85514-44-9Relevant academic research and scientific papers
Amidoalkylindoles as Potent and Selective Cannabinoid Type 2 Receptor Agonists with in Vivo Efficacy in a Mouse Model of Multiple Sclerosis
Shi, Ying,Duan, Yan-Hui,Ji, Yue-Yang,Wang, Zhi-Long,Wu, Yan-Ran,Gunosewoyo, Hendra,Xie, Xiao-Yu,Chen, Jian-Zhong,Yang, Fan,Li, Jing,Tang, Jie,Xie, Xin,Yu, Li-Fang
, p. 7067 - 7083 (2017/09/07)
Selective CB2 agonists represent an attractive therapeutic strategy for the treatment of a variety of diseases without psychiatric side effects mediated by the CB1 receptor. We carried out a rational optimization of a black market designer drug SDB-001 that led to the identification of potent and selective CB2 agonists. A 7-methoxy or 7-methylthio substitution at the 3-amidoalkylindoles resulted in potent CB2 antagonists (27 or 28, IC50 = 16-28 nM). Replacement of the amidoalkyls from 3-position to the 2-position of the indole ring dramatically increased the agonist selectivity on the CB2 over CB1 receptor. Particularly, compound 57 displayed a potent agonist activity on the CB2 receptor (EC50 = 114-142 nM) without observable agonist or antagonist activity on the CB1 receptor. Furthermore, 57 significantly alleviated the clinical symptoms and protected the murine central nervous system from immune damage in an experimental autoimmune encephalomyelitis (EAE) mouse model of multiple sclerosis.
Anti-androgenic cyclo and bicyclo alkenes
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, (2008/06/13)
Compounds having the formula (i), (ii) and (iii), STR1 where R is H, alkyl of 1 to 6 carbons, or CO--R 2 where R 2 is alkyl of 1 to 6 carbons; R 1 is H, CH 3, or (CH 2) m --CH 3 ; n is an integer having the values of 2 to 10, m is an integer having the values of 1 to 6, have anti-androgen activity on secondary androgen receptor sites. The compounds are useful for treating mammals, including humans afflicted with acne, male pattern baldness, adhesions and keloids. The compounds are also effective for treating other diseases or conditions which are related to androgen receptors, such as undesirable formation of breast capsules in females after breast augmentation surgery, osteoarthritis and symptoms of Alzheimer''s disease. The compounds also have inhibitory effect on the metabolism of certain microorganisms and fungi of the kind, the metabolism of which is normally known to be controllable by anti-androgen compounds.
Enantiomeric synthesis of 9-hydroxy-(E)-2-decenoic acid, a queen honeybee pheromone
Kandil, Ali A.,Slessor, Keith N.
, p. 1166 - 1168 (2007/10/02)
S-(+)-, R-(-)-, and (+/-)-9-hydroxy-(E)-2-decenoic acid have been synthesized by organocuprate-catalyzed opening of S-(-)-, R-(+)-, and racemic methyl oxiranes.This acid, of unknown chirality, is an important constituent of the honeybee queen's mandibular gland.
