Literature DB >> 17574413

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.

Mark C Manfredi1, Yingzhi Bi, Alexandra A Nirschl, James C Sutton, Ramakrishna Seethala, Rajasree Golla, Blake C Beehler, Paul G Sleph, Gary J Grover, Jacek Ostrowski, Lawrence G Hamann.   

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.

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Year:  2007        PMID： 17574413     DOI： 10.1016/j.bmcl.2007.06.007

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  6 in total

Review 1.  Protective actions of sex steroid hormones in Alzheimer's disease.

Authors:  Christian J Pike; Jenna C Carroll; Emily R Rosario; Anna M Barron
Journal:  Front Neuroendocrinol       Date:  2009-05-07       Impact factor: 8.606

2.  Discovery of the selective androgen receptor modulator MK-0773 using a rational development strategy based on differential transcriptional requirements for androgenic anabolism versus reproductive physiology.

Authors:  Azriel Schmidt; Donald B Kimmel; Chang Bai; Angela Scafonas; Sujane Rutledge; Robert L Vogel; Sheila McElwee-Witmer; Fang Chen; Pascale V Nantermet; Viera Kasparcova; Chih-Tai Leu; Hai-Zhuan Zhang; Mark E Duggan; Michael A Gentile; Paul Hodor; Brenda Pennypacker; Patricia Masarachia; Evan E Opas; Sharon A Adamski; Tara E Cusick; Jiabing Wang; Helen J Mitchell; Yuntae Kim; Thomayant Prueksaritanont; James J Perkins; Robert S Meissner; George D Hartman; Leonard P Freedman; Shun-ichi Harada; William J Ray
Journal:  J Biol Chem       Date:  2010-03-31       Impact factor: 5.157

3.  Evaluation of betulinic acid effects on pain, memory, anxiety, catalepsy, and oxidative stress in animal model of Parkinson's disease.

Authors:  M Abrishamdar; Yaghoob Farbood; A Sarkaki; M Rashno; M Badavi
Journal:  Metab Brain Dis       Date:  2022-06-16       Impact factor: 3.584

Review 4.  Selective androgen receptor modulators as function promoting therapies.

Authors:  Shalender Bhasin; Ravi Jasuja
Journal:  Curr Opin Clin Nutr Metab Care       Date:  2009-05       Impact factor: 4.294

Review 5.  Selective androgen receptor modulators in preclinical and clinical development.

Authors:  Ramesh Narayanan; Michael L Mohler; Casey E Bohl; Duane D Miller; James T Dalton
Journal:  Nucl Recept Signal       Date:  2008-11-26

6.  Molecular targets of androgen signaling that characterize skeletal muscle recovery and regeneration.

Authors:  James G MacKrell; Benjamin C Yaden; Heather Bullock; Keyue Chen; Pamela Shetler; Henry U Bryant; Venkatesh Krishnan
Journal:  Nucl Recept Signal       Date:  2015-10-07
  6 in total

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