- Synthesis and evaluation of novel imidazo[4,5-: C] pyridine derivatives as antimycobacterial agents against Mycobacterium tuberculosis
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The current study involves the synthesis of novel imidazo[4,5-c]pyridine derivatives (IPD) containing amide/urea/sulfonamide. The synthesized compounds were evaluated for in vitro and in vivo antimycobacterial activities against Mycobacterium tuberculosis. The pharmacological activities were determined by the objective to better understand their structure-activity relationship (SAR) for their in vitro antimycobacterial activity against M. tuberculosis. Some synthesized compounds showed significant activity against M. tuberculosis based on the agar dilution method. Among the forty-one compounds screened, compounds 21, 22 and 23 were found to be the most active compounds against M. tuberculosis. In the in vivo animal model, 21, 22 and 23 decreased the bacterial load in lung and spleen tissues at the dose of 50 mg kg-1 body weight.
- Madaiah, Malavalli,Prashanth, Maralekere K.,Revanasiddappa, Hosakere D.,Veeresh, Bantal
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p. 9194 - 9204
(2016/11/11)
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- ALKYNYL ALCOHOLS AND METHODS OF USE
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The invention relates to compounds of Formula (0): wherein A1-A8, R4 and R5 each has the meaning as described herein. Compounds of Formula (0) and pharmaceutical compositions thereof are useful in the treatment of diseases and disorders in which undesired or over-activation of NF-kB signaling is observed.
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Paragraph 0557; 0558
(2015/03/04)
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- ALKYNYL ALCOHOLS AND METHODS OF USE
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The invention relates to compounds of Formula (0): wherein A1-A8, R4 and R5 each has the meaning as described herein. Compounds of Formula (0) and pharmaceutical compositions thereof are useful in the treatment of diseases and disorders in which undesired or over-activation of NF-kB signaling is observed.
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Page/Page column 138; 139
(2015/03/13)
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- Synthesis, initial SAR and biological evaluation of 1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine derived inhibitors of IκB kinase
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A new series of tricyclic-based inhibitors of IKK have been derived from an earlier lead compound. The synthesis and structure-activity relationships (SAR) are described. Compound 4k inhibited TNF production in rats stimulated with LPS.
- Kempson, James,Guo, Junqing,Das, Jagabandhu,Moquin, Robert V.,Spergel, Steven H.,Watterson, Scott H.,Langevine, Charles M.,Dyckman, Alaric J.,Pattoli, Mark,Burke, James R.,Yang, XiaoXia,Gillooly, Kathleen M.,McIntyre, Kim W.,Chen, Laishun,Dodd, John H.,McKinnon, Murray,Barrish, Joel C.,Pitts, William J.
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scheme or table
p. 2646 - 2649
(2009/12/31)
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- 1, 6 -DIHYDRO- 1,3, 5, 6-TETRAAZA-AS-INDACENE BASED TRICYCLIC COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS COMPRISING SAME AS INHIBITORS OF IKK ENZYME ACTIVITY
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The present invention provides for tricyclic compounds having the formula (I) wherein R1, R2, R5, R6, R7, and R8 are as described herein. The present invention further provides pharmaceutical compositions comprising such compounds, as well as the use of such compounds for treating inflammatory and immune diseases.
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Page/Page column 74
(2010/11/24)
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- 8H-IMIDAZO[4,5-D]THIAZOLO[4,5-B]PYRIDINE BASED TRICYCLIC COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS COMPRISING SAME
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The present invention provides for thiazolopyridine-based tricyclic compounds having the formula (I) wherein R1, R2, R5 and R6 are as described herein. The present invention further provides pharmaceutical compo
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Page/Page column 59
(2008/06/13)
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