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Forests have historically been under significant land use pressures that cause periods of degradation, clearance, and recovery. To understand these changes, studies are needed that place trends in a historical landscape context and also examine recent dynamics. Here, we use historical investigation (c. 1800) and an examination of land use and land cover change between 1973 and 2006 to establish a baseline trajectory of the forested system of the south-central United States (US) plains. The study culminates in a highly detailed accounting of the processes and causes of land change between 2001 and 2006. In the study region, the forest transitioned from early low-intensity use, to clearance for farming and timber, to widespread recovery from degradation beginning in the 1930s. By 1970, the region was transitioning from recovered woodlands to an intensive regime of recurrent timber harvest and replanting. The recurring cycle inherent in intensive silviculture has been the main cause of land change for the past several decades, accounting for more than 95% of the total extent of change between 2001 and 2006. The transition to forest recovery in the south-central US was an important historical occurrence. However, the dynamic post-transition landscape needs to be better understood. [ABSTRACT FROM AUTHOR]

Abstract: Optically active α-amino 4H-[1,2,4]oxadiazol-5-ones (oxadiazolones) were prepared from optically active α-amino acids in five synthetic steps. The oxadiazolone moiety serves as a bioisosteric replacement for the carboxylic acid. Incorporation of an α-amino oxadiazolone into a representative dipeptide mimic is described. [Copyright &y& Elsevier]

Abstract: A novel series of bacterial topoisomerase (3-aminoquinazolinediones) inhibitors are described. The side-chain SAR against Gram-positive and Gram-negative organisms as well as DNA gyrase activity is reported. [Copyright &y& Elsevier]

Abstract: Novel 2,4-diaminopyrimidine-based small molecule renin inhibitors are disclosed. Through high throughput screening, parallel synthesis, X-ray crystallography, and structure based drug design, we have developed the first non-chiral, non-peptidic, small molecular template to possess moderate potency against renin. The designed compounds consist of a novel 6-ethyl-5-(1,2,3,4-tetrahydroquinolin-7-yl)pyrimidine-2,4-diamine ring system that exhibit moderate potency (IC50: 91–650nM) against renin while remaining ‘Rule-of-five’ compliant. [Copyright &y& Elsevier]

Abstract: Several novel series of nitrile-containing fluoroquinolones with weakly basic amines are reported which have reduced potential for hERG (human ether-a-go-go gene) channel inhibition as measured by the dofetilide assay. The new fluoroquinolones are potent against both Gram-positive and fastidious Gram-negative strains, including Methicillin resistant Staphylococcus aureus and fluoroquinolone-resistant Streptococcus pneumoniae. Several analogs also showed low potential for human genotoxicity as measured by the clonogenicity test. Compounds 22 and 37 (designated PF-00951966 and PF-02298732, respectively), which had good in vitro activity and in vitro safety profiles, also showed good pharmacokinetic properties in rats. [Copyright &y& Elsevier]

Abstract: A series of 3-aminoquinazolinediones was synthesized and evaluated for its antibacterial and DNA gyrase activity. The SAR around the quinazolinedione core was explored and the optimal substitutions were combined to give two compounds, 2r and 2s, with exceptional enzyme potency (IC50 = 0.2μM) and activity against Gram-positive organisms (MIC’s = 0.015–0.06μ g/mL). [Copyright &y& Elsevier]

Abstract: A systematic investigation of the S3 sub-pocket activity requirements was conducted. It was observed that linear and sterically small side chain substituents are preferred in the S3 sub-pocket for optimal renin inhibition. Polar groups in the S3-sub-pocket were not well tolerated and caused a reduction in renin inhibitory activity. Further, compounds with clog P’s⩽3 demonstrated a dramatic reduction in CYP3A4 inhibitory activity. [Copyright &y& Elsevier]

Abstract: Processes for the synthesis of fluorinated 1,8-naphthyridinone derivatives including 6,7-difluoro-1,8-naphthyridin-2-one are described. [Copyright &y& Elsevier]

Abstract: A series of regioisomerically monofluorinated 1-(naphthalen-1-yl)piperazines is described. [Copyright &y& Elsevier]