SCOPUS 정보 검색 플랫폼

Volumn 4, Issue 15, 1994, Pages 1855-1860

Structure-activity relationships involving the catechol subunit of rolipram

Author keywords

[No Author keywords available]

Indexed keywords

PHOSPHODIESTERASE; PHOSPHODIESTERASE INHIBITOR; ROLIPRAM; ROLIPRAM DERIVATIVE;

ARTICLE; DRUG SYNTHESIS; ENZYME BINDING; ENZYME INHIBITION; STRUCTURE ACTIVITY RELATION;

EID: 0027966942 PISSN: 0960894X EISSN: None Source Type: Journal
DOI: 10.1016/S0960-894X(01)80384-X Document Type: Article

Times cited : (17)

References (21)

4
- 84908837770
- Bäckström, R.; Honkanen, E.; Raasmaja, A.; Linden, I.-B. Int. Pat. Appl. (PCT) WO 91/16303 (26 Apr 1991).

5
- 84908837769
- Bagli, J.F.; Lombardo, L.J.; Skotnicki, J.S. Eur. Pat. Appl. 0 511 865 A1 (30 Apr 1992).

6
- 84908837768
- Bender, P.E.; Christensen, S.B. Int. Pat. Appl. (PCT) WO 93/07141 (2 Oct 1992).

9
- 84908837767
- 3: C, 64.38; H, 5.40; N, 6.83. Found: C, 64.23; H, 5.39; N, 6.74.

10
- 84908837766
- 3: C, 65.74; H, 5.98; N, 6.39. Found: C, 65.75; H, 6.02; N, 6.40.

11
- 84908837765
- 3: C, 70.31; H, 7.01; N, 5.12. Found: C, 70.28; H, 7.06; N, 5.07.

12
- 84908837764
- i = 26 μM and 〉 100 μM, respectively, demonstrating the requirement that both ether groups be present for significant PDE IV inhibition.

13
- 0027365792
- This minimum-energy rolipram conformation was calculated by semi-empirical (PM3) calculations within SPARTAN (Wavefunction Inc) and is in good agreement with the recently published crystal structure of (+)-1-(4-bromobenzyl)-4-(3-, cyclopentoxy)-4-methoxyphenyl)pyrrolidin-2-one:
- (1993) J. Med. Chem. , vol.36 , pp. 3274
- Baures¹ Eggleston² Erhard³ Cieslinski⁴ Torphy⁵ Christensen⁶

15
- 84908837763
- 3: C, 71.56; H, 6.71; N, 4.91. Found: C, 71.43; H, 6.73; N, 4.93.

16
- 84908837762
- The syntheses of 14 and 15 are reported elsewhere: Stafford, J.A.; Valvano, N.L. J. Org. Chem., in press.

17
- 84908837761
- 2O: C, 71.18; H, 7.72; N, 4.61. Found: C, 71.16; H, 7.67; N, 4.35.

18
- 84908837760
- 2O. The reaction is initiated by the addition of 20 μL of an enzyme solution containing 50 μg/mL of 5′-nucleotidase and hrPDE IV that has been diluted appropriately into [[Truncated]]

21
- 84908837758
- *) performed on systems modelled to mimic 5 and 7, 7-methoxybenzofuran (5′) and 7-methoxy-2,3-dihydrobenzofuran (7′), respectively, confirmed that the dipole vectors are oriented differently. For 5′ the vector coordinates are x=0.93, y=0.0, z=0.43 (μ=1.06 D); for 7′ the vector coordinates are x=0.14, y=−0.79, z=1.18 (μ=1.49 D).

* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.