SYNTHESIS AND ANTICONVULSANT ACTIVITIES OF SMALL N-SUBSTITUTED 2, 5-DIMETHYL PYRROLE AND BIPYRROLE

A series of N-substituted 2, 5-dimethyl pyrrole and bipyrrole derivatives were synthesized by Paal-Knorr method and evaluated for anticonvulsant activity at NIH. Anticonvulsant activity was determined after intraperitoneal (i.p.) administration to mice by maximal electroshock (MES) and subcutaneous metrazol (ScMET) induced seizure method at 30, 100 and 30 mg/kg dose levels. Minimal motor impairment was determined by rotorod test at the same dose levels. Compound 7 and 10 showed trace signs of anticonvulsant protection in the primary model screens, therefore selected for reevaluation screening in the 6 Hz model. Compound 10 was found to possess anticonvulsant activity at 100 mg/kg dose level in 6 Hz test

Serotonin-Norepinephrine Reuptake Inhibitors for Pain Control: Premise and Promise

The precise mechanisms of pain perception and transmission in the central nervous system have not been fully elucidated. However, extensive data support a role for the monoamine neurotransmitters, serotonin and norepinephrine, in the modulation of pain. Experiments with animal models of pain indicate that noradrenergic interventions, and to a lesser extent serotonergic interventions, reduce pain-related behavior. This is supported by data from clinical trials in humans in which antidepressants have been shown to reduce pain and functional impairment in central and neuropathic pain conditions. These effects are particularly well-studied in trials with serotonin-norepinephrine reuptake inhibitors (SNRIs), which have provided a useful tool in the clinician’s arsenal, particularly considering the limitations of other classes of pain medications such as opioids, anti-inflammatories, and anticonvulsants (i.e., limited efficacy, safety and tolerability issues). Moreover, painful physical symptoms are frequently comorbid with major psychiatric disorders such as major depressive disorder and anxiety disorders. This paper reviewed and summarized the rationale and potential role of SNRIs for the control of pain including clinical and preclinical background. Currently evidence does not definitely support a role of the SNRIs, while limited data propose a putative promise of SNRIs in the treatment of pain related disorders including fibromyalgia and depressed patients with multiple somatic complaints. More researches are warranted to generalize currently available preliminary evidences

Multifractal behavior of linear polymers in disordered media

The scaling behavior of linear polymers in disordered media modelled by self-avoiding random walks (SAWs) on the backbone of two- and three-dimensional percolation clusters at their critical concentrations p_c is studied. All possible SAW configurations of N steps on a single backbone configuration are enumerated exactly. We find that the moments of order q of the total number of SAWs obtained by averaging over many backbone configurations display multifractal behavior, i.e. different moments are dominated by different subsets of the backbone. This leads to generalized coordination numbers \mu_q and enhancement exponents \gamma_q, which depend on q. Our numerical results suggest that the relation \mu_1 = p_ c \mu between the first moment \mu_1 and its regular lattice counterpart \mu is valid.Comment: 11 pages, 12 postscript figures, to be published in Phys. Rev.

STUDIES OF ULTRASONIC AND VISCOMETRIC BEHAVIOR OF AZITHROMYCIN WITH DIFFERENT SOLVENT SYSTEMS DIOXANE-WATER AND METHANOL-WATER MIXTURE AT 305.15 K

ABSTRACT Antibiotic drug Azithromycin is mainly used for treatments of infectious disease caused by bacteria such as respiratory,skin,ear and sexually transmitted diseases such great importance of azithromycine in human life the densities, ultrasonic velocities and viscosities of azithromycine have been evaluated in different concentrations in 70% dioxane-water and 70% methanol-water mixtures at 305.15 K. Experimental data of sound velocities and densities of solutions in 70% dioxane-water helps to determine the various acoustical parameters such as adiabatic compressibility, apparent molal volumes, intermolecular free length, specific acoustic impedance, relative association etc. for evaluating the molecular interactions present in different solutions were studied. Keywords: Azithromycin drug, dioxane water and viscometric measurements. INTRODUCTION In the fields of medicinal, industrial, biochemistry etc the study of molecular interactions between solutes molecule and solvent media has got great importance. It also helps the study of solute solvent and solventsolvent interactions can by the measurement of relative viscosity and ultrasonic velocity of an electrolyte in solutions EXPERIMENTAL SECTION The chemicals used were of AR grade and were purified by standard methods. Requisite amount of chemicals weighing was done by using electronic balance.By using the Pyknometers the densities of solutions were determined, which was standardized by the standard procedure. Ostwald's Viscometer was used for measurements of viscosity which was kept in elite thermostatic water bath (±0.1°C). The ultrasonic velocity of solution and solvent was determined by using single crystal interferometer (Mittal Enterprises, Model F-81) with accuracy of ± 0.03% and 2 MHz frequency. RESULTS AND DISCUSSION Acoustic parameters, densities and relative viscosities have been determined for all the solutions and were calculated by using different equations 14 and are presented in the followin

Machine Learning in Automated Text Categorization

The automated categorization (or classification) of texts into predefined categories has witnessed a booming interest in the last ten years, due to the increased availability of documents in digital form and the ensuing need to organize them. In the research community the dominant approach to this problem is based on machine learning techniques: a general inductive process automatically builds a classifier by learning, from a set of preclassified documents, the characteristics of the categories. The advantages of this approach over the knowledge engineering approach (consisting in the manual definition of a classifier by domain experts) are a very good effectiveness, considerable savings in terms of expert manpower, and straightforward portability to different domains. This survey discusses the main approaches to text categorization that fall within the machine learning paradigm. We will discuss in detail issues pertaining to three different problems, namely document representation, classifier construction, and classifier evaluation.Comment: Accepted for publication on ACM Computing Survey

Endometrial receptivity and implantation require uterine BMP signaling through an ACVR2A-SMAD1/SMAD5 axis.

During early pregnancy in the mouse, nidatory estrogen (E2) stimulates endometrial receptivity by activating a network of signaling pathways that is not yet fully characterized. Here, we report that bone morphogenetic proteins (BMPs) control endometrial receptivity via a conserved activin receptor type 2 A (ACVR2A) and SMAD1/5 signaling pathway. Mice were generated to contain single or double conditional deletion of SMAD1/5 and ACVR2A/ACVR2B receptors using progesterone receptor (PR)-cre. Female mice with SMAD1/5 deletion display endometrial defects that result in the development of cystic endometrial glands, a hyperproliferative endometrial epithelium during the window of implantation, and impaired apicobasal transformation that prevents embryo implantation and leads to infertility. Analysis of Acvr2a-PRcre and Acvr2b-PRcre pregnant mice determined that BMP signaling occurs via ACVR2A and that ACVR2B is dispensable during embryo implantation. Therefore, BMPs signal through a conserved endometrial ACVR2A/SMAD1/5 pathway that promotes endometrial receptivity during embryo implantation