51220-52-1Relevant academic research and scientific papers
Discovery of Benzamide Analogues as a Novel Class of 5-HT3 Receptor Agonists
Jorgensen, Charlotte G.,Frolund, Bente,Kehler, Jan,Jensen, Anders A.
body text, p. 725 - 736 (2012/01/06)
A 5-HT3 receptor agonist based on a benzamide scaffold was identified in a screening of a small commercial compound library, and an elaborate SAR study originating from this hit was performed. The design, synthesis, and functional characterisation of benzamide analogues at the 5-HT3A receptor yielded substantial information concerning the analogues as 5-HT3 receptor agonists. However, the potencies of the derived analogues were not significantly improved over that of the initial hit. The benzamide scaffold constitutes a novel type of 5-HT3 receptor agonist, as it does not possess a positively charged functionality, which is essential for the binding of all orthosteric ligands to the receptor. Preliminary investigations suggest that the compounds may exert their effects on 5-HT3 receptors by binding to an allosteric site in the receptor complex.
Synthesis and study of some compounds containing oxazolone ring, showing biological activity
Tandel,Mammen, Denni
, p. 932 - 937 (2008/12/23)
Synthesis of the oxazolone ring has been performed by the condensation of 4-substituted alkoxy benzoyl glycine with appropriate 4-substituted alkoxy benzaldehyde, in the presence of acetic anhydride and anhydrous sodium acetate. The antibacterial activity has been checked against Micrococcus luteus and Escherichia coli and antifungal activity against Alternaria alternate and Phoma multirostata for all the compounds. The cytotoxicity has been checked against the monocots barley seeds: Hordeum vulgare L and dicots moong seeds; Phaseolus aureus. The compounds having electron releasing group exhibit antibacterial activity. Compounds with nitro group cause total inhibition of seed germination, exhibiting cytotoxic behaviour. The structures of the synthesized compounds have been characterized by elemental analysis and spectral data and the purity of the compounds has been checked by TLC method.
Polymer-Supported Mitsunobu Ether Formation and its Use in Combinatorial Chemistry
Krchnak, Viktor,Flegelova, Zuzka,Weichsel, Aleksandra S.,Lebl, Michal
, p. 6193 - 6196 (2007/10/02)
Aromatic hydroxy acids have been attached to a polymeric solid support and the phenolic hydroxy groups have been reacted with a variety of primary and secondary alcohols under the conditions of the Mitsunobu reaction (triphenylphosphine and diethyl azodicarboxylate) in tetrahydrofuran.In most cases the reaction provided a nearly quantitative yield of alkyl aryl ethers, as determined after cleaving theproduct from the resin.To demonstrate that the polymer-supported Mitsunobu reaction is useful for combinatorial library synthesis, we synthesized a number of model compounds and a simple three randomization step library composed of 4,200 different compounds.
