Nitroarenes as Antitubercular Agents: Stereoelectronic Modulation to Mitigate Mutagenicity

Nitroarenes are less preferred in drug discovery due to their potential to be mutagenic. However, several nitroarenes were shown to be promising antitubercular agents with specific modes of action, namely, nitroimidazoles and benzothiazinones. The nitro group in these compounds is activated through different mechanisms, both enzymatic and non‐enzymatic, in mycobacteria prior to binding to the target of interest. From a whole‐cell screening program, we identified a novel lead nitrobenzothiazole (BT) series that acts by inhibition of decaprenylphosphoryl‐β‐d ‐ribose 2′‐epimerase (DprE1) of Mycobacterium tuberculosis (Mtb). The lead was found to be mutagenic to start with. Our efforts to mitigate mutagenicity resulted in the identification of 6‐methyl‐7‐nitro‐5‐(trifluoromethyl)‐1,3‐benzothiazoles (cBTs), a novel class of antitubercular agents that are non‐mutagenic and exhibit an improved safety profile. The methyl group ortho to the nitro group decreases the electron affinity of the series, and is hence responsible for the non‐mutagenic nature of these compounds. Additionally, the co‐crystal structure of cBT in complex with Mtb DprE1 established the mode of binding. This investigation led to a new non‐mutagenic antitubercular agent and demonstrates that the mutagenic nature of nitroarenes can be solved by modulation of stereoelectronic properties.     

Optimized Path and Reduced Rule Caching Cost for Software Defined Network (SDN) Based Internet of Things (IOT)

Wireless Personal Communications - 2In Software Defined Network based Internet of Things (SDN-IoT), the path selected for forwarding the packets as per rules, should be Quality of Service (QoS)...     

River mapping from a flying robot: state estimation, river detection, and obstacle mapping

Accurately mapping the course and vegetation along a river is challenging, since overhanging trees block GPS at ground level and occlude the shore line when viewed from higher altitudes. We present a multimodal perception system for the active exploration and mapping of a river from a small rotorcraft. We describe three key components that use computer vision, laser scanning, inertial sensing and intermittant GPS to estimate the motion of the rotorcraft, detect the river without a prior map, and create a 3D map of the riverine environment. Our hardware and software approach is cognizant of the need to perform multi-kilometer missions below tree level with size, weight and power constraints. We present experimental results along a 2?km loop of river using a surrogate perception payload. Overall we can build an accurate 3D obstacle map and a 2D map of the river course and width from light onboard sensing.     

Efficient multiple moving object detection and tracking using combined background subtraction and clustering

Object detection and tracking is a fundamental, challenging task in computer vision because of the difficulties in tracking. Continuous deformation of objects during movement and background clutter leads to poor tracking. In this paper, a method of multiple moving object detection and tracking by combining background subtraction and K-means clustering is proposed. The proposed method can handle objects occlusion, shadows and camera jitter. Background subtraction filters irrelevant information, and K-means clustering is employed to select the moving object from the remaining information, and it is capable of handling merging and splitting of moving objects using spatial information. Experimental results show that the proposed method is robust when compared to other techniques.