110440-68-1Relevant academic research and scientific papers
Synthesis, spectral properties and structure of new novel 3,3'-dibenzoyl-1,1'-(propan-1,3-diyl)-bisthiourea
Aydin, Fatma,Aykac, Dogan,Uenver, Hueseyin,Iskeleli, Nazan Ocak
, p. 381 - 387 (2012)
A new 3,3'-dibenzoyl-1,1'-propan-1,3-diyl)bisthiourea was synthesized by using benzoylisothiocyanate with 1,3-diaminopropane in aprotic solvent. The structure was determinated by means of FT-IR, 1H-NMR, 13C-NMR and mass spectroscopic
Structure-Activity Relationship of Hetarylpropylguanidines Aiming at the Development of Selective Histamine Receptor Ligands?
Pockes, Steffen,Wifling, David,Buschauer, Armin,Elz, Sigurd
, p. 285 - 297 (2019/04/04)
New classes of alkylated hetarylpropylguanidines with different functionality and variation in spacer length were synthesized to determine their behavior at the four histamine receptor (H1R, H2R, H3R, H4R) subtypes. Alkylated guanidines with different terminal functional groups and varied basicity, like amine, guanidine and urea were developed, based on the lead structure SK&F 91486 (2). Furthermore, heteroatomic exchange at the guanidine structure of 2 led to simple analogues of the lead compound. Radioassays at all histamine receptor subtypes were accomplished, as well as organ bath studies at the guinea pig (gp) ileum (gpH1R) and right atrium (gpH2R). Ligands with terminal functionalization led to, partially, highly affine and potent structures (two digit nanomolar), which showed up a bad selectivity profile within the histamine receptor family. While the benzoylurea derivative 144 demonstrated a preference towards the human (h) H3R, S-methylisothiourea analogue 143 obtained high affinity at the hH4R (pKi=8.14) with moderate selectivity. The molecular basis of the latter finding was supported by computational studies.
