Synthesis and evaluation of substituted 4-arylimino-3-hydroxybutanoic acids as potential HIV-1 integrase inhibitors

A series of readily accessible 4-arylimino-3-hydroxybutanoic acids have been prepared and evaluated as potential HIV-1 Integrase inhibitors. None of the ligands exhibited significant toxicity against human embryonic kidney (HEK 293) cells, while five of them showed activity against HIV-1 integrase – the most active (6c) with an IC₅₀ value of 3.5?μM. In silico docking studies indicate the capacity of ligand 6c to interact with several amino acid residues and the two Mg²⁺ cations in the HIV-1 integrase receptor cavity.     

The Impact of Climate Change on the Potential Distribution of Agricultural Pests: The Case of the Coffee White Stem Borer (Monochamus leuconotus P.) in Zimbabwe

The production of agricultural commodities faces increased risk of pests, diseases and other stresses due to climate change and variability. This study assesses the potential distribution of agricultural pests under projected climatic scenarios using evidence from the African coffee white stem borer (CWB), Monochamus leuconotus (Pascoe) (Coleoptera: Cerambycidae), an important pest of coffee in Zimbabwe. A species distribution modeling approach utilising Boosted Regression Trees (BRT) and Generalized Linear Models (GLM) was applied on current and projected climate data obtained from the WorldClim database and occurrence data (presence and absence) collected through on-farm biological surveys in Chipinge, Chimanimani, Mutare and Mutasa districts in Zimbabwe. Results from both the BRT and GLM indicate that precipitation-related variables are more important in determining species range for the CWB than temperature related variables. The CWB has extensive potential habitats in all coffee areas with Mutasa district having the largest model average area suitable for CWB under current and projected climatic conditions. Habitat ranges for CWB will increase under future climate scenarios for Chipinge, Chimanimani and Mutare districts while it will decrease in Mutasa district. The highest percentage change in area suitable for the CWB was for Chimanimani district with a model average of 49.1% (3 906 ha) increase in CWB range by 2080. The BRT and GLM predictions gave similar predicted ranges for Chipinge, Chimanimani and Mutasa districts compared to the high variation in current and projected habitat area for CWB in Mutare district. The study concludes that suitable area for CWB will increase significantly in Zimbabwe due to climate change and there is need to develop adaptation mechanisms.