146097-08-7Relevant academic research and scientific papers
Synthesis, SAR and selectivity of 2-acyl- and 2-cyano-1-hetarylalkyl- guanidines at the four histamine receptor subtypes: A bioisosteric approach
Geyer, Roland,Igel, Patrick,Kaske, Melanie,Elz, Sigurd,Buschauer, Armin
, p. 72 - 81 (2014/01/06)
In the search for potential bioisosteres of the 4-imidazolyl ring in acylguanidines (e.g. UR-AK24), known to possess affinity to several histamine receptor subtypes (HxR, x = 1-4), and cyanoguanidine-type H 4R agonists (e.g. UR-PI376
Synthesis and matrix metalloproteinase-12 inhibitory activity of ageladine A analogs
Ando, Naoki,Terashima, Shiro
experimental part, p. 579 - 596 (2011/06/26)
Synthesis of the 37 ageladine A analogs was accomplished by employing the total synthetic route of natural ageladine A previously explored by us. From the matrix metalloproteinase-12 (MMP-12) inhibitory activity assay carried out using the novel analogs, it appeared evident that the halogen atom at the 2-position of pyrrole ring was essential for the inhibitory activity and that the introduction of a bromine atom into the 4-position of pyrrole ring is very effective for producing potent activity. In addition, exchange of the pyrrole ring to an imidazole ring was extremely effective in increasing activity, and the analog 29 thus obtained was found to show approximately 4 times more potent activity than natural ageladine A.
The design and synthesis of inhibitors of imidazoleglycerol phosphate dehydratase as potential herbicides
Cox,Hawkes,Bellini,Ellis,Barrett,Swanborough,Russell,Walker,Barnes,Knee,Lewis,Davies
, p. 297 - 311 (2007/10/03)
The discovery and exploration of a new class of broad-spectrum postemergent herbicides with a novel mode of action, namely the disruption of histidine biosynthesis via inhibition of imidazoleglycerol phosphate dehydratase (IGPD; E.C. 4.2.1.19), are described. Clear structural similarities between the first member, produced during an attempt to produce analogues of glyphosate, and intermediates in histidine biosynthesis were noted. Several series of targets were designed, to mimic both the enzyme substrate and a putative reaction intermediate, and synthesised. Some examples were found to be both extremely potent inhibitors of the enzyme, having K(i) values as low as 0·3 nM, and phloem-mobile herbicides with levels of weed control similar to those shown by glyphosate. Further logical progress awaits a high-resolution X-ray structure determination of an enzyme-inhibitor complex.
Triazole phosphoric acid derivatives and their use as herbicides
-
, (2008/06/13)
A herbicidal compound of formula (I) STR1 or a salt, tautomer or cyclic derivative thereof; where R1 and R2 are hydrogen and A is an optionally substituted saturated or unsaturated chain or ring of three carbon atoms. Methods for pre
