Current Bioactive Compounds - Volume 2, Issue 1, 2006

Conventional drug development, which likely to be remain a dominant strategy in the near future, is based on the discovery of potent molecular entities. Scientific literature is full of the reports of discovery or development of interesting molecular exciting against different therapeutic targets. However, only a handful of these exciting discoveries are seriously followed mainly due to lack of access to most readily available and updated literature reports. The quarterly journal Current Bioactive Compounds is an attempt to fill this gap. We are glad that this journal has already received attention of the fraternity scientists working in the field of drug development and discovery. This issue of Current Bioactive Compounds contains brief descriptions and chemical structures of lead discoveries, taken from the most authentic literature sources, and divided into thirteen therapeutic categories. This will hopefully enable readers to quickly spot the potential leads for further exploration. Keeping in view of the importance of in-depth analysis of various classes of bioactive compounds against various diseases, we have decided to include selected review articles in CBC starting from this issue. The articles are contributed by leading researchers in the field and focuses on various classes of bioactive chemical compounds along with their mechanisms of action and structure-activity relationships. I hope this innovation in the format and scope of the Current Bioactive Compounds will be welcomed by the readers and will further enhance this impact of the publication. At the end we acknowledge the editorial and secretarial staff of the Bentham Science Publishers, for their help in bringing this issue timely and neatly. Notable among them are the team leader Mr. Mahmood Alam, and staff members, Dr. Ghulam Murtaza Maharvi and Miss Samreen Laeeq.

Several families of novel synthetic ion channels have now been developed. They exhibit many, but not all, of the properties of protein ion channels. Some are peptides, but none is naturally occurring. Their ability to insert in membranes and disrupt ion homeostasis confers cellular toxicity upon them. Because these compounds are both abiotic and cytotoxic to a range of microbes, they have been investigated as antibiotics.

In this review we critically examine PI (Padmakar-Ivan) index of organic compounds acting as drugs and discussed its applications in Computer-Aided designing of bioactive compounds with special reference to designing of carbonic anhydrase inhibitors, lipophilicity, toxicity, tadpole narcosis, bio-concentration factor, diuretic activity and carcinogenic activity of aromatic hydrocarbons and heterocycles etc.

Eugenol (4-allyl-2-methoxyphenol) is a fragrant compound that is commonly contained in various sorts of plants, especially in spices and medicinal herbs. Eugenol has been used for dental analgesic, which also has anticonvulsive and anti-microbial activities. Besides, anti-inflammatory and antioxidative activities of eugenol are known. A body of evidence suggests that eugenol can be used as a drug for treatment of Alzheimer's disease (AD). According to recent reports, the extract of a medicinal plant Rhizoma Acori Graminei (RAG) alleviates neurotoxicity induced by amyloid beta peptides (Aβ) in vitro and the active constituent of RAG is eugenol. Eugenol inhibits Aβ-induced excessive influx of calcium ion into neurons that causes neuronal death. Moreover, eugenol possesses an antidepressant-like activity. Eugenol, like other antidepressants, increases expression of brain-derived neurotrophic factor (BDNF) gene in the hippocampus, which is necessary for an antidepressant to exhibit its activity. Furthermore, eugenol inhibits monoamine oxidase A (MAO-A) and may restore monoamines that are decreased in the brain of patients with depression. Thus, eugenol can be a good medicine for AD and depression. Here we suggest that eugenol and its analogs can be used also for other diseases of the central nervous system (CNS) including Parkinson's disease (PD). This article reviews the previous investigations concerning effects of eugenol including its analogs on the CNS and describes perspectives of this highly potential compound.

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