Introduced to the Market in the Last Decade (2001−2011) Jiang Wang,† María Sańchez-Rosello,́‡,§ Jose ́ Luis Aceña, Carlos del Pozo,‡ Alexander E. Sorochinsky, Santos Fustero,*,‡,§ Vadim A. Soloshonok,* and Hong Liu*,† †Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zu Chong Zhi Road, Shanghai 201203, China ‡Department of Organic Chemistry, Faculty of Pharmacy, University of Valencia, Av. Vicente Andreś Estelleś, 46100 Burjassot, Valencia, Spain Laboratorio de Molećulas Orgańicas, Centro de Investigacioń Príncipe Felipe, C/ Eduardo Primo Yuf́era 3, 46012 Valencia, Spain Department of Organic Chemistry I, Faculty of Chemistry, University of the Basque Country UPV/EHU, Paseo Manuel Lardizab́al 3, 20018 San Sebastian, Spain IKERBASQUE, Basque Foundation for Science, Alameda Urquijo, 36-5 Plaza Bizkaia, 48011 Bilbao, Spain Institute of Bioorganic Chemistry and Petrochemistry, National Academy of Sciences of Ukraine, Murmanska Street 1, 02660 Kyiv-94, Ukraine

Fluorine in pharmaceutical industry: fluorine-containing drugs introduced to the market in the last decade (2001-2011).

Large-Scale Carbonyl Reductions in the Pharmaceutical Industry

Recent advances bioactive 1,2,4-triazole-3-thiones.

Resistance to antibiotics is a major global problem and there is an urgent need to develop new therapeutic agents. Although many classes of active compounds have been established as efficient derivatives in diverse fields of antimicrobial therapy, they have not yet found wide application against a few deadly microbes. In recent years, compounds have been developed that have solved some of the problems posed; for example improved bioavailability is one of the targets achieved with most of the more recent compounds, allowing for once-daily dosing. Benzofuran and its derivatives are found to be suitable structures, existing widely in natural products and unnatural compounds with a wide range of biological and pharmacological applications; thus, considerable attention has been focused on the discovery of new drugs in the fields of drug invention and development. Some benzofuran derivatives, such as psoralen, 8-methoxypsoralen and angelicin have been used in the treatment of skin diseases such as cancer or psoriasis. The unique structural features of benzofuran and its wide array of biological activities make it a privileged structure in the field of drug discovery, especially in the search for efficient antimicrobial candidates. Recently, this scaffold has emerged as a pharmacophore of choice for designing antimicrobial agents that are active toward different clinically approved targets. To pave the way for future research, there is a need to collect the latest information in this promising area. In the present review, we collated the published reports on this versatile core to provide a deeper insight, so that its full therapeutic potential can be utilized for the treatment of microbial diseases. This study systematically provides a comprehensive report on current developments in benzofuran-based compounds as antimicrobial agents and is also helpful for the researchers working on a substitution pattern around the nucleus, with an aim to help medicinal chemists to develop structure activity relationships (SAR) on these derivatives as antimicrobial drugs.

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Benzofuran: an emerging scaffold for antimicrobial agents

A review on antioxidant potential of bioactive heterocycle benzofuran: Natural and synthetic derivatives

Previously unknown biphenyl containing 5-phenyl-1-benzofuran-2-yl derivatives; methanones (2a–i), tertiary alcohols (3a–l), and carbinols (4a–f) were synthesized and evaluated for their antimicrobial and antioxidant activities to study the effect of functionalization at the carbonyl carbon and substitution at biphenyl ring on these activities. The introduction of hydroxyl group at carbonyl carbon enhanced the antioxidant property (3a, 3g, 3h, 4a, and 4b), while antimicrobial activity decreased; the carbinol and tertiary alcohols corresponding to methanone 2a and 2b showed no antimicrobial activity. Biphenyl methanones 1, 2a, 2f, and 2g exhibited antimicrobial activity with minimal inhibitory concentration ranging between 0.001 and 0.500 mg/mL, tertiary alcohols 3a, 3g, and 3h and carbinols 4a and 4b exhibited the promising antioxidant property. The mode of action of these active compounds was carried out by docking of receptor GlcN6P synthase with newly synthesized candidate ligands 1, 2a, 2e, 2f, 2g, 2h, 3a, 3g, 3h, 4c, and 4d.

5-phenyl-1-benzofuran-2-yl derivatives: synthesis, antimicrobial, and antioxidant activity

A series of 1,2,4-triazole-based Schiff base heterocyclic compounds (5a-f and 8a-i) and phenethylamines (7a-h) were synthesized and evaluated for antioxidant properties by free-radical scavenging, anti-hemolytic activity, lipid peroxidation, and their protective effects against DNA oxidative damage. Compounds 7c, 7d, 7h, 8b, and 8i showed promising DPPH(•) radical scavenging activity with the level of inhibition between 86.8% and 94%. Compounds 8a, 8b, 8d, 8g, and 8i were effective against the oxidative hemolysis of human erythrocytes and lipid peroxidation, in a dose-dependent manner, with IC50 values in the range of 55.7-80.7 and 53.2-81.2 µg/mL, respectively. Compounds 8a and 8b were effective against oxidative damage on erythrocyte ghost membrane proteins, and 8g and 8i were able to protect against DNA oxidative damage.

Synthesis and evaluation of antioxidant properties of novel 1,2,4-triazole-based schiff base heterocycles.

Diastereoselective Reduction of the Enone Intermediate of Travoprost

This invention relates to novel process for the preparation of prostaglandin compounds having formula (K), wherein R is selected from the group consisting of C1-C7 alkyl; C7-C17 aralkyl wherein the aryl group is unsubstituted or substituted with one to three substituents selected from the group consisting of C1-C6 alkyl, halo and CF3; and (CH2)nOR2 wherein n is from 1 to 3 and R2 represents a C6-C10 aryl group which is unsubstituted or substituted with one to three substituents selected from the group consisting of C1-C6 alkyl, halo and CF3; and R1 is selected from OR3 and NHR3 wherein R3 is C1-C6 alkyl, H; and dashed lines represents a double bond or a single bond, is disclosed. Novel intermediates are also disclosed.

A novel process for the preparation of prostaglandins and intermediates thereof

The present invention relates to a novel process for the preparation of S(+)-2-ethoxy-4-[N-{1-(2-piperidinophelyl)-3-methyl-1-butyl} aminocarbonylmethyl]-benzoic acid derivatives.

Chandrashekar Aswathanarayanappa

Papers

5-phenyl-1-benzofuran-2-yl derivatives: synthesis, antimicrobial, and antioxidant activity

Synthesis and evaluation of antioxidant properties of novel 1,2,4-triazole-based schiff base heterocycles.

Diastereoselective Reduction of the Enone Intermediate of Travoprost

A novel process for the preparation of prostaglandins and intermediates thereof

Process for the preparation of s(+)-2-ethoxy-4-[n-{1-(2-piperidinophelyl)-3-methyl-1- butyl} aminocarbonylmethyl]benzoic acid derivatives