Design, synthesis, and biological evaluation of phosphoramide derivatives as urease inhibitors

The design, synthesis, and biological evaluation of phosphoramide derivatives as urease inhibitors to reduce the loss of ammonia has been carried out. Forty phosphorus derivatives were synthesized and their inhibitory activities evaluated against that of jack bean urease. In addition, in vivo assays have been carried out. All of the compounds were characterized by IR, (1)H NMR, MS, and elemental microanalysis. In some cases, detailed molecular modeling studies were carried out, and these highlighted the interaction between the enzyme active center and the compounds and also the characteristics related to their activity as urease inhibitors. According to the IC(50) values for in vitro inhibitory activity, 12 compounds showed values below 1 microM and 8 of them represent improvements of activity in comparison to the commercial urease inhibitor N-n-butylthiophosphorictriamide (NBPT) (100 nM) (AGROTAIN). On the basis of the activity results and the conclusions of the molecular modeling study, a structural model for new potential inhibitors has been defined.     

Plant and animal endemism in the eastern Andean slope: challenges to conservation

Background

The Andes-Amazon basin of Peru and Bolivia is one of the most data-poor, biologically rich, and rapidly changing areas of the world. Conservation scientists agree that this area hosts extremely high endemism, perhaps the highest in the world, yet we know little about the geographic distributions of these species and ecosystems within country boundaries. To address this need, we have developed conservation data on endemic biodiversity (~800 species of birds, mammals, amphibians, and plants) and terrestrial ecological systems (~90; groups of vegetation communities resulting from the action of ecological processes, substrates, and/or environmental gradients) with which we conduct a fine scale conservation prioritization across the Amazon watershed of Peru and Bolivia. We modelled the geographic distributions of 435 endemic plants and all 347 endemic vertebrate species, from existing museum and herbaria specimens at a regional conservation practitioner's scale (1:250,000-1:1,000,000), based on the best available tools and geographic data. We mapped ecological systems, endemic species concentrations, and irreplaceable areas with respect to national level protected areas.

Results

We found that sizes of endemic species distributions ranged widely (< 20 km² to > 200,000 km²) across the study area. Bird and mammal endemic species richness was greatest within a narrow 2500-3000 m elevation band along the length of the Andes Mountains. Endemic amphibian richness was highest at 1000-1500 m elevation and concentrated in the southern half of the study area. Geographical distribution of plant endemism was highly taxon-dependent. Irreplaceable areas, defined as locations with the highest number of species with narrow ranges, overlapped slightly with areas of high endemism, yet generally exhibited unique patterns across the study area by species group. We found that many endemic species and ecological systems are lacking national-level protection; a third of endemic species have distributions completely outside of national protected areas. Protected areas cover only 20% of areas of high endemism and 20% of irreplaceable areas. Almost 40% of the 91 ecological systems are in serious need of protection (= < 2% of their ranges protected).

Conclusions

We identify for the first time, areas of high endemic species concentrations and high irreplaceability that have only been roughly indicated in the past at the continental scale. We conclude that new complementary protected areas are needed to safeguard these endemics and ecosystems. An expansion in protected areas will be challenged by geographically isolated micro-endemics, varied endemic patterns among taxa, increasing deforestation, resource extraction, and changes in climate. Relying on pre-existing collections, publically accessible datasets and tools, this working framework is exportable to other regions plagued by incomplete conservation data.     

Clinical features and outcomes of phacoemulsification in 39 horses: a retrospective study (1993-2003)

OBJECTIVE: To identify visual outcome and postoperative complications following phacoemulsification of equine cataracts. ANIMALS: Records of 39 horses (55 eyes) with cataracts were reviewed. METHODS: Eyes with cataracts removed by phacoemulsification were included in the study. Data collected included age, breed, sex, stage and etiology of cataract, unilateral vs. bilateral involvement, and ultrasound findings. Horses were grouped by etiology of the cataract. Visual outcome and complications were evaluated for each group and the overall population. RESULTS: Immediately postoperatively 46 out of 47 eyes (98%) were sighted. Four weeks postoperatively 23 of 29 operated eyes (79%) were sighted [13/18 (72%) eyes with congenital/juvenile onset, 6/6 (100%) eyes with traumatic and 4/5 (90%) eyes with uveitis-induced cataracts], with 18 eyes lost to follow-up. The most common postoperative complications included corneal edema (19 eyes/40%), fibrin in the anterior chamber (11 eyes/23%), postoperative ocular hypertension (9 eyes/19%), synechia/dyscoria (9 eyes/19%), and hyphema (7 eyes/15%). CONCLUSIONS: Prognosis for vision is favorable for horses following phacoemulsification and planned posterior continuous tear circular capsulorrhexis. Success rates depend on age of patient, cause of cataract and pre-existing intraocular disease. The highest success rate occurred in eyes with traumatic cataracts.