Zobrazeno 1 - 10
of 33
pro vyhledávání: '"Ming Fai Chan"'
Autor:
Shashidhar N. Rao, Kalyanaraman Ramnarayan, Vitukudi Narayanaiyengar Balaji, Salvatore Profeta, Ming Fai Chan
Publikováno v:
International Journal of Peptide and Protein Research. 45:366-376
As a part of the development of conformational guidelines for the design of metabolically altered peptidomimetics, we present conformational energy calculations on model dipeptide compounds with glycine (Gly), L-alanine (Ala), alpha-aminoisobutyric a
Autor:
Achim H.-P. Krauss, Charles E. Protzman, Licheng Shi, R. M. Burk, R. Chen, Steven W. Andrews, George Sachs, H. T. T. Dinh, Heather A. Krauss, Karen M. Kedzie, A.M. Bogardus, L. J. Kaplan, Michael B. Roof, M. E. Garst, Ming Fai Chan, Larry A. Wheeler, R. A. Ross, John W. Regan, Todd S. Gac, June Chen, Kristen L. Pierce, D.F. Woodward, D. W. Gil
Publikováno v:
British Journal of Pharmacology. 130:1933-1943
Replacement of the carboxylic acid group of PGF(2alpha) with the non-acidic substituents hydroxyl (-OH) or methoxy (-OCH(3)) resulted in an unexpected activity profile. Although PGF(2alpha) 1-OH and PGF(2alpha) 1-OCH(3) exhibited potent contractile e
Autor:
Ilya Okun, Raju Bore Gowda, Chengde Wu, Fiona Stavros, Ming Fai Chan, Rosario Silvestre Castillo
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 7:2093-2098
A series of 2-aryloxycarbonylthiophene-3-sulfonamides were synthesized and evaluated to determine their antagonistic activity at the endothelin receptors. N-(4-chloro-3-methyl-5-isoxazolyl)-2-[(3,4-methylenedioxy)phenoxycarbonyl]thiophene-3-sulfonami
Publikováno v:
Bulletin of the Chemical Society of Japan. 70:293-299
Peptides with conformationally restricted 1-aminocyclopropane-1-carboxylic acid (Acc3) moieties were previously shown to exhibit preference for γ-turn structures in the solution phase and solid phase. We present conformational energy calculations on
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 7:939-944
The potential proteolytic instability of the amide bond present in some ET A selective thiophenesulfonamide endothelin antagonists exemplified by TBC-10708 led us to investigate the replacement of this moiety with stable amide bond surrogates such as
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 7:933-938
The aryloxymethylene group was used as a replacement for an ester or amide bond present in a series of ETA selective endothelin antagonists. The effect of such replacement on the binding affinity is described.
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 6:2651-2656
The synthesis and in vitro binding affinities of a series of thiophenesulfonamides as ETA selective endothelin receptor antagonists is described. The most potent inhibitor displayed an IC50 of 43 nM and 3 μM to ETA and ETB receptors, respectively.
Autor:
Ilya Okun, Ming Fai Chan, Rosario Silvestre Castillo, Fiona Stavros, Raju Bore Gowda, Emily Hwang, Balaji Vitukudi Narayanaiyenga, Adam Kois, Chengde Wu, Erik Verner
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 6:2393-2398
Replacement of the 4-methyl group in a series of N-(3,4-dimethylisoxazolyl)benzenesulfonamide endothelin antagonists with a bromine or chlorine atom resulted in a three- to ten-fold increase in the binding affinity for both the ETA and ETB receptors.
Publikováno v:
Protein & Peptide Letters. 3:31-38
Abstract: We present conformational energy calculations on model compounds contammg 1-amino cycloalkane carboxylic acid with 5- (Acc5 )and 6- (Acc6) membered rings using molecular mechanics methods. The low energy models adopt conformations charact
Publikováno v:
Journal of Structural Biology. 115:267-274
We present conformation energy calculations on the model dipeptide 1-acetylamino- N -methyl-2,5-cyclohexadiene-1-carboxamide (1) and its two derivatives in which the C-2 and C-6 of the cyclohexadiene ring are substituted. The energy calculations have