Publications by authors named "I Ia Kaula"
Article Synopsis
- Researchers have identified leucinyl benzenesulfonamides as a new class of effective inhibitors for leucyl-tRNA synthetase, a crucial enzyme in protein synthesis.
- Using isothermal titration calorimetry and docking studies, they analyzed how these inhibitors bind to the enzyme, providing insight into their binding energetics.
- The most basic compound in this series showed high affinity for the enzyme and demonstrated antibacterial effects against Gram-negative bacteria, suggesting its potential as a lead candidate for developing new antibiotics.
2-(3-(Naphthalen-2-yl)propanamido)cyclohex-1-enecarboxylic acid and its 6-hydroxynaphthalen-2-yl analogue are well-known hydroxyl-carboxylic acid (HCA) receptor HCA2 agonists. A series of novel aryl derivatives of 2-amidocyclohex-1-ene carboxylic acid that contained rigidity elements, such as an E-double bond, triple bond, and trans or cis-substituted cyclopropane rings, instead of the saturated ethane linker in the amide part of the molecules were designed and synthesized, and the derivatives' potency for the activation of HCA1, HCA2, and HCA3 receptors by 3'-5'-cyclic adenosine monophosphate (cAMP) assay were evaluated. The SAR studies revealed that the rigidifying of appropriate molecules enabled modulation of the potency and selectivity of the HCA2 receptor activation.
View Article and Find Full Text PDFFour methods of the synthesis of model glycosides with 11-deoxyprostaglandin E1 and a connecting polymethylene chain as the aglycone are compared. Interaction of potassium salt of prostaglandin PG with omega-iodoalkylglycosides is the most promising approach.
View Article and Find Full Text PDFHydroxyl-containing 11-deoxyprostaglandin E1 esters were synthesised by using the methods of mixed anhydrides and nucleophilic displacement.
View Article and Find Full Text PDF