Mini Reviews in Medicinal Chemistry - Volume 10, Issue 8, 2010

Fullerenes, the third carbon allotrope, have emerged as agents which could revolutionize the treatment of many diseases. Fullerenes possess different biological applications like neuroprotective agents, antioxidants, anti-HIV activity, enzyme inhibition, antiapoptotic activity and the list is ever increasing. Moreover, they are being utilized as drug carrier systems and also for many non-biological applications like supercondu Read More

Phthalimide analogues have been extensively used in medicinal chemistry owing to their wide range of applications as anti-convulsant, anti-inflammatory, analgesic, hypolipidimic and immunomodulatory activities. Number of anti-inflammatory phthalimide analogues have been synthesized as tumor necrosis factor-α (TNF-α) inhibitors. TNF-α plays a critical role in certain physiological immune systems and its over Read More

Quantitative structure-activity relationships (QSAR) analyses have been attempted on a new set of 4- oxothiazolidines and 5-arylidines derivatives using linear free energy related (LFER) model of Hansch to explain the structural requirements for lipoxygenase inhibition. The QSAR study showed that successful correlation can be achieved for inhibitory activity of 4-oxothiazolidines and 5-arylidines (R>0.9, Q2>0.7). The result of th Read More

Cyclodextrins are pharmaceutical excipients used to enhance the solubility, stability, safety and bioavailability of drugs. Recent findings have shown them to display adjuvant activity in vaccine therapy and prophylactic and therapeutic activity in the treatment of several host-pathogen infections. This article focuses on their activity and mechanism of action.

Guanine-rich DNA sequences can form planar four-stranded structures via Hoogsteen hydrogen bonds. These sequences in telomeric DNA and some oncogenes have been identified as targets for novel anticancer drugs. Consequently, there is great current interest in developing small molecules that can facilitate the formation of, and stabilize G-quadruplexes as potent antitumor chemotherapeutic agents. Metal compl Read More

In this review we have focused on the utilization of the biocompatible nanomaterials to reverse multidrug resistance (MDR), a major clinical obstacle in cancer therapeutics. Based on the comprehension of the mechanism of MDR and common reversal methods, the strategies and key properties of anti-MDR nanomaterials are explored and described to show how these features could provide the potential therapeutic ef Read More

The development of an adequate immune response against pathogens is mediated by molecular interactions between different cell types. Among them, binding of antigenic peptides to the Major Histocompatibility Complex (MHC) molecule expressed on the membrane of antigen presenting cells (APCs), and their subsequent recognition by the T cell receptor have been demonstrated to be crucial for developing an adequate i Read More

Saxagliptin (BMS-477118), a recently FDA approved drug for the management of T2DM, has been developed by Bristol-Myers Squibb and AstraZeneca under the trade name Onglyza™. Saxagliptin is a nitrile-containing selective, potent, reversible and durable DPP IV inhibitor developed as an alternative second-line to Metformin in place of a sulphonylurea. Saxagliptin increases and prolongs the action of incretin hormon Read More

Despite the beneficial effect of the HAART, adverse reactions and drug interaction have been observed. Abnormalities in lipid and glucose metabolism make HIV-positive patients to high risk for the development of coronary heart disease and diabetes, respectively. Besides adverse reactions, drug interaction with other medication can also be observed. In fact, drug interaction may interfere in the periodontal therap Read More