- Structure-activity relationships of antitubercular nitroimidazoles. 2. determinants of aerobic activity and quantitative structure-activity relationships
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The (S)-2-nitro-6-substituted 6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazines have been extensively explored for their potential use as new antituberculars based on their excellent bactericidal properties on aerobic whole cells of Mycobacterium tuberculosis. A
- Kim, Pilho,Kang, Sunhee,Boshoff, Helena I.,Jiricek, Jan,Collins, Margaret,Singh, Ramandeep,Manjunatha, Ujjini H.,Niyomrattanakit, Pornwaratt,Zhang, Liang,Goodwin, Michael,Dick, Thomas,Keller, Thomas H.,Dowd, Cynthia S.,Barry III, Clifton E.
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experimental part
p. 1329 - 1344
(2009/12/07)
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- 5,6,7,8-TETRAHYDRO-IMIDAZO[1,5-A]PYRAZINE DERIVATIVES
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The invention relates to 5,6,7,8-tetrahydro-imidazo[1,5-a]pyrazine derivatives of formula (I),wherein X represents CH2 or O; R1 represents a phenyl group, which group is independently mono-, di-, or tri-substituted wherein the substituents are independently selected from the group consisting of (C1-4)alkyl, (C1-4)alkoxy, halogen, cyano, trifluoromethoxy and trifluoromethyl; R2 represents (C1-4)alkyl, (C1-4)alkoxy, (C2-4)alkenyl, halogen, cyano, hydroxymethyl, trifluoromethyl, C(O)NR5R6 or cyclopropyl; R3 represents (C1-4)alkyl, (C1-4)alkoxy-methyl or halogen; R4 represents (C1-4)alkyl; R5 represents hydrogen or (C1-4)alkyl; and R6 represents hydrogen or (C1-4)alkyl. The invention also relates to pharmaceutically acceptable salts of such compounds; and to the use of such compounds as medicaments; especially as orexin receptor antagonists.
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Page/Page column 56
(2008/12/06)
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