Suppression of pain and inflammation still continues to be a challenge despite the availability of a number of non-steroidal anti-inflammatory drugs (NSAIDs). This is because NSAIDs do not only exhibit a different spectrum of analgesic, anti-pyretic and anti-inflammatory effects but also cause gastrointestinal (GI) complications ranging from dyspepsia to fatal upper GI tract bleeding and perforation (1). Efforts to improve the adverse effect profile of the current NSAIDs have been focused on developing prodrugs (2) or modifications of marketed formulations (3). These approaches have been only partially successful. A recent approach is development of selective cyclooxygenase (COX)-2 inhibitors (4-6). COX is the key enzyme that catalyzes the conversion of arachidonic acid to prostaglandins and thromboxans. There are two types of cyclooxygenase enzymes, COX-1 and COX-2. Currently available NSAIDs inhibit both COX-1 and COX-2 enzymes. Inhibition of COX-1 reduces basal production of cytoprotective prostaglandins (PGs) PGE2 and PGI2 and hence causes ulceration while inhibition of COX-2 inhibits inflammation. Complete inhibition of COX-1 is therefore not preferred and drugs that inhibit the COX-2 enzyme are better anti-inflammatory agents (7,8).Owing to the continuous efforts in exploring the structural insights to aid the design (9, 10) and synthesis of safer novel anti-inflammatory agents, 2-amino-5-sulfanyl--1,3,4-thiadiazole was identified as the central nucleus. To date, 2-amino-5-sulfanyl--1,3,4-thiadiazole derivatives have not been reported to exhibit anti-inflammatory and A new series of cyclooxygenase-2 inhibitors with 2-amino--5-sulfanyl-1,3,4-thiadiazole as the central scaffold unit has been synthesized. The newly synthesized compounds were characterized by analytical and spectral methods. Compounds were screened for cyclooxygenase inhibitory activity by the colorimetric COX (ovine) inhibitor screening assay, anti-inflammatory activity by the carrageenean induced rat paw oedema test and analgesic activity by the tail flick method. Some compounds exhibited significant biological activity.

A new series of 2-amino-5-sulfanyl-1,3,4-thiadiazole derivatives has been synthesized. The newly synthesized compounds were characterized by analytical and spectral methods. Compounds were screened for central nervous system activity. Compounds 1, 5, 7, 10, 14 exhibited significant antidepressant, anxiolytic and anticonvulsant activity in comparison to the reference drugs.

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Skin aging is a complex biological process influenced by a combination of endogenous (intrinsic) and exogenous (extrinsic) factors. Because of the fact that skin health and beauty is considered one of the principal factors representing overall "well-being" and the perception of "health" in humans, several antiaging strategies have been developed during the last years. It is the intention of this article to review the most important anti-aging strategies that dermatologists have nowadays in hand, including preventive measurements, cosmetological strategies, topical and systemic therapeutic agents and invasive procedures.

The development of resistant malaria and lethality of the disease demands the search for new therapeutic candidates. In this line-up, thiolactone was identified as the potential lead structure and subjected to hologram quantitative structure-activity relationship (HQSAR), comparative molecular field analysis (CoMFA) and comparative molecular similarity indices analysis (CoMSIA). Overall, the QSAR results shows that the LOO cross-validated q(2) values of HQSAR, CoMFA and CoMSIA models are 0.791, 0.737 and 0.753, respectively. According to HQSAR, the hydrogen bond donor and acceptor were found to play an important role in governing antimalarial activity of thiolactone derivatives. The fragment contribution map of HQSAR, and contour maps of CoMFA and CoMSIA showed the presence of an electronegative group at the fifth position, and a bulky group at the third and fourth positions of the thiolactone ring, positively contributing to antimalarial activity. Furthermore, molecular docking was performed to analyze the binding mode of newly designed thiolactones with the active site residues of pf KAS I/II. The prediction of newly designed thiolactone molecules based on QSAR and docking score are in good accordance with each other. Therefore the ligand-based QSAR models and target structure-based docking model developed in this study may be successfully utilized for the design of new antimalarial agents.