zone, survival of infective eggs in the soil could be affected by the climate while more importantly, in agricultural areas with a high buffalo population, Toxocara vitulorum could account for human toxocariasis. Using a species specific double sandwich ELISA based on 57 kDa protein of T. canis ES antigen, it is demonstrated that 91% of the seropositives were due to T. canis. Thus along with rabies and dirofilariasis, toxocariasis is an important zoonotic health hazard from dogs in Sri Lanka and prevention is indicated.  相似文献   
29.
Biological and chemical inhibitors of NF-kappaB sensitize SiHa cells to cisplatin-induced apoptosis   总被引:8,自引:0,他引:8  
Venkatraman M  Anto RJ  Nair A  Varghese M  Karunagaran D 《Molecular carcinogenesis》2005,44(1):51-59
Cisplatin, a chemotherapeutic agent, is known to induce apoptosis of cancer cells. We examined the role of NF-kappaB during cisplatin-induced apoptosis in two human cervical cancer cell lines, HeLa and SiHa, known to differ in their response to cisplatin treatment. We found that SiHa cells were relatively more resistant than HeLa cells to the cytotoxic effects induced by cisplatin as measured by MTT assays. HeLa cells were more sensitive to the apoptotic effects induced by cisplatin as shown by increases in annexin staining, DNA fragmentation, and loss of mitochondrial membrane potential. Similarly the activities of caspases 3, 8, and 9 and cleavage of PARP induced by cisplatin were more in HeLa than SiHa cells. Cisplatin induced NF-kappaB DNA binding activity in HeLa and SiHa cells but not in primary cervical cells and the active DNA binding complex in SiHa cells consists of p50 and RelA heterodimers. However, when NF-kappaB DNA binding activity was blocked by chemical (curcumin, PDTC, or salicylic acid) or biological inhibitors (NIK-KM or IKK-beta DN), the cell viability was less in SiHa cells with cisplatin treatment, but these effects were not observed in HeLa cells. Similarly upon treatment with cisplatin SiHa cells had more activation of caspases compared to that seen in HeLa cells under conditions of NF-kappaB inhibition by biological or chemical inhibitors. These results suggest that NF-kappaB may contribute to the resistance of human cervical cancer cells to cisplatin and highlight the potential use of combination therapy involving cisplatin and NF-kappaB inhibitors.  相似文献   
30.
Concealed penis   总被引:4,自引:0,他引:4  
Radhakrishnan J  Razzaq A  Manickam K 《Pediatric surgery international》2002,18(8):668-672
A small phallus causes great concern regarding genital adequacy. A concealed penis, although of normal size, appears small either because it is buried in prepubic tissues, enclosed in scrotal tissue penis palmatus (PP), or trapped due to phimosis or a scar following circumcision or trauma. From July 1978 to January 2001 we operated upon 92 boys with concealed penises; 49 had buried penises (BP), while PP of varying degrees was noted in 14. Of 29 patients with a trapped penis, phimosis was noted in 9, post-circumcision cicatrix (PCC) in 17, radical circumcision in 2, and posttraumatic scarring in 1. The BP was corrected at 2-3 years of age by incising the inner prepuce circumferentially, degloving the penis to the penopubic junction, dividing dysgenetic bands, and suturing the dermis of the penopubic skin to Buck's fascia with nonabsorbable sutures. Patients with PP required displacement of the scrotum in addition to correction of the BP. Phimosis was treated by circumcision. Patients with a PCC were recircumcised carefully, preserving normal skin, but Z-plasties and Byars flaps were often required for skin coverage. After radical circumcision and trauma, vascularized flaps were raised to cover the defect. Satisfactory results were obtained in all cases although 2 patients with BP required a second operation. The operation required to correct a concealed penis has to be tailored to its etiology.  相似文献   
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