88811-16-9Relevant academic research and scientific papers
Design and synthesis of conformationally restricted inhibitors of active thrombin activatable fibrinolysis inhibitor (TAFIa)
Brink, Mikael,Dahlen, Anders,Olsson, Thomas,Polla, Magnus,Svensson, Tor
, p. 2261 - 2268 (2014/04/17)
A series of 4,5,6,7-tetrahydro-1H-benzimidazole-5-carboxylic acid and 5,6,7,8-tetrahydroimidazo[1,2-a]pyridine-7-carboxylic acid derivatives designed as inhibitors of TAFIa has been prepared via a common hydrogenation-alkylation sequence starting from the appropriate benzimidazole and imidazopyridine system. We present a successful design strategy using a conformational restriction approach resulting in potent and selective inhibitors of TAFIa. The X-ray structure of compound 5 in complex with a H333Y/H335Q double mutant TAFI indicate that the conformational restriction is responsible for the observed potency increase.
Acyclic nucleoside analogues as inhibitors of Plasmodium falciparum dUTPase
Nguyen, Corinne,Ruda, Gian Filippo,Schipani, Alessandro,Kasinathan, Ganasan,Leal, Isabel,Musso-Buendia, Alexander,Kaiser, Marcel,Brun, Reto,Ruiz-Pérez, Luis M.,Sahlberg, Britt-Louise,Johansson, Nils Gunnar,González-Pacanowska, Dolores,Gilbert, Ian H.
, p. 4183 - 4195 (2007/10/03)
We report the discovery of novel uracil-based acyclic compounds as inhibitors of deoxyuridine 5′-triphosphate nucleotidohydrolase (dUTPase), an enzyme involved in nucleotide metabolism that has been identified as a promising target for the development of
Anti-MRSA cephems. Part 2: C-7 cinnamic acid derivatives
Springer, Dane M.,Luh, Bing-Yu,Goodrich, Jason,Bronson, Joanne J.
, p. 265 - 279 (2007/10/03)
Forty-five novel cephalosporin derivatives with activity against methicillin-resistant Staphylococcus aureus (MRSA) are described. The compounds contain novel cinnamic acid moieties at C-7 that were synthesized using a key Heck reaction followed by nucleophilic aromatic substitution reactions. The most active compound (41) displayed an MIC90 against MRSA of 1.0 μg/mL, and a PD50 of 0.8 mg/kg. Compound 14 was found to be very safe in a mouse model of acute toxicity.
Pharmaceuticals
-
, (2008/06/13)
The present invention provides compounds of formula (I) as well as the use of such compounds in pharmaceutical compositions and methods of treatment. The compounds described herein represent a class of TAFIla inhibitors suitable for use in treating condit
Efficient synthesis of azetidine through N-trityl- or N- dimethoxytritylazetidines starting from 3-amino-1-propanol or 3- halopropylamine hydrohalides
Huszthy,Bradshaw,Krakowiak,Wang,Dalley
, p. 1197 - 1207 (2007/10/02)
Efficient synthetic routes for the preparation of azetidine starting from commercially available 3-amino-1-propanol or 3-halopropylamine hydrohalides are reported. First, the appropriate N-trityl- or N-dimethoxytrityl protected tosyloxy- or halopropylamines were prepared. These precursors were then cyclized into the N-trityl- or N-dimethoxytritylazetidines. The N-protecting groups were removed in the presence of perchloric acid giving the hydrogen perchlorate salt of azetidine. The latter compound was transformed into its free base using a strong base under anhydrous conditions. The relatively expensive 4,4'-dimethoxytrityl chloride and less expensive trityl chloride used in these synthetic procedures were recycled in good yields. Azetidine hydrogenperchlorate can be used to prepare N-substituted azetidines without the need to isolate the free azetidine.
2-AMINOPYRIMIDINE-4-CARBOXAMIDE DERIVATIVES, THEIR PREPARATION AND THEIR APPLICATION IN URINARY THERAPEUTICS
-
, (2008/06/13)
A compound of formula (I) STR1 in which n denotes 2, 3, 4, or 5, p denotes 0 or 1,m denotes 0, 1, 2, 3, 4, or 5, and R 1 denotes a hydrogen atom or a methyl group,each X, which may be identical or different to any other X if m is greater than 1, denotes fluorine, chlorine, methoxy, isopropyl or cyclopropyl,in the form of a free base or an acid addition salt.
AMINOALKYL AND RELATED SUBSTITUTED PHOSPHINIC ACID ANGIOTENSIN CONVERTING ENZYME INHIBITORS
-
, (2008/06/13)
Compounds of the structure STR1 are provided which are inhibitors of angiotensin converting enzyme and are useful in the treatment of hypertension.
