View source for Chemistry:CD38-IN-78c

{{Short description|Chemical compound}}
{{Drugbox
| IUPAC_name = 4-{[(1R,4R)-4-(2-methoxyethoxy)cyclohexyl]amino}-1-methyl-6-(1,3-thiazol-5-yl)quinolin-2-one
| image = CD38-IN-78c Structure.svg
<!--Clinical data-->
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| legal_US = 
| legal_status = 

<!--Pharmacokinetic data-->
| bioavailability =  
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<!--Identifiers-->
| CAS_number = 1700637-55-3
| PubChem = 118736856
| UNII = 
| ChemSpiderID = 
| DrugBank = 

<!--Chemical data-->
| C=22 | H=27 | N=3 | O=3 | S=1 
| SMILES = CN1C2=C(C=C(C=C2)C3=CN=CS3)C(=CC1=O)NC4CCC(CC4)OCCOC
| StdInChI=1S/C22H27N3O3S/c1-25-20-8-3-15(21-13-23-14-29-21)11-18(20)19(12-22(25)26)24-16-4-6-17(7-5-16)28-10-9-27-2/h3,8,11-14,16-17,24H,4-7,9-10H2,1-2H3
| StdInChIKey = VJQALSOBHVEJQM-UHFFFAOYSA-N
}}

'''CD38-IN-78c''' is a drug which acts as a potent and selective [[Biology:Enzyme inhibitor|inhibitor]] of the [[Chemistry:Glycoprotein|glycoprotein]] enzyme [[Biology:CD38|CD38]].<ref name="pmid25828863">{{cite journal | vauthors = Haffner CD, Becherer JD, Boros EE, Cadilla R, Carpenter T, Cowan D, Deaton DN, Guo Y, Harrington W, Henke BR, Jeune MR, Kaldor I, Milliken N, Petrov KG, Preugschat F, Schulte C, Shearer BG, Shearer T, Smalley TL, Stewart EL, Stuart JD, Ulrich JC | display-authors = 6 | title = Discovery, Synthesis, and Biological Evaluation of Thiazoloquin(az)olin(on)es as Potent CD38 Inhibitors | journal = Journal of Medicinal Chemistry | volume = 58 | issue = 8 | pages = 3548–71 | date = April 2015 | pmid = 25828863 | doi = 10.1021/jm502009h | s2cid = 43192793 }}</ref> In animal studies it boosts levels of [[Chemistry:Nicotinamide adenine dinucleotide|nicotinamide adenine dinucleotide]] (NAD+) in tissues via inhibition of CD38 mediated breakdown of nicotinamide riboside (NR) and [[Chemistry:Nicotinamide mononucleotide|nicotinamide mononucleotide]] (NMN), and has been shown to ameliorate metabolic dysfunction associated with the aging process.<ref>{{cite journal | vauthors = Tarragó MG, Chini CC, Kanamori KS, Warner GM, Caride A, de Oliveira GC, Rud M, Samani A, Hein KZ, Huang R, Jurk D, Cho DS, Boslett JJ, Miller JD, Zweier JL, Passos JF, Doles JD, Becherer DJ, Chini EN | title = A Potent and Specific CD38 Inhibitor Ameliorates Age-Related Metabolic Dysfunction by Reversing Tissue NAD+ Decline | journal = Cell Metabolism | volume = 27 | issue = 5 | pages = 1081–1095.e10 | date = May 2018 | pmid = 29719225 | pmc = 5935140 | doi = 10.1016/j.cmet.2018.03.016 }}</ref> It also has potential therapeutic application in the treatment of [[Medicine:Asthma|asthma]].<ref name="pmid27939939">{{cite journal | vauthors = Deshpande DA, Guedes AG, Lund FE, Kannan MS | title = CD38 in the pathogenesis of allergic airway disease: Potential therapeutic targets | journal = Pharmacology & Therapeutics | volume = 172 | pages = 116–126 | date=2017 | doi = 10.1016/j.pharmthera.2016.12.002 | pmc =5346344 | pmid = 27939939}}</ref>

== References ==
{{Reflist}}


[[Category:Enzyme inhibitors]]

{{Sourceattribution|CD38-IN-78c}}