Journal of enzyme inhibition and medicinal chemistry, 35(1), 109-117 (2019-11-07)
With the aim to obtain novel compounds possessing both strong affinity against human carbonic anhydrases and low toxicity, we synthesised novel thiourea and sulphonamide derivatives 3, 4 and 10, and studied their in vitro inhibitory properties against human CA I, CA
We here report on the synthesis of new series of polycyclic amines initially designed as ring-rearranged analogs of amantadine and featuring pentacyclo, hexacyclo, and octacyclo rings. A secondary amine, 3-azahexacyclo[7.6.0.0¹,⁵.0⁵,¹².0⁶,¹⁰.0¹¹,¹⁵]pentadeca-7,13-diene, 3, effectively inhibited A/M2 proton channel function, and, moreover, possessed
European journal of medicinal chemistry, 139, 412-428 (2017-08-19)
Recent findings suggest that treatment with 11β-HSD1 inhibitors provides a novel approach to deal with age-related cognitive dysfunctions, including Alzheimer's disease. In this work we report potent 11β-HSD1 inhibitors featuring unexplored pyrrolidine-based polycyclic substituents. A selected candidate administered to 12-month-old
European journal of medicinal chemistry, 84, 107-117 (2014-07-13)
Optimization of an essentially inactive 3,4-dihydro-2H-pyrano[3,2-c]quinoline carboxylic ester derivative as acetylcholinesterase (AChE) peripheral anionic site (PAS)-binding motif by double O → NH bioisosteric replacement, combined with molecular hybridization with the AChE catalytic anionic site (CAS) inhibitor 6-chlorotacrine and molecular dynamics-driven
Brazilian journal of biology = Revista brasleira de biologia, 70(4), 1065-1068 (2010-12-25)
The increase in the resistance to antimicrobial drugs in use has attracted the attention of the scientific community, and medicinal plants have been extensively studied as alternative agents for the prevention of infections. The Candida genus yeast can become an