Discovery of novel series of 2-substituted benzo[d]oxazol-5-amine derivatives as multi-target directed ligands for the treatment of Alzheimer’s disease was written by Gutti, Gopichand;Kakarla, Ramakrishna;Kumar, Devendra;Beohar, Mahima;Ganeshpurkar, Ankit;Kumar, Ashok;Krishnamurthy, Sairam;Singh, Sushil Kumar. And the article was included in European Journal of Medicinal Chemistry in 2019.HPLC of Formula: 3438-16-2 This article mentions the following:
Alzheimer’s disease (AD) is associated with multifactorial neuropathol. conditions, which included cholinergic deficit, amyloid-beta plaques formation, loss of neuronal plasticity and neuronal death. Treating such multifactorial conditions with a single target directed approach was considered to be inadequate. Accordingly, multi-target directed ligand (MTDL) strategy has been evolved as an auspicious approach for the treatment of AD. In light of that, a library of 2-substituted benzo[d]oxazol-5-amine derivatives I [Ar = Ph, pyridin-2-yl, 4-bromophenyl, etc.; n = 0, 1, 2, C(O); X = C, N; Y = N, CH2, O] was designed using the scaffold hopping guided MTDLs strategy, synthesized and evaluated through various in-vitro and in-vivo biol. studies. The optimal compound I [Ar = 4-bromophenyl, n = C(O); X = N, Y = N] exhibited potent inhibitory activities against AChE (IC50 = 0.052 ± 0.010 μM), BuChE (IC50 = 1.085 ± 0.035 μM) and significant amyloid-beta aggregation (20 μM) inhibition. The compound I [Ar = 4-bromophenyl, n = C(O); X = N, Y = N] possessed better blood-brain barrier permeability (Pe = 10.80 ± 0.055 x 10-6 cm s-1) in PAMPA assay and neuro protective properties (40 μM) on SH-SY5Y neuroblastoma cell lines. Furthermore, in-vivo behavioral studies were performed on Y-maze test (scopolamine-induced amnesia model) and Morris water maze test (Aβ1-42 induced ICV rat model). The compound I [Ar = 4-bromophenyl, n = C(O); X = N, Y = N], at a dose of 10 mg/kg oral administration, demonstrated a substantial improvement of the cognitive and special memory impairment. In summary, both in-vitro and in-vivo investigations evidenced that compound I [Ar = 4-bromophenyl, n = C(O); X = N, Y = N] was a potential lead for the discovery of safe and effective disease-modifying agents for AD. In the experiment, the researchers used many compounds, for example, 5-Chloro-2-methoxybenzoic acid (cas: 3438-16-2HPLC of Formula: 3438-16-2).
5-Chloro-2-methoxybenzoic acid (cas: 3438-16-2) belongs to organic chlorides. Chlorination modifies the physical properties of hydrocarbons in several ways. These compounds are typically denser than water due to the higher atomic weight of chlorine versus hydrogen. Alkyl chlorides readily react with amines to give substituted amines. Alkyl chlorides are substituted by softer halides such as the iodide in the Finkelstein reaction.HPLC of Formula: 3438-16-2
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics