Design, synthesis and evaluation of 3-quinoline carboxylic acids as new inhibitors of protein kinase CK2.

In this article, the derivatives of 3-quinoline carboxylic acid were studied as inhibitors of protein kinase CK2. Forty-three new compounds were synthesized. Among them 22 compounds inhibiting CK2 with IC in the range from 0.

THE USE OF DEXMEDETOMIDINE IN COMBINATION NEFOPAM FOR POSTOPERATIVE ANALGESIA AFTER LAPAROSCOPIC CORRECTION OF MORBID OBESITY.

Aim: To study the possibility of using a combination of dexmedetomidine with nefopam for postoperative analgesia in patients with morbid obesity after bariatric surgery in anesthesia quality aspects and theimpact of the study on the combination during the inflammatory response to surgical trauma.

Subjects And Methods: A prospective cohort study of 48 patients with obesity.

Results: Based on the analysis of hemodynamic parameters, evaluation of pain using a numeric rating scale pain concluded that selective agonist of o-2 adrenergic dexmedetomidine in combination with nefopam provides effective postoperative pain relief in patients who underwent bariatric surgery, and is not a factor for suppression of postoperative inflammatory response Unlike the effects of ketorolac tromethamine, do not always provide a sufficient level of analgesia and reduce the rate of growth in the level of IL-6.

Design, synthesis and biological evaluation of 2-aminopyrimidinones and their 6-aza-analogs as a new class of CK2 inhibitors.

In order to find the new potent CK2 inhibitors the 60 derivatives of 2-aminopyrimidinone and their 6-aza-substituted analogs were synthesized and tested in vitro. Among them, the most efficient inhibitor 2-hydroxy-5-[4-(4-methoxyphehyl)-6-oxo-1,6-dihydropyrimidin-2-ylamino] benzoic acid was identified (IC50 = 1.1 μM).

Design, synthesis and evaluation of 2-phenylisothiazolidin-3-one-1,1-dioxides as a new class of human protein kinase CK2 inhibitors.

The synthesis and in vitro evaluation of 40 new 2-phenylisothiazolidin-3-one-1,1-dioxide derivatives are described. The optimization based on biological screening data and molecular modeling resulted in a 10-fold increase in inhibitory activity compared with previously reported inhibitors of this class and led to the identification of 3-{[2-chloro-4-(1,1-dioxido-3-oxoisothiazolidin-2-yl)benzoyl]amino}benzoic acid, a potent inhibitor of human protein kinase CK2 (ІC₅₀ = 1.5 μM).

Rational design of apoptosis signal-regulating kinase 1 inhibitors: discovering novel structural scaffold.

Increased activity of apoptosis signal-regulating kinase 1 (ASK1) is associated with a number of human disorders and the inhibitors of ASK1 may become important compounds for pharmaceutical application. Here we report novel ASK1 inhibitor scaffold, namely 5-(5-Phenyl-furan-2-ylmethylene)-2-thioxo-thiazolidin-4-one, that has been identified using virtual screening and biochemical tests. A series of derivatives has been synthesized and evaluated in vitro towards human protein kinase ASK1.