Mahmood, Abid; Ali Shah, Syed Jawad; Iqbal, Jamshed published the artcile< Design and synthesis of adamantane-1-carbonyl thiourea derivatives as potent and selective inhibitors of h-P2X4 and h-P2X7 receptors: An Emerging therapeutic tool for treatment of inflammation and neurological disorders>, Quality Control of 51605-97-1, the main research area is adamantanoyl thiourea preparation SAR receptor inhibitor inflammation docking; Ca(2+) flux assay; Carboxamides; Fura-2 AM dye; Molecular docking studies; P2XR antagonists; Purinergic signaling; Thiourea derivatives.
Adamantane ring has been reported to exhibit significant inhibitory potential towards P2X receptors, especially for P2X7R. Uniqueness of adamantan radicals in synthesized compounds RC(O)NHC(S)NHR1 [R = adamantan-1-yl; R1 = 2-bromo-4-isopropylphenyl, quinolin-8-yl, 3-(dimethylamino)propan-1-yl, etc.] introduced different substitutes to improve potency and selectivity for the P2XR subtypes used. Among synthesized derivatives, RC(O)NHC(S)NHR1 [R = adamantan-1-yl; R1 = 2-bromo-4-isopropylphenyl, quinolin-8-yl] were found to be most potent and selective inhibitors for h-P2X4R and h-P2X7R, resp. Compound RC(O)NHC(S)NHR1 [R = adamantan-1-yl; R1 = 2-bromo-4-isopropylphenyl] was found to be highly selective for h-P2X4R with IC50 ± SEM = 0.04 ± 0.01μM, that is 22 times more potent than BX-430, a standard selective inhibitor of h-P2X4R. Compound RC(O)NHC(S)NHR1 [R = adamantan-1-yl; R1 = quinolin-8-yl] has IC50 ± SEM of 0.073 ± 0.04μM, which is comparable with the known antagonists of h-P2X7R. In silico studies were also conducted to find the type of interactions as well as mode of inhibition. Compound RC(O)NHC(S)NHR1 [R = adamantan-1-yl; R1 = 2-bromo-4-isopropylphenyl, quinolin-8-yl] were studied for mode of inhibition of P2XRs and both were found to be neg. allosteric modulators.
European Journal of Medicinal Chemistry published new progress about Adamantanes Role: PAC (Pharmacological Activity), PRP (Properties), RCT (Reactant), SPN (Synthetic Preparation), THU (Therapeutic Use), BIOL (Biological Study), RACT (Reactant or Reagent), PREP (Preparation), USES (Uses). 51605-97-1 belongs to class bromides-buliding-blocks, and the molecular formula is C9H12BrN, Quality Control of 51605-97-1.
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary