62530-07-8

Upstream product

• 934-32-7 1H-benzimidazol-2-amine 
• 333-20-0 potassium thioacyanate 
• 6160-65-2 1,1'-Thiocarbonyldiimidazole 
• 6846-35-1 5-amino-3H-1,2,4-dithiazole-3-thione 
• 95-54-5 1,2-diamino-benzene 
• 83584-34-3 N-benzoyl-N'-(benzimidazol-2-yl)thiourea 

Relevant academic research and scientific papers

Metal-mediated inhibition of escherichia coli methionine aminopeptidase: Structure-activity relationships and development of a novel scoring function for metal-ligand interactions

We report the discovery of thiabendazole as a potent inhibitor (K 1 = 0.4 μM) of Escherichia coli methionine aminopeptidase (ecMetAP) and the synthesis and pharmacological evaluation of thiabendazole congeners with activity in the upper nanomolar range, Elucidation of the X-ray structure of ecMetAP in complex with thiabendazole and an unrelated inhibitor that was independently described by another group showed that that both compounds bind to an additional CoII ion at the entrance of the active site. This unexpected finding explains the inactivity of the compounds under in vivo conditions. It also allows us to discuss the structure-activity relationships of this series of compounds in a meaningful way, based upon docking runs with an auxiliary metal ion, We describe a new scoring function for the evaluation of metal-mediated inhibitor binding that, unlike the previously used scoring function implemented in the docking program, allows us to distinguish between active and inactive compounds, Finally, conclusions for the structure-based design of in vivo-active inhibitors of ecMetAP are drawn.

GUANIDINE COMPOUNDS, AND USE THEREOF AS BINDING PARTNERS FOR 5-HT5 RECEPTORS

The invention relates to guanidine compounds of general formula (I), corresponding enantiomeric, diastereomeric, and/or tautomeric forms thereof, and pharmaceutically acceptable salts thereof. The invention further relates to the use of guanidine compounds as binding partners for 5-HT5 receptors in order to treat diseases modulated by 5-HT5 receptor activity, especially treat neurodegenerative and neuropsychiatric disorders and the signs, symptoms, and malfunctions associated therewith.

Five-membered heterocyclic compounds as inhibitors of SRC family protein kinase.

The present invention refers to novel substituted aromatic heteroaryl derivatives of formula (I). with the definitions of A, L1, L2, G, J, X and Y according to claim 1. These novel compounds are useful for the inhibition of protein kinases, particularly of the inhibition of Src family protein kinases. Methods for inhibiting kinases by contacting kinases with these novel compounds are disclosed. In another embodiment the present invention refers to pharmaceutical compositions containing these novel compounds and their use for the preparation of medicaments for treating diseases or disorders associated with unphysiological activity of kinases in the body, particularly for the treatment of cancer, immunosuppression, and osteoporosis.

Pyrimidinone antibiotics - Heterocyclic analogues with improved antibacterial spectrum

We report the synthesis and pharmacological evaluation of new derivatives of the natural dipeptide antibiotic TAN 1057 A,B containing heterocycles either in the β-amino acid side chain or as mimics of the urea function. In the course of this program, we identified novel analogues that display activity towards a broader panel of Gram-positive bacteriae.