No abstract

Benzothiazole, a fused heterocyclic moiety, has attracted synthetic and medicinal chemists for good reasons. It is a valuable scaffold that possesses diverse biological activities, such as anticancer, anti-inflammatory, antimicrobial, antiviral, antimalarial, and anticonvulsant effects. This review mainly focusses on the recent research work on the different biological activities of benzothiazole-based compounds.

ObjectiveAccurate localization of a seizure onset zone (SOZ) from independent components (IC) of resting-state functional magnetic resonance imaging (rs-fMRI) improves surgical outcomes in children with drug-resistant epilepsy (DRE). Automated IC sorting has limited success in identifying SOZ localizing ICs in adult normal rs-fMRI or uncategorized epilepsy. Children face unique challenges due to the developing brain and its associated surgical risks. This study proposes a novel SOZ localization algorithm (EPIK) for children with DRE.MethodsEPIK is developed in a phased approach, where fMRI noise-related biomarkers are used through high-fidelity image processing techniques to eliminate noise ICs. Then, the SOZ markers are used through a maximum likelihood-based classifier to determine SOZ localizing ICs. The performance of EPIK was evaluated on a unique pediatric DRE dataset (n = 52). A total of 24 children underwent surgical resection or ablation of an rs-fMRI identified SOZ, concurrently evaluated with an EEG and anatomical MRI. Two state-of-art techniques were used for comparison: (a) least squares support-vector machine and (b) convolutional neural networks. The performance was benchmarked against expert IC sorting and Engel outcomes for surgical SOZ resection or ablation. The analysis was stratified across age and sex.ResultsEPIK outperformed state-of-art techniques for SOZ localizing IC identification with a mean accuracy of 84.7% (4% higher), a precision of 74.1% (22% higher), a specificity of 81.9% (3.2% higher), and a sensitivity of 88.6% (16.5% higher). EPIK showed consistent performance across age and sex with the best performance in those < 5 years of age. It helped achieve a ~5-fold reduction in the number of ICs to be potentially analyzed during pre-surgical screening.SignificanceAutomated SOZ localization from rs-fMRI, validated against surgical outcomes, indicates the potential for clinical feasibility. It eliminates the need for expert sorting, outperforms prior automated methods, and is consistent across age and sex.

Cancer is one of the severe diseases in which abnormal cells divide and proliferate in an uncontrolled manner without any regulation. Globally cancer is among the leading causes of death; according to a recent report of by the WHO, around 10 million people died in 2018 due to cancer. It has also been reported that by 2040, approximately 30 million new cases will be reported every year. The increase in the incidences of cancer is taking a toll on the health care system worldwide. Considerable scientific literature is available on anticancer agents but newer therapeutic strategies are still required in this field to address novel approaches to drug design and discovery to counter this problem. Imidazothiazole represents a privileged scaffold in medicinal chemistry and provides the medicinal chemist the possibility to modulate the physiochemical properties of the lead compound. In recent times, imidazothiazole scaffold is broadly explored for its anticancer activity, which acts through various mechanisms such as EGFR, B-RAF, DHFR kinase inhibition and tubulin polymerization inhibition and other molecular mechanisms of action. Due to their feasible synthetic accessibility and promising pharmacological profile, it has attracted various medicinal chemists to explore and develop imidazothiazole derivatives as potent and safe anticancer agents. In the present article, we have reviewed various potent imidazothiazole scaffold-based derivatives reported as anticancer agents, their synthetic strategies, Structure Activity Relationship (SAR), mechanism of action, and molecular docking along with their future perspective. This review will be very useful for medicinal chemists for drug design and development of imidazothiazole-based potent antiproliferative agents.

Gestures that share similarities in their forms and are related in their meanings, should be easier for learners to recognize and incorporate into their existing lexicon. In that regard, to be more readily accepted as standard by the Deaf and Hard of Hearing community, technical gestures in American Sign Language (ASL) will optimally share similar in forms with their lexical neighbors. We utilize a lexical database of ASL, ASL-LEX, to identify lexical relations within a set of technical gestures. We use automated identification for 3 unique sub-lexical properties in ASL-location, handshape and movement. 𝐸𝑑𝐺𝐶𝑜𝑛 assigned an iconicity rating based on the lexical property similarities of the new gesture with an existing set of technical gestures and the relatedness of the meaning of the new technical word to that of the existing set of technical words. We collected 30 ad hoc crowdsourced technical gestures from different internet websites and tested them against 31 gestures from the DeafTEC technical corpus. We found that 𝐸𝑑𝐺𝐶𝑜𝑛 was able to correctly auto-assign the iconicity ratings 80.76% of the time. 1