title: Synthesis and SAR of tetrahydropyrrolo[1,2-b][1,2,5]thiadiazol-2(3H)-one 1,1-dioxide analogues as highly potent selective androgen receptor modulators.
abstract: Replacement of the 3-oxo group of 2-chloro-4-[(7R,7aS)-7-hydroxy-1,3-dioxotetrahydro-1H-pyrrolo[1,2c]imidazol-2(3H)-yl]-3-methylbenzonitrile resulted in a sulfamide series of selective androgen receptor modulator (SARM) agonists.
authors.affiliation: Bristol-Myers Squibb Research and Development, Princeton, NJ 08543-4000, USA. mark.manfredi@bms.com
authors.forename: Mark C
authors.initials: MC
authors.lastname: Manfredi
authors.forename: Yingzhi
authors.initials: Y
authors.lastname: Bi
authors.forename: Alexandra A
authors.initials: AA
authors.lastname: Nirschl
authors.forename: James C
authors.initials: JC
authors.lastname: Sutton
authors.forename: Ramakrishna
authors.initials: R
authors.lastname: Seethala
authors.forename: Rajasree
authors.initials: R
authors.lastname: Golla
authors.forename: Blake C
authors.initials: BC
authors.lastname: Beehler
authors.forename: Paul G
authors.initials: PG
authors.lastname: Sleph
authors.forename: Gary J
authors.initials: GJ
authors.lastname: Grover
authors.forename: Jacek
authors.initials: J
authors.lastname: Ostrowski
authors.forename: Lawrence G
authors.initials: LG
authors.lastname: Hamann
mesh_terms: D000728:Androgens; D000818:Animals; D004305:Dose-Response Relationship, Drug; D008297:Male; D015394:Molecular Structure; D018482:Muscle, Skeletal / Q000187:drug effects / Q000254:growth & development; D011467:Prostate / Q000187:drug effects / Q000254:growth & development; D011485:Protein Binding; D051381:Rats; D011944:Receptors, Androgen / Q000378:metabolism; D013329:Structure-Activity Relationship; D045165:Testosterone Congeners / Q000138:chemical synthesis* / Q000494:pharmacology*; D013830:Thiadiazoles / Q000138:chemical synthesis* / Q000494:pharmacology*
chemical_list: D000728:Androgens; D011944:Receptors, Androgen; D045165:Testosterone Congeners; D013830:Thiadiazoles