Safety of 4-Methoxybenzaldehyde. Authors Khoramjouy, M; Rezaee, E; Khoshnevis, A; Nazari, M; Nematpour, M; Shahhosseini, S; Tabatabai, SA; Faizi, M in ACADEMIC PRESS INC ELSEVIER SCIENCE published article about in [Khoramjouy, Mona; Faizi, Mehrdad] Shahid Beheshti Univ Med Sci, Sch Pharm, Dept Pharmacol & Toxicol, Tehran, Iran; [Rezaee, Elham; Khoshnevis, Afshan; Nazari, Maryam; Nematpour, Manijeh; Shahhosseini, Soraya; Tabatabai, Sayyed Abbas] Shahid Beheshti Univ Med Sci, Sch Pharm, Dept Pharmaceut Chem, Tehran, Iran in 2021, Cited 48. The Name is 4-Methoxybenzaldehyde. Through research, I have a further understanding and discovery of 123-11-5
Benzodiazepines (BZDs) have been widely used in neurological disorders such as insomnia, anxiety, and epilepsy. The use of classical BZDs, e.g., diazepam, has been limited due to adverse effects such as interaction with alcohol, ataxia, amnesia, psychological and physical dependence, and tolerance. In the quest for new benzodiazepine agonists with more selectivity and low adverse effects, novel derivatives of 4,6-diphenylpyrimidin-2-ol were designed, synthesized, and evaluated. In this series, compound 2, 4-(2-(benzyloxy)phenyl)-6-(4-fluorophenyl) pyrimidin-2-ol, was the most potent analogue in radioligand binding assay with an IC50 value of 19 nM compared to zolpidem (IC50 = 48 nM), a nonbenzodiazepine central BZD receptor (CBR) agonist. Some compounds with a variety of affinities in radioligand receptor binding assay were selected for in vivo evaluations. Compound 3 (IC50 = 25 nM), which possessed chlorine instead of fluorine in position 4 of the phenyl ring, exhibited an excellent ED50 value in most in vivo tests. Proper sedative-hypnotic effects, potent anticonvulsant activity, appropriate antianxiety effect, and no memory impairment probably served compound 3, a desirable candidate as a benzodiazepine agonist. The pharmacological effects of compound 3 were antagonized by flumazenil, a selective BZD receptor antagonist, confirming the BZD receptors? involvement in the biological effects of the novel ligand.
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Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles