118708-36-4Relevant academic research and scientific papers
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)
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.
MONOBACTAM ORGANIC COMPOUNDS FOR THE TREATMENT OF BACTERIAL INFECTIONS
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Paragraph 0888, (2015/11/10)
This invention pertains generally to antibacterial compounds of Formula I, as further described herein, and pharmaceutically acceptable salts and formulations thereof. In certain aspects, the invention pertains to methods of using such compounds to treat infections such as those caused by Gram-negative bacteria.
THIAZOLE DERIVATIVES ACTIVE ON THE CHOLINERGIC SYSTEM, PROCESS FOR OBTENTION AND PHARMACEUTICAL COMPOSITIONS
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, (2008/06/13)
The invention relates to thiazole derivatives corresponding to the general formula: STR1 in which: R 1 and R 2 each independently represent hydrogen; a C 1-C 4 alkyl group; a phenyl group or a phenyl group monosubstituted or polysubstituted by a halogen a
