Thiophene bioisosteres
WebOn the basis of the 6′,7′-dihydrospiro[piperidine-4,4′-thieno[3,2-c]pyran] framework, a series of more than 30 σ ligands with versatile substituents in 1-, 2′-, and 6′-position has been synthesized and pharmacologically evaluated in order to find novel structure–affinity relationships. It was found that a cyclohexylmethyl residue at the piperidine N-atom … Web开馆时间：周一至周日7:00-22:30 周五 7:00-12:00; 我的图书馆
Thiophene bioisosteres
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WebOct 7, 2014 · The isosteric replacement changes one or more characteristics of the molecule: size, shape, hydrophobicity, solubility, pKa, reactivity. ... 1,2-Benzoxathiin-4 (3H)-one 2,2-dioxide – an... Weba thiophene ring. Thiophenes can be considered as bioisoteres of phenyl rings, and maintain the steric bulk, pi-electron cloud and planar structure of a phenyl ring. Thiophenes, …
WebJan 10, 2024 · The replacement of para -substituted benzenes with saturated bi- and polycyclic bioisosteres – bicyclo [1.1.1]pentane, bicyclo [2.2.2]octane and cubane, – often increases the potency, selectivity and metabolic stability of bioactive compounds. WebNov 1, 2013 · Thiophene bioisosteres of spirocyclic σ receptor ligands: relationships between substitution pattern and σ receptor affinity. C. Oberdorf, D. Schepmann, J. Vela, H. Buschmann, J. Holenz, B. Wünsch Chemistry Journal of medicinal chemistry 2012 TLDR
WebNov 9, 2024 · Optimized geometries with the labeled atoms of the anionic (left) and neutral (right) forms of two bioisosteres (-SO2NCF3-/-SO2NHCF3 on the top and -CO2-/-CO2H at the bottom) capped with a phenyl ring. Conformer 1 of the carboxylic bioisostere is displayed in the middle and conformer 2 is on the right. WebOct 21, 2024 · Thieno[2,3-d]pyrimidines are a type of pyrimidine structurally fused with thiophene . They can be regarded as bioisosteres of quinazolines and nucleobases which possibly possess similar biological activities as such [ 11 , 12 ].
WebThiophene and its monomethyl derivatives do not undergo coupling with diazonium salts in intermolecular reactions 〈84CHEC-I(4)763〉.Surprisingly, however, it has been found …
WebFeb 2, 2024 · Both thiophene bioisosteres show a slight preference for GluN2B receptors over both σ receptors. The data indicate that the bioisosteric replacement of benzene or substituted benzene rings by a thiophene ring is well tolerated by the NMDA receptor. Furthermore, the benzylic OH moiety seems not to be essential for high GluN2B affinity. … shipchandler marina aeroportoWebJan 10, 2024 · Both thiophene bioisosteres show a slight preference for GluN2B receptors over both σ receptors. The data indicate that the bioisosteric replacement of benzene or … shipchandler monacoWebIn light of the emergence of resistance against the currently available EGFR inhibitors, our study focuses on tackling this problem through the development of dual EGFR/HER2 inhibitors with improved enzymatic affinities. Guided by the binding mode of the marketed dual EGFR/HER2 inhibitor, Lapatinib, we proposed the design of dual EGFR/HER2 … shipchandler mauritaniaWebDec 12, 2024 · Bioisosteres are then defined as any pair of ligands that share similar interaction patterns with their native target protein. Because the selection is directly based on protein–ligand interactions it does not require any pairwise similarity calculation between either ligands or binding sites. shipchandler manilaWebOn the basis of the 6′,7′-dihydrospiro[piperidine-4,4′-thieno[3,2-c]pyran] framework, a series of more than 30 σ ligands with versatile substituents in 1-, 2′-, and 6′-position has been synthesized and pharmacologically evaluated in order to find novel structure–affinity relationships.It was found that a cyclohexylmethyl residue at the piperidine N-atom … shipchandler onlineWebJan 7, 2024 · Benzene, thiophene and pyridine illustrate this concept is shown as Figure 1.[5] A -CH=CH- group in benzene is replaced by the divalent sulfur, -S-, in thiophene and a - ... shipchandler parisWebFeb 1, 2005 · In this paper, we will discuss bioisosterism as a strategy of molecular modification, showing its importance in building a new series of congeners compounds designed as candidate of new drugs,... shipchandler martigues