volume 11 issue 23 pages 3035-3039

Beta 3 agonists. Part 1: evolution from inception to BMS-194449

W.N. Washburn 1
P.M. Sher 1
K.M. Poss 1
R.N. Girotra 1
P. J. McCann 1
A.V. Gavai 1
A.B. Mikkilineni 1
Arvind Mathur 1
P. Cheng 1
T.C. Dejneka 1
C. Q. Sun 1
Tao Wang 1
T.W. Harper 1
A. Russell 1
D.A. Slusarchyk 1
S. Skwish 1
G. E. Allen 1
D.E. Hillyer 1
B H Frohlich 1
B.E. Abboa-Offei 1
M. cap 1
T L Waldron 1
R. P. George 1
B Tesfamariam 1
C.P. Ciosek 1
D. Ryono 1
D. A. Young 1
K E Dickinson 1
A A Seymour 1
Cynthia Arbeeny 1
R E Gregg 1
Publication typeJournal Article
Publication date2001-12-01
scimago Q2
wos Q2
SJR0.472
CiteScore5.1
Impact factor2.2
ISSN0960894X, 14643405
Organic Chemistry
Drug Discovery
Biochemistry
Molecular Biology
Pharmaceutical Science
Clinical Biochemistry
Molecular Medicine
Abstract
Screening of the BMS collection identified 4-hydroxy-3-methylsulfonanilidoethanolamines as full beta 3 agonists. Substitution of the ethanolamine nitrogen with a benzyl group bearing a para hydrogen bond acceptor promoted beta(3) selectivity. SAR elucidation established that highly selective beta(3) agonists were generated upon substitution of C(alpha) with either benzyl to form (R)-1,2-diarylethylamines or with aryl to generate 1,1-diarylmethylamines. This latter subset yielded a clinical candidate, BMS-194449 (35).(1)
Found 
Found 

Top-30

Journals

1
2
3
4
5
6
7
Bioorganic and Medicinal Chemistry Letters
7 publications, 38.89%
Organic and Biomolecular Chemistry
2 publications, 11.11%
Journal of Medicinal Chemistry
1 publication, 5.56%
Journal of Combinatorial Chemistry
1 publication, 5.56%
Drug Discovery Today
1 publication, 5.56%
Current Opinion in Chemical Biology
1 publication, 5.56%
Medicinal Chemistry Research
1 publication, 5.56%
Bioorganic and Medicinal Chemistry
1 publication, 5.56%
Progress in Medicinal Chemistry
1 publication, 5.56%
1
2
3
4
5
6
7

Publishers

2
4
6
8
10
12
Elsevier
11 publications, 61.11%
American Chemical Society (ACS)
2 publications, 11.11%
Royal Society of Chemistry (RSC)
2 publications, 11.11%
Springer Nature
1 publication, 5.56%
2
4
6
8
10
12
  • We do not take into account publications without a DOI.
  • Statistics recalculated weekly.

Are you a researcher?

Create a profile to get free access to personal recommendations for colleagues and new articles.
Metrics
18
Share
Cite this
GOST |
Cite this
GOST Copy
Washburn W. et al. Beta 3 agonists. Part 1: evolution from inception to BMS-194449 // Bioorganic and Medicinal Chemistry Letters. 2001. Vol. 11. No. 23. pp. 3035-3039.
GOST all authors (up to 50) Copy
Washburn W., Sher P., Poss K., Girotra R., McCann P. J., Gavai A., Mikkilineni A., Mathur A., Cheng P., Dejneka T., Sun C. Q., Wang T., Harper T., Russell A., Slusarchyk D., Skwish S., Allen G. E., Hillyer D., Frohlich B. H., Abboa-Offei B., cap M., Waldron T. L., George R. P., Tesfamariam B., Ciosek C., Ryono D., Young D. A., Dickinson K. E., Seymour A. A., Arbeeny C., Gregg R. E. Beta 3 agonists. Part 1: evolution from inception to BMS-194449 // Bioorganic and Medicinal Chemistry Letters. 2001. Vol. 11. No. 23. pp. 3035-3039.
RIS |
Cite this
RIS Copy
TY - JOUR
DO - 10.1016/S0960-894X(01)00628-X
UR - https://doi.org/10.1016/S0960-894X(01)00628-X
TI - Beta 3 agonists. Part 1: evolution from inception to BMS-194449
T2 - Bioorganic and Medicinal Chemistry Letters
AU - Washburn, W.N.
AU - Sher, P.M.
AU - Poss, K.M.
AU - Girotra, R.N.
AU - McCann, P. J.
AU - Gavai, A.V.
AU - Mikkilineni, A.B.
AU - Mathur, Arvind
AU - Cheng, P.
AU - Dejneka, T.C.
AU - Sun, C. Q.
AU - Wang, Tao
AU - Harper, T.W.
AU - Russell, A.
AU - Slusarchyk, D.A.
AU - Skwish, S.
AU - Allen, G. E.
AU - Hillyer, D.E.
AU - Frohlich, B H
AU - Abboa-Offei, B.E.
AU - cap, M.
AU - Waldron, T L
AU - George, R. P.
AU - Tesfamariam, B
AU - Ciosek, C.P.
AU - Ryono, D.
AU - Young, D. A.
AU - Dickinson, K E
AU - Seymour, A A
AU - Arbeeny, Cynthia
AU - Gregg, R E
PY - 2001
DA - 2001/12/01
PB - Elsevier
SP - 3035-3039
IS - 23
VL - 11
PMID - 11714605
SN - 0960-894X
SN - 1464-3405
ER -
BibTex |
Cite this
BibTex (up to 50 authors) Copy
@article{2001_Washburn,
author = {W.N. Washburn and P.M. Sher and K.M. Poss and R.N. Girotra and P. J. McCann and A.V. Gavai and A.B. Mikkilineni and Arvind Mathur and P. Cheng and T.C. Dejneka and C. Q. Sun and Tao Wang and T.W. Harper and A. Russell and D.A. Slusarchyk and S. Skwish and G. E. Allen and D.E. Hillyer and B H Frohlich and B.E. Abboa-Offei and M. cap and T L Waldron and R. P. George and B Tesfamariam and C.P. Ciosek and D. Ryono and D. A. Young and K E Dickinson and A A Seymour and Cynthia Arbeeny and R E Gregg},
title = {Beta 3 agonists. Part 1: evolution from inception to BMS-194449},
journal = {Bioorganic and Medicinal Chemistry Letters},
year = {2001},
volume = {11},
publisher = {Elsevier},
month = {dec},
url = {https://doi.org/10.1016/S0960-894X(01)00628-X},
number = {23},
pages = {3035--3039},
doi = {10.1016/S0960-894X(01)00628-X}
}
MLA
Cite this
MLA Copy
Washburn, W.N., et al. “Beta 3 agonists. Part 1: evolution from inception to BMS-194449.” Bioorganic and Medicinal Chemistry Letters, vol. 11, no. 23, Dec. 2001, pp. 3035-3039. https://doi.org/10.1016/S0960-894X(01)00628-X.