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J Med Chem 2022 Aug 3. Epub 2022 Aug 3.

Max-Delbrück-Centrum für Molekulare Medizin in der Helmholtz-Gemeinschaft (MDC), Robert-Rössle-Str. 10, 13125 Berlin-Buch, Germany.

Tryptophan hydroxylases catalyze the first and rate-limiting step in the synthesis of serotonin. Serotonin is a key neurotransmitter in the central nervous system and, in the periphery, functions as a local hormone with multiple physiological functions. Studies in genetically altered mouse models have shown that dysregulation of peripheral serotonin levels leads to metabolic, inflammatory, and fibrotic diseases. Read More

Sci Rep 2022 Jul 29;12(1):13004. Epub 2022 Jul 29.

Departamento de Ciencias Biomédicas, Facultad de Veterinaria, Universidad de León, 24071, León, Spain.

The control of gastrointestinal nematodes in livestock is becoming increasingly difficult due to the limited number of available drugs and the rapid development of anthelmintic resistance. Therefore, it is imperative to develop new anthelmintics that are effective against nematodes. Under this context, we tested the potential toxicity of three compounds in mice and their potential anthelmintic efficacy in Mongolian gerbils infected with Haemonchus contortus. Read More

Int J Mol Sci 2022 Jul 27;23(15). Epub 2022 Jul 27.

Laboratory of Chemistry of Biologically Active Compounds, Faculty of Chemistry, University of Gdańsk, Wita Stwosza 63, 80-308 Gdańsk, Poland.

Mastoparan (MP) is an antimicrobial cationic tetradecapeptide with the primary structure INLKALAALAKKIL-. This amphiphilic α-helical peptide was originally isolated from the venom of the wasp . MP shows a variety of biological activities, such as inhibition of the growth of Gram-positive and Gram-negative bacteria, as well as hemolytic activity and activation of mast cell degranulation. Read More

Chem Asian J 2022 Jul 26. Epub 2022 Jul 26.

Indian Institute of Technology-Hyderabad, Chemistry, Kandi Medak Telangana India 502285, 502285, 502285, Hyderabad, INDIA.

The first discrete seven-membered cyclic zinc(II) complex catalyzed room temperature Knoevenagel condensation reactions, and the synthesis of perimidine derivatives has been reported under mild reaction conditions. The cyclic zinc(II) complex [( L) ZnBr 2 ] ( 1 ) was isolated from the reaction between 1-(2-hydroxyethyl)-3-isopropyl-benzimidazole-2-thione ( L ) and ZnBr 2 . Complex 1 was characterized by different analytic techniques such as FT-IR, CHNS, TGA, NMR, and SCXRD. Read More

Biochem Biophys Res Commun 2022 Jul 16;623:17-22. Epub 2022 Jul 16.

Hwa Mei Hospital, University of Chinese Academy of Sciences, Ningbo, 315000, China; Ningbo Institute of Life and Health Industry, University of Chinese Academy of Sciences, Ningbo, 315000, China. Electronic address:

Inhibition of the bromodomain of the CREB (cyclic-AMP response element-binding protein) binding protein (CBP) is a particularly promising new therapeutic approach for cancer. Benzimidazole derivatives CCS1477 and its analogues (8 and 9) are highly potent and selective CBP bromodomain inhibitors, with K values of 26.4, 37. Read More