Minor groove binders: some recent research in drug development

The role of the naturally occurring polyamides distamycin and netropsin as antibacterial agents is described. Also, the importance of the modifications to the lipophilic and hydrophobic moieties is discussed. It has also been shown that these DNA minor groove binding compds. can be used to treat other diseases such as sleeping sickness when the right modifications have been employed. Examples of the synthetic strategy of these polypyrroles are also highlighted in this review

Editorial: Female genital cutting/mutilation in Africa deserves special concern: An overview

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Methyl 2-amino-5-iso­propyl-1,3-thia­zole-4-carboxyl­ate

The title compound, C8H12N2O2S, forms a supramolecular network based on N-HN hydrogen-bonded centrosymmetric dimers that are linked in turn by N-HO contacts

Shooting Neural Networks Algorithm for Solving Boundary Value Problems in ODEs

The objective of this paper is to use Neural Networks for solving boundary value problems (BVPs) in Ordinary Differential Equations (ODEs). The Neural networks use the principle of Back propagation. Five examples are considered to show effectiveness of using the shooting techniques and neural network for solving the BVPs in ODEs. The convergence properties of the technique, which depend on the convergence of the integration technique and accuracy of the interpolation technique are considered

2,2,2-Trifluoro-N-(isoquinolin-5-ylmeth­yl)acetamide

The mol­ecular structure of the title compound at 123 K, C12H9F3N2O, presents a rotationally disordered CF3 group. Hydrogen bonds between the amide NH group and the N atom of the isoquinoline form a chain in the b-axis direction. The packed structure forms alternate layers of isoquinoline and amide groups parallel to the ab plane

DNA minor groove binders-inspired by nature

The synthesis and biological activity of a variety of analogues to the naturally occurring anti-bacterial and anti-fungal Distamycin A were explored by a number of authors. These compounds were subject to a large array of assays. Some of these compounds showed high activity against a range of Gram-positive, Gram-negative bacteria as well as fungi. To explore the anti-parasitic activity of this class of compounds, specific modifications had to be made. A number of these compounds proved to be active against Trypanosoma brucei. The binding of a number of these compounds to short sequences of DNA were also examined using footprinting assays as well as NMR spectroscopy. Computer modelling was employed on selected compounds to understand the way these compounds bind to specific DNA sequences. A large number of variations were made to the standard structure of Distamycin. These changes involved the replacement of the pyrrole moieties as well as the head and tail groups with a number of heterocyclic compounds. Some of these MGBs were also investigated for their capability for the treatment of cancer and in particular lung cancer

Analysing an Imbalanced Stroke Prediction Dataset Using Machine Learning Techniques

A stroke is a medical condition characterized by the rupture of blood vessels within the brain which can lead to brain damage. Various symptoms may be exhibited when the brain's supply of blood and essential nutrients is disrupted. To forecast the possibility of brain stroke occurring at an early stage using Machine Learning (ML) and Deep Learning (DL) is the main objective of this study. Timely detection of the various warning signs of a stroke can significantly reduce its severity. This paper performed a comprehensive analysis of features to enhance stroke prediction effectiveness. A reliable dataset for stroke prediction is taken from the Kaggle website to gauge the effectiveness of the proposed algorithm. The dataset has a class imbalance problem which means the total number of negative samples is higher than the total number of positive samples. The results are reported based on a balanced dataset created using oversampling techniques. The proposed work used Smote and Adasyn to handle imbalanced problem for better evaluation metrics. Additionally, the hybrid Neural Network and Random Forest (NN-RF) utilizing the balanced dataset by Adasyn oversampling achieves the highest F1-score of 75% compared to the original unbalanced dataset and other benchmarking algorithms. The proposed algorithm with balanced data utilizing hybrid NN-RF achieves an accuracy of 84%. Advanced ML techniques coupled with thorough data analysis enhance stroke prediction. This study underscores the significance of data-driven methodologies, resulting in improved accuracy and comprehension of stroke risk factors. Applying these methodologies to medical fields can enhance patient care and public health outcomes. By integrating our discoveries, we can enhance the efficiency and effectiveness of the public health system

Effect of zero tillage and different weeding methods on grain yield of durum wheat in semi-arid regions

Received: September 28th, 2020 ; Accepted: December 1st, 2020 ; Published: December 10th, 2020 ; Correspondence: [email protected] high grain yield of wheat is limited by the dominance of weeds, particularly wild oat. Therefore, to improve wheat yield under these conditions, a field experiment was carried out in Maru Agricultural Research Station, Jordan during 2015–2016 and 2016–2017 to investigate yield response of two wheat varieties (Triticum durum L.) to different tillage and weeding treatments. The experimental design used was a split-split arrangement in a randomized complete block design with three replicates. Two-tillage treatments (conventional vs. zero tillage) were applied to the main plot, two wheat varieties to sub-plot, and five weeding methods (hand weeding, broadleaf + narrow leaf herbicide, broadleaf herbicide, narrow leaf herbicide, and controls) as a sub-sub-plot. The variety ‘Umqais’ had higher plant height, biological, grain, and straw yield than the variety ‘Sham’. Hand weeding slightly increased grain yield compared with mixed herbicides (the 2,4-D plus Antelope Clodinatop- propagyl). Furthermore, mixed herbicides presented a higher grain yield than using either single herbicide. The interaction between tillage systems and weeding methods was significant in both years. The highest (P < 0.05) straw yield (5,990 kg ha-1 ) was obtained by hand weeding under conventional tillage in the first season while the highest grain yield (2,005 kg ha-1 ) was obtained by hand weeding under zero tillage in the second season. Under all weed control treatments, the variety ‘Umqais’ had higher biological, grain, and straw yields than the variety ‘Sham’ in the second season indicating that variety ‘Umqais’ performed better under dry conditions. Our results confirmed the superior of zero tillage for increasing the grain yield of the variety ‘Umqais’, and for increasing the biological and straw yields of the variety ‘Sham’ under semi-arid rainfed conditions of Jordan

Gallbladder cancer: 7-Year experience from Qatar

Thirty-five patients presented with GC during the study period, 10 females (28.6%) and 25 males (71.4%). Fourteen patients (40%) were diagnosed incidentally after laparoscopic cholecystectomy, 16 (48.6%) were diagnosed pathologically, and 4 (11.4%) were diagnosed radiologically. The median age at diagnosis was 54 years (31–78). 74.3% of the disease occurred in patients less than 60 years old. Metastatic disease was discovered in 25 patients (71.4%) versus no metastasis in 10 patients (28.6%). The most common sites for metastasis were the liver (42.9%), peritoneum (25.7%), and lymph nodes (25.7%). Curative central hepatic resection was done in 8 patients (22.9%). Pathology showed adenocarcinoma in 27 patients (77.1%), neuroendocrine tumor in 3 patients (8.6%) and high-grade dysplasia in 1 patient (2.9%). No histopathology was available for 4 patients (11.4%). Twenty-eight patients (80.0%) had regular follow up, with 22 (62.9%) still alive. Six patients (17.1%) died during follow up with survival after diagnosis ranging from 42 days to 6.8 years

Crystal structure of N,N-dimethyl-2-[(4-methylbenzyl)sulfonyl]ethanamine

In the crystal, the title compound, C12H19NO2S, has a disordered structure with two equally populated conformations of the amine fragment. A pair of weak C—HO intermolecular interactions between the CH2 and SO2 groups gives a one-dimensional supramolecular structure that propagates through translation along the a-axis direction