17322-91-7

Usage

Uses

Used in Pharmaceutical Drug Development:
1H-PYRROLO[3,2-B]PYRIDIN-5-OL is used as a key intermediate in the synthesis of various pharmaceutical drugs due to its unique structure and biological activity. Its presence in drug molecules can contribute to their efficacy and therapeutic potential.
Used in Organic Synthesis:
In the realm of organic synthesis, 1H-PYRROLO[3,2-B]PYRIDIN-5-OL is utilized as a versatile building block for the preparation of a range of bioactive molecules. Its chemical properties allow for the creation of diverse compounds with potential applications in medicine and other fields.
Used in Medicinal Chemistry Research:
1H-PYRROLO[3,2-B]PYRIDIN-5-OL is employed as a research tool in medicinal chemistry to explore its pharmacological properties and to understand its interactions with biological targets. This research can lead to the discovery of new drugs and therapeutic agents.
Used in Drug Discovery:
1H-PYRROLO[3,2-B]PYRIDIN-5-OL is used in drug discovery processes to identify potential lead compounds with therapeutic value. Its unique structure and biological activity make it a promising candidate for the development of new medications.

Upstream product

• 24509-73-7 1-(1H-pyrrolo[3,2-b]pyridin-1-yl)ethanone 
• 28489-45-4 6-methyl-5-nitropyridin-2-ol 
• 127792-77-2 2-<6-(benzyloxy)-3-nitro-2-pyridyl>acetonitrile 
• 75926-54-4 2-(benzyloxy)-5-nitropyridine 
• 17288-41-4 5-(benzyloxy)pyrrolo<3,2-b>pyridine 

Downstream Products

• 127792-75-0 1,4-dihydro-3-(1,2,3,6-tetrahydro-4-pyridinyl)-5H-pyrrol[3,2-b]pyridin-5-one 
• 514182-83-3 C₁₃H₁₀N₂O 

Relevant academic research and scientific papers

Amide derivatives and application thereof in heart and cerebral vessels

The invention discloses amide derivatives, with a structural general formula (I) shown in the description, wherein R1 is selected from H, OH or CH3; R2 is selected from H, OH or CH3. The amide derivatives disclosed by the invention show favorable bioactivity in an an-giotensin II mediated ApoE mouse model, indicating that the amide derivatives are of positive significance to the prevention and/or treatment of cardiovascular and cerebrovascular diseases and can be further studied in terms of hypertension, hyperlipidemia and/or atherosclerosis.

Amide derivative, and applications thereof in cardiovascular and cerebrovascular diseases

The invention discloses an amide derivative. The structure general formula of the amide derivative is represented by formula I, wherein R1 is selected from H, OH, or CH3, R2 is selected form H, OH, orCH3, and R3 is selected form H, OH, or CH3. The amide derivative possesses excellent biological activity in angiotensin II mediated ApoE mice models. It is shown that the amide derivative possesses active meaning in prevention and/or treatment of cardiovascular and cerebrovascular diseases, and deep research on applications on prevention and treatment of hypertension, hyperlipidemia, and/oratherosclerosis is needed.

Amide type derivative and application thereof to hypertension, hyperlipidemia and atherosclerosis

The invention discloses an amide type derivative. A structural general formula of the amide type derivative is shown as a formula (I): the formula (I) is shown in the description, wherein R1 is selected from H, OH or CH3, R2 is selected from H, OH or CH3, and R3 is selected from H, OH or CH3; the amide type derivative disclosed by the invention has good bioactivity in angiotensin II mediated ApoE-/-mouse model and shows that the amide type derivative disclosed by the invention has positive significance in prevention and/or treatment of cardiovascular and cerebrovascular diseases and can be used for carrying out deeper researches in the aspects of hypertension, hyperlipidemia and/or atherosclerosis.

Amides derivative and application thereof in hypertension, hyperlipidemia and atherosclerosis

The invention discloses an amides derivative. The structural formula of the amides derivative is shown in the formula (I) in the description, wherein R1 is selected from H or OH or CH3, R2 is selectedfrom H or OH or CH3, R3 is selected from H or OH or CH3. The amides derivative shows good bioactivity in an angiotensin II mediated ApoE-/- mouse model, it is shown that the amides derivative has positive significance in prevention and/or treatment of cardiovascular and cerebrovascular diseases, and deeper research can be conducted in the aspects of hypertension, hyperlipidemia and/or atherosclerosis.

Core Replacements in a Potent Series of VEGFR-2 Inhibitors and Their Impact on Potency, Solubility, and hERG

Anti-VEGF therapy has been a clinically validated treatment of age-related macular degeneration (AMD). We have recently reported the discovery of indole based oral VEGFR-2 inhibitors that provide sustained ocular retention and efficacy in models of wet-AMD. We disclose herein the synthesis and the biological evaluation of a series of novel core replacements as an expansion of the reported indole based VEGFR-2 inhibitor series. Addition of heteroatoms to the existing core and/or rearranging the heteroatoms around the 6-5 bicyclic ring structure produced a series of compounds that generally retained good on-target potency and an improved solubility profile. The hERG affinity was proven not be dependent on the change in lipophilicity through alteration of the core structure. A serendipitous discovery led to the identification of a new indole-pyrimidine connectivity: from 5-hydroxy to 6-hydroxyindole with potentially vast implication on the in vitro/in vivo properties of this class of compounds.

Pharmaceutically active 3-(1,2,5,6-tetrahydropyridyl)-pyrrolopyridines

Compounds of the formula STR1 wherein one of A, B, D and E is N and the remaining three atoms are C; R1 and R2 are independently selected from hydrogen and C1 to C6 alkyl; and R3, R4, R5 and R6 are independently selected from hydrogen, halogen, hydroxy, C1 -C6 alkyl, C1 -C8 alkoxy, phenyl-C1 -C6 alkoxy, phenoxy --NR7 R8 wherein R7 and R8 are independently selected from hydrogen, C1 -C8 alkyl, C1 -C6 alkanoyl and COOR9 wherein R9 is hydrogen or C1 -C6 alkyl, cyano, COOR10 wherein R10 is hydrogen or C1 -C6 alkyl, and CONR11 R12 where R10 and R11 are independently selected from hydrogen and C1 -C6 alkyl, and the pharmaceutically acceptable salts thereof. The compounds are useful psychotherapeutics and may be used in treating obesity, depression and disorders wherein aggression is a symptom.

3-(1,2,5,6-Tetrahydropyrid-4-yl)pyrrolo[3,2-b]pyrid-5-one: a potent and selective serotonin (5-HT(1B)) agonist and rotationally restricted phenolic analogue of 5-methoxy-3-(1,2,5,6-tetrahydropyrid-4-yl)indole

The synthesis and in vitro and in vivo characteristics of 3-(1,2,5,6-tetrahydropyrid-4-yl)pyrrolo[3,2-b]pyrid-5-one (1, CP-93,129) are described. This rotationally restricted phenolic analogue of RU-24,969 is a potent (15 nM) and selective (200x vs the 5-

THE SYNTHESIS OF ROTATIONALY RESTRICTED PHENOLIC ANALOG OF 5-METHOXY-3-(1,2,5,6-TETRAHYDROPYRID-4-YL)INDOLE (RU-24,969)

Pyrrolopyrid-5-one represents a rotationally restricted phenolic analog of 5-hydroxyindole.The synthesis of the rotationally restricted phenolic analog of the serotonin agonist, 5-methoxy-3-(1,2,5,6-tetrahydropyrid-4-yl)indole (RU-24,969), is prese