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"Barrier, reservoir, target site, those are but some of the possible functions of biological lipid membranes in the complex interplay of drugs with the organism. A detailed knowledge of lipid membranes and of the various modes of drug-membrane interaction is therefore the prerequisite for a better understanding of drug action. Many of today's pharmaceuticals are amphiphilic or catamphiphilic, enabling them to interact with biological membranes. Crucial membrane properties are surveyed and techniques to elucidate drug-membrane interactions presented, including computer-aided predictions. Effects of membrane interaction on drug action and drug distribution are discussed, and numerous examples are given.This unique reference volume builds on the authors' long experience in the study of drug-membrane interaction. "

"The only reference on current methods to generate pharmacokinetic and safety profiles of drug candidates, as well as how they must be balanced against one other for the best selection of candidates for further development. Following a brief introduction to the necessities of filtering and risk assessment of potential new drug molecules before actual drug development, the two equally important aspects of pharmacological (ADME) and safety (toxicity) profiling are covered in separate parts. The ADME section covers the profiling of basic physicochemical parameters, such as solubility and permeability, as well as more complex traits, such as the likelihood of drug-drug interactions, metabolic clearance and protein binding properties. The toxicology part addresses, among others, recent advances in early genetic toxicity testing, bioactivation screening, organ-specific toxicity assays for liver, heart, kidney and blood, as well as profiling for autoimmune reactions. By addressing both drug efficiency and drug safety, this modern practical reference shows readers how each individual aspect figures in shaping the key decisions on which the entire drug development process hinges. In short, this is a complete toolbox for assessing the risk/benefit ratio for any novel compound during the early drug development stages, using both in vitro and in silico methods."

"This practice-oriented handbook surveys current knowledge on the prediction and prevention of adverse drug reactions related to off-target activity of small molecule drugs. It is unique in collating the current approaches into a single source, and includes several highly instructive case studies that may be used as guidelines on how to improve drug development projects. With its large section on ADME-related effects, this is key knowledge for every drug developer."

"This first systematic overview for more than a decade is tailor-made for the medicinal chemist. All the chapters are written by experienced drug developers and include practical examples from real drug candidates. Following an introduction to global drug properties and their impact on drug research, screening and combinatorial chemistry libraries, this handbook demonstrates the best and fastest way to estimate those properties most relevant for the efficiency and pharmacokinetic performance of a drug molecule: lipophilicity,solubility, electronic properties and conformation."

"Summary:This book describes some of the most exciting developments for the discovery of new drugs, such as Fragment-based methods. This book includes experimental approaches using X-ray crystallography and NMR for Fragment-based screening as well as other biophysical methods for studying protein/ligand interactions"

"Obat Antiinflamasi Nonsteroid (AINS) merupakan salah satu obat anti-inflamasi yang dipakai secara luas oleh pasien tertentu. Mekanisme kerja AINS umumnya adalah menginhibisi sintesis prostaglandin dengan menginhibisi aktivitas COX secara tidak selektif. Adanya inhibisi COX-1 dapat menyebabkan timbulnya efek samping pada saluran gastrointestinal. Walaupun begitu, AINS masih tetap menjadi obat pilihan untuk terapi inflamasi. Karena itu, sampai saat ini pengembangan baru obat AINS masih dilakukan, khususnya untuk memperoleh inhibitor selektif COX-2 dengan profil keamanan yang baik, terlebih dengan munculnya fakta bahwa inhibitor selektif COX-2 dapat menyebabkan risiko kardiovaskular. Beberapa penelitian pengembangan inhibitor selektif COX-2 telah dilakukan menggunakan derivat-derivat tertentu dengan memperhatikan hubungan antara struktur dan aktivitas. Dari hasil penelitian-penelitian tersebut diketahui bahwa gugus aminosulfonil dan metansulfonil merupakan bagian terpenting dalam menghasilkan selektivitas terhadap COX-2 dan efikasinya. Ulasan ini membahas lebih lanjut perkembangan pengembangan inhibitor selektif COX-2 berdasarkan pengaruh modifikasi struktur terhadap tingkat selektivitasnya sehingga dapat menghasilkan senyawa dengan risiko kardiovaskular yang rendah.

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Nonsteroidal Anti-inflammation Drugs (NSAID) is one of anti-inflammation drug that is used extensively by certain patients. The mechanism of action of NSAID is by inhibiting prostaglandins synthesis by inhibiting COX activity. Inhibition of COX-1 activity can lead to some side effects in the gastrointestinal tract. However, NSAID is still a drug of choice. Therefore, until now, new drug NSAID development is still being carried out, primarily to obtain COX-2 selective inhibitors with a good safety profile, especially with the emergence of the fact that COX-2 selective inhibitors can cause cardiovascular risk. Some research for developing COX-2 selective inhibitor has been done using certain derivatives by considering the relationship between its structure and activity. The results of these studies are known that the aminosulfonyl and methanesulfonyl groups are the most important part of producing selectivity to COX-2 and its efficacy. This review further discusses the development of COX-2 selective inhibitors based on the effect of structural modification on its level of selectivity to produce compounds with low cardiovascular risk."