3-Aryl-1-phenyl-1H-pyrazole derivatives as new multitarget directed ligands for the treatment of Alzheimer's disease, with acetylcholinesterase and monoamine oxidase inhibitory properties

A series of 3-aryl-1-phenyl-1H-pyrazole derivatives was synthesized in good yield and assayed in vitro as inhibitors of the mice acetylcholinesterase (AChE) and two goat liver monoamine oxidase (MAO) isoforms, MAO-A and MAO-B. Most of the compounds demonstrated a good AChE and selective MAO-B inhibitory activities in the nanomolar or low micromolar range. N-((3-(4-chlorophenyl)-1-phenyl-1H-pyrazole-4-yl) methylene) benzenamine (3e, pIC50 = 4.2) and N-((4-fluorophenyl)-1-phenyl-1H-pyrazole-4-yl) methylene) methanamine (3f, pIC50 = 3.47) were the most potent AChE and highly selective MAO-B inhibitors respectively. Structure activity relationships showed that chloro derivatives were more effective AChE inhibitors as compared to fluoro derivatives while reverse trend was observed in MAO-B inhibitory activity. With the aid of modeling studies, potential binding orientations as well as interactions of the compounds in the AChE and MAO-B active sites were examined

Synthesis and antimalarial potential of some novel quinoline-pyrazolopyridine derivatives

oai:eldorado.tu-dortmund.de:2003/35825A series of 1-(4-methylquinolin-2-yl)-4,6-diaryl-1H-pyrazolo[3,4-b]pyridin-3-amine derivatives was synthesized by the reaction of 3-cinnamoyl-4-hydroxy-6-methyl-2H-pyran-2-ones with 2-chloro-4,6-diphenylnicotinonitrile analogues in the presence of 2-hydrazino-4-methyl quinoline and ethanol. The newly synthesized compounds were characterized by IR, 1H NMR and mass spectral data. The synthetic series of novel quinolinepyrazolopyridine hybrids were screened for in vitro schizont maturation assay against chloroquine sensitive 3D7 strain of Plasmodium falciparum, from which the most five active analogues were further evaluated for in vivo 4-day suppressive test in Swiss albino mice. Among the series, 5p (containing 4-Cl substituent attached to both aryl ring) portrayed considerable potent antimalarial activity during in vitro as well as in vivo stud

Model Predictive Control System Analysis for Sugarcane Crushing Mill Process

MPC is a computer based technique that requires the process model to anticipate the future outputs of that process. An optimal control action is taken by MPC based on this prediction. The MPC is so popular since its control performance has been reported to be best among other conventional techniques to control the multivariable dynamical plants with various inputs and outputs constraints. In this paper the performance of an MPC controller on a single stage of milling train of sugar mill is analyzed. A linear model of the plant is taken with flap position and turbine speed set point as manipulated variables and mill torque and buffer chute height as controlled variables. The set point tracking responses are compared for constrained and unconstrained cases. The effect of presence of unmeasured disturbance also is investigated

Model Predictive Control System Design for Boiler Turbine Process

MPC is a computer based technique that requires the process model to anticipate the future outputs of that process. An optimal control action is taken by MPC based on this prediction. The MPC is so popular since its control performance has been reported to be best among other conventional techniques to control the multivariable dynamical plants with various inputs and outputs constraints. In the present work the control of boiler turbine process with three manipulated variables namely fuel flow valve position, steam control valve position and feed water flow valve position and three controlled variables namely drum pressure, output power and drum water level deviation [8] has been attempted using MPC technique. Boiler turbine process is very complex and nonlinear multivariable process. A linearized model obtained using Taylor series expansion around operating point has been used

Customized ocular prosthesis: A case report

The eye is a vital organ and an important component of facial expression. Loss of an eye has a crippling effect on the psychology of the patient. Enucleation of the eye is therefore normally followed by fabrication of an ocular prosthesis to improve esthetics. This article describes a technique of rehabilitation of a patient with missing the left eye with custom-made ocular prosthesis

PERFORMANCE SIMULATION AND BER COMPARISION OFDM-MIMO SYSTEMS IN AWGN AND RAYLEIGH FADING CHANNELS WITH BPSK MODULATION SCHEMES

Behavior of communication medium play vital role in the growth of wireless communication system. To understand various wireless channel environments such as additive white Gaussian noise (AWGN) and Rayleigh fading channels in orthogonal frequency division multiplexing (OFDM) along with multiple input and multiple output (MIMO) system, we analyze mathematical relation of bit error rate (BER) against Signal to Noise ratio (SNR) and verified the same using MATLAB simulation, while considering the BPSK modulation scheme. The performance measured in terms of BER is evaluated for various channels of OFDM-MIMO system along with variation in number of antennas at transmitter and receiver side. It has been demonstrated that the BER and probability of detection improves against SNR per bit, as the diversity employs at transmitter or/and receiver end

A NOVEL APPROACH FOR VERIFIABLE SECRET SHARING IN PROACTIVE NETWORK USING RSA

We consider perfect verifiable secret sharing (VSS) in a synchronous network of n processors (players) where a designated player called the dealer wishes to distribute a secret s among the players in a way that none of them obtain any information, but any t + 1 players obtain full information about the secret. The round complexity of a VSS protocol is defined as the number of rounds performed in the sharing phase. Gennaro, Ishai, Kushilevitz and Rabin showed that three rounds are necessary and sufficient when n > 3t. Sufficiency, however, was only demonstrated by means of an inefficient (i.e., exponential-time) protocol and the construction of inefficient three-round protocol were left as an open problem. In this paper, we present an efficient three-round protocol for VSS. The solution is based on a three-round solution of so-called weak verifiable secret sharing (WSS), for which we also prove that three rounds are a lower bound. Furthermore, we also demonstrate that one round is sufficient for WSS when n > 4t, and that VSS can be achieved in 1 + " amortized rounds (for any " > 0) when n > 3t

Engineering Properties of Laterite Stone Scrap Blocks

A study was conducted to determine the engineering properties viz. compressive strength, toughness index and water absorption capacity of the laterite stone scrap blocks. Paddy husk ash, saw dust and processed fly ash were used as other constituents and added to the laterite stone scrap in the range of 3 to 9%, 3 to 9%, 20 to 30% respectively. The cement was used as binding material and added in the range of 8 to 16%. The maximum compressive strength 13.6 N/mm2 was observed for the block having 68% laterite stone scrap, 8% cement and 20% processed fly ash. The maximum toughness index of 14.3 was observed for the block having 81% laterite stone scrap, 16% cement and 3% paddy husk ash. The minimum water absorption capacity of 18.6 was observed for the block having 84% laterite stone scrap and 16% cement. The lowest cost of laterite stone scrap block was found to be Rs. 22.94 for the block having 85% laterite stone scrap, 12% cement and 3% paddy husk ash which satisfies BIS standards