95494-51-2Relevant articles and documents
Small molecular compound SPAM1 for up-regulating neuropeptide PACAP and receptor PAC1-R thereof and preparation method and application thereof
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Paragraph 0037-0038, (2020/08/25)
The invention discloses a small molecule compound SPAM1 for up-regulating neuropeptide PACAP and receptor PAC1-R thereof and a preparation method and application thereof. The structure of the small molecule compound SPAM1 is as shown in formula (I), and R = none or H20 or HCl; the SPAM1 is small in molecular weight, and can efficiently pass through biological barriers including a blood brain barrier, a blood testis barrier and the like; expression of neurotransmitter/conditioned PACAP secreted by hypothalamus-pituitary gland and a specific receptor PAC1-R of the neurotransmitter/conditioned PACAP acts on downstream glands of a gonad axis and an adrenal axis so that the regulation and control effects of the neurotransmitter/conditioned PACAP are comprehensive; the SPAM1 specifically targetsPAC1-R1, only acts on cells and tissues for naturally expressing a PAC1-R nervous system and an endocrine system, and is relatively small in side effect. Therefore, the SPAM1 will become a novel small-molecule compound medicine for effectively treating and preventing functional aging and disorder of the nervous system, the endocrine system and the immune system which are closely related to the neuropeptide PACAP.
Synthesis and SAR studies of potent H+/K+-ATPase inhibitors of quinazolinone-Schiff's base analogues
Rakesh,Shantharam,Manukumar
, p. 1 - 8 (2016/07/15)
A series of quinazolinone derived Schiff base derivatives 7–36 were synthesized and characterized by analytical and spectroscopic techniques. The synthesized analogues were screened for their in vitro H+/K+-ATPase inhibition. Most of the compounds showed excellent activity, compared to that of omeprazole, a reference drug. In particular, hydroxy and methoxy derivatives 13–24 were the most active compounds possessing a significant increase for different substituents on the benzene ring thus, contributing positively to gastric H+/K+-ATPase inhibition. Preliminary structure-activity relationship revealed that the compounds 13–24 with electron donating moiety (OH, OCH3) were found to be excellent activity and compounds 9–12 and 25–36 with electron withdrawing moiety (Cl, F, NO2 and Br) were found to be least antiulcer agents.