Pyridazinone hybrids: Design, synthesis and evaluation as potential anticonvulsant agents.

A series of new hybrid benzothiazole containing pyridazinones derivatives were designed and synthesized fulfilling all the pharmacophoric requirements essential for the anticonvulsant activity. In-silico and in vitro studies revealed that some of these hybrid derivatives demonstrated admirable GABA AT inhibitory activity. An attempt has also been made to validate the results of in vitro GABA AT inhibition of the most potent compound SPS-5F (IC 9.

N-terminally modified linear and branched spermine backbone dipeptidomimetics against planktonic and sessile methicillin-resistant Staphylococcus aureus.

Toward the discovery of useful therapeutic molecules, we report the design and synthesis of a focused library of new ultrashort N-terminally modified dipeptidomimetics, with or without modifications in the spermine backbone leading to linear (series 1) or branched (series 2) tryptophans, as antimicrobial agents. Eight peptidomimetics in the library showed good antibacterial activity (MICs of 1.77 to 14.

Pharmacological significance of triazole scaffold.

The triazole nucleus is one of the most important and well known heterocycles which is a common and integral feature of a variety of natural products and medicinal agents. Triazole nucleus is present as a core structural component in an array of drug categories such as antimicrobial, anti-inflammatory, analgesic, antiepileptic, antiviral, antineoplastic, antihypertensive, antimalarial, local anaesthetic, antianxiety, antidepressant, antihistaminic, antioxidant, antitubercular, anti-Parkinson's, antidiabetic, antiobesity and immunomodulatory agents, etc. The broad and potent activity of triazole and their derivatives has established them as pharmacologically significant scaffolds.

2(3H)-furanones and 2(3H)-pyrrolones: synthesis and antimycobacterial evaluation.

A series of 3-arylidene-5-(substituted phenyl)-2(3H)-furanones (3-10) and their nitrogen analogues, 3-arylidene-5-(substituted phenyl)-1-benzyl-2(3H)-pyrrolone (11-14), and 3-arylidene-5-(substituted phenyl)-2(3H)-pyrrolones (15-21) were synthesized. All the compounds were screened for their antimycobacterial activity in vitro against Mycobacterium tuberculosis H37Rv (ATCC 27294) in BACTEC medium using the Microplate Alamar Blue Assay (MABA). Among the synthesized compounds, compound 19, 3-(4-chlorobenzylidene)-5-(4-methylphenyl)-2(3H)-pyrrolone, emerged as a lead compound having the highest activity against Mycobacterium tuberculosis.

[Inequalities in health expectancies in England and Wales--small area analysis from the 2001 Ccensus.

This study investigates inequalities in the expectation of life without disability and life in good health using 2001 Census data at small area (ward) level for England and Wales. Inequalities were examined both nationally and within regions by computing life expectancies and health expectancies in groups of wards (twentieths) aggregated according to the Carstairs deprivation score. The results showed that the inequality gaps were significantly larger for health expectancies compared with life expectancy; they were wider for disability-free life expectancy than healthy life expectancy; and, for all measures, were wider for males.

Socio-demographic characteristics of the healthcare workforce in England and Wales-- results from the 2001 Census.

Based on Census 2001 data, this article presents analysis of the socio-demographic characteristics of people working in the healthcare sector, focusing particularly on four key healthcare occupations: doctors, dentists, nurses and midwives. Unlike the NHS workforce statistics, which only include people directly employed by the NHS, census data also include those working in the private healthcare market and those who are self-employed. The article als examines patterns of distribution key healthcare professions per head of population by local authority and by area deprivation.