In the past decade, alternative benign organic methodologies have become an imperative part of organic syntheses and chemical reactions. The various new and innovative sustainable organic reactions and methodologies using no solvents or catalysts and employing alternative energy inputs such as microwaves, sonication, conventional and room temperature heating conditions, mechanochemical mixing, and high-speed ball milling are discussed in detail. Environmentally benign and pharmaceutically important reactions such as multicomponent, condensation, and Michael addition reactions; ring opening of epoxides; and oxidation and other significant organic reactions are discussed. An overview of benign reactions through solvent- and catalyst-free (SF-CF) chemistry and a critical perspective on emerging synergies between SF-CF organic reactions are discussed.

Solvent-free and catalysts-free chemistry: a benign pathway to sustainability.

Metalloenzymes are central to a wide range of essential biological activities, including nucleic acid modification, protein degradation, and many others The role of metalloenzymes in these processes also makes them central for the progression of many diseases and, as such, makes metalloenzymes attractive targets for therapeutic intervention Increasing awareness of the role metalloenzymes play in disease and their importance as a class of targets has amplified interest in the development of new strategies to develop inhibitors and ultimately useful drugs In this Review, we provide a broad overview of several drug discovery efforts focused on metalloenzymes and attempt to map out the current landscape of high-value metalloenzyme targets

Targeting Metalloenzymes for Therapeutic Intervention

Studies on synthesis and pharmacological activities of 3,6-disubstituted-1,2,4-triazolo[3,4-b]-1,3,4-thiadiazoles and their dihydro analogues.

The invention relates to compounds of formula (I) their derivatives comprising a detectable label, their compositions and their use in the treatment of human immunodeficiency virus (HIV) infection. In particular, the invention provides novel inhibitors of HIV replication, pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HIV infection.

Inhibitors of human immunodeficiency virus replication

2011 Hidayat Hussain,*,† Ahmed Al-Harrasi,*,† Ahmed Al-Rawahi,† Ivan R. Green,‡ and Simon Gibbons* †UoN Chair of Oman’s Medicinal Plants and Marine Natural Products, University of Nizwa, P.O. Box 33, Birkat Al Mauz, Nizwa 616, Sultanate of Oman ‡Department of Chemistry and Polymer Science, University of Stellenbosch, Private Bag X1, Matieland, Stellenbosch 7600, South Africa Department of Pharmaceutical and Biological Chemistry, UCL School of Pharmacy, London WC1N 1AX, United Kingdom

Fruitful Decade for Antileishmanial Compounds from 2002 to Late 2011

Linker-modified quinoline derivatives targeting HIV-1 integrase: synthesis and biological activity.

New HIV-1 replication inhibitors of the styryquinoline class bearing aroyl/acyl groups at the C-7 position: synthesis and biological activity.

Novel variants of HIV-1 replication inhibitors of the styrylquinoline class harboring aroyl/acyl group at the C-7 position have been synthesized. In sharp contrast with styrylquinolines bearing a carboxylic acid group at C-7, these compounds proved to be inactive toward HIV-1 integrase in in vitro assays.

Claire-Marie Thomas

Papers

Linker-modified quinoline derivatives targeting HIV-1 integrase: synthesis and biological activity.

New HIV-1 replication inhibitors of the styryquinoline class bearing aroyl/acyl groups at the C-7 position: synthesis and biological activity.

New HIV‐1 Replication Inhibitors of the Styryquinoline Class Bearing Aroyl/Acyl Groups at the C‐7 Position: Synthesis and Biological Activity.