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Application of thin-layer chromatographic data in quantitative structure-activity relationship assay of thiazole and benzothiazole derivatives with H1-antihistamine activity. I.
TLDR
The best multivariate relationships useful in predicting the pharmacological activity of thiazole and benzothiazole derivatives were obtained under the condition of experiment with RP2 TLC plates using the developing solvent acetonitrile-methanol-buffer (40:40:20, v/v). Expand
Non-Imidazole Histamine H3 Ligands. Part VII. Synthesis, In Vitro and In Vivo Characterization of 5-Substituted-2-thiazol-4-n-propylpiperazines
TLDR
SAR studies on novel non-imidazole, 5-substituted-2-thiazol-4-n-propyl-piperazines 3 showed that the most active compound 3a possessed a weak competitive H1-antagonistic activity, so compound ADS-531 was chosen for further evaluation for its affinity to the recombinant rat and human histamine H3 receptors. Expand
Non‐Imidazole Histamine H3 Ligands, Part 2: New 2‐Substituted Benzothiazoles as Histamine H3 Antagonists
TLDR
Lipophilic and not‐too‐bulky substituents like n‐propyl attached to the nitrogen at the piperazine or piperidine ring lead to potent H3 receptor antagonists with pA2 values ranging from 7.0 to 7.2. Expand
Non-imidazole histamine H3 ligands. Part I. Synthesis of 2-(1-piperazinyl)- and 2-(hexahydro-1H-1,4-diazepin-1-yl)benzothiazole derivatives as H3-antagonists with H1 blocking activities.
TLDR
New 2-(1-Piperazinyl)- and 2-(hexahydro-1H-1,4-diazepin-1-yl)benzothiazoles were prepared and tested as H1- and H3-receptor antagonists and showed weak H2-antagonistic activity and 4-phenylalkyl substitution, regardless of the different physicochemical properties of the para substituents at the phenyl ring. Expand
Histamine H1 receptor ligands. Part I. Novel thiazol-4-ylethanamine derivatives: synthesis and in vitro pharmacology.
TLDR
A series of 2-substituted thiazol-4-ylethanamines have been synthesized and tested for their histaminergic H1-receptor activities, and the compounds with 2-phenyl substitution showed weak H 1-agonistic activity. Expand
Loratadine analogues as MAGL inhibitors.
TLDR
A novel dual-acting pharmacological tool possessing both MAGL-inhibitory and antihistaminergic activities is found, which is found to be a potent and reversible inhibitor of human recombinant MAGL. Expand
Non-imidazole histamine H3 ligands. Part III. New 4-n-propylpiperazines as non-imidazole histamine H3-antagonists.
TLDR
By comparison of homologous pairs the thiazolo derivatives have slightly higher activity than their oxazolo analogues, and the most potent compound is the 1-thiazolo[4,5-c]pyridine)-4-n-propylpiperazine. Expand
Optically active analogues of ebastine: synthesis and effect of chirality on their antihistaminic and antimuscarinic activity.
TLDR
It was found that introduction of the benzhydryl chiral center yielded significant stereoselectivity for both antihistaminic and antimuscarinic activities. Expand
Histamine H1 receptor ligands: part II. Synthesis and in vitro pharmacology of 2-[2-(phenylamino)thiazol-4-yl]ethanamine and 2-(2-benzhydrylthiazol-4-yl)ethanamine derivatives.
TLDR
New 2-phenylamino substitution with meta-halide substituents at the phenyl ring and benzhydryl groups of classic antihistamines yielded compounds that exhibited slightly improved H1-antagonistic activity. Expand
Search for multifunctional agents against Alzheimer's disease among non-imidazole histamine H3 receptor ligands. In vitro and in vivo pharmacological evaluation and computational studies of
TLDR
The most promising compound, A12, chemically methyl(4-phenylbutyl){2-[2-(4-propylpiperazin-1-yl)-1,3-thiazol-5-yl]ethyl}amine, possesses good balanced multifunctional profile with potency toward studied targets - H3 antagonist activity and inhibitory activity against both AChE and BuChE. Expand
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