- 4,6-Diphenylpyrimidine Derivatives as Dual Inhibitors of Monoamine Oxidase and Acetylcholinesterase for the Treatment of Alzheimer's Disease
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Alzheimer's disease (AD) is a neurodegenerative disorder with multifactorial pathogenesis. Monoamine oxidase (MAO) and acetylcholinesterase enzymes (AChE) are potential targets for the treatment of AD. A total of 15 new propargyl containing 4,6-diphenylpy
- Kumar, Bhupinder,Dwivedi, Ashish Ranjan,Sarkar, Bibekananda,Gupta, Sukesh Kumar,Krishnamurthy, Sairam,Mantha, Anil K.,Parkash, Jyoti,Kumar, Vinod
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p. 252 - 265
(2019/01/24)
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- Synthesis, characterization and antiamoebic activity of chalcones bearing N -substituted ethanamine tail
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A series of chalcones (4-21) possessing N-substituted ethanamine were synthesized by the aldol condensation reaction of 1-(4-(2-substituted ethoxy)phenyl)ethanones with different aldehydes preceded by the reaction of 2-chloro N-substituted ethanamine hydr
- Leeza Zaidi, Saadia,Mittal, Sonam,Rajala, Maitreyi S.,Avecilla, Fernando,Husain, Mohammad,Azam, Amir
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p. 179 - 189
(2015/06/08)
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- Design and synthesis of 1,3-biarylsulfanyl derivatives as new anti-breast cancer agents
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A new series of 1,3-biarylsulfanyl derivatives (homodibenzyl core motif) have been designed and synthesized as new estrogen receptor ligands by chopping benzothiophene core of raloxifene to engender seco-raloxifene scaffold. All the synthesized compounds were screened for anti-proliferative, anti-osteoporotic, and anti-implantation activity. Compounds (35, 36) having basic amino anti-estrogenic side chain were exhibiting potential anti-proliferative activity in MCF-7, MDA-MB-231 and ishikawa cell lines. Some of the synthesized compounds having homodibenzyl motif (5, 8, 10) have shown moderate anti-osteoporotic activity.
- Kumar, Atul,Tripathi, Vishwa Deepak,Kumar, Promod,Gupta, Lalit Prakash,Akanksha,Trivedi, Ritu,Bid, Hemant,Nayak,Siddiqui, Jawed A.,Chakravarti, Bandana,Saxena, Ruchi,Dwivedi, Anila,Siddiquee,Siddiqui,Konwar, Rituraj,Chattopadhyay, Naibedya
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scheme or table
p. 5409 - 5419
(2011/10/31)
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- 6-Aryl-4-methylsulfanyl-2H-pyran-2-one-3-carbonitriles as PPAR-γ activators
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Various 6-aryl-3-cyano/methoxycarbonyl-4-methylsulfanyl-2H-pyran-2-ones have been synthesized as a potential substitute of 2,4-thiazolidinedione head group to express potent PPAR-γ transactivation response. Some of the screened compounds have shown promis
- Sharon, Ashoke,Pratap, Ramendra,Vatsyayan, Rit,Maulik, Prakas R.,Roy, Uma,Goel, Atul,Ram, Vishnu Ji
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p. 3356 - 3360
(2007/10/03)
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- 3-PHENYL ANALOGS OF TOXOFLAVINE AS KINASE INHIBITORS
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The present invention concerns the compounds of formula (I) the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n represents an integer being 0, 1 or 2; m represents an integer being 0 or 1; R1 represents C I -4alkyl; R2 represents C I -4alkyl; R3 represents CI-4alkyl; or R2 and R3 taken together with the carbon atom to which they are attached form a C3-8cycloalkyl or Het1 wherein said C3-8cycloalkyl or Het1 each independently may optionally be substituted with C1-4alkyloxycarbonyl; R4 represents halo or C I -4alkyloxy; R5 represents C 1-4alkyloxycarbonyl, -O-(mono- or di(C1-4alkyl)aminosulfonyl), CI-4alkyl substituted with one or where possible more substituent being selected from Het3 or NR6R7, C1-4alkyloxy substituted with one or where possible more substituents being selected from amino, Het4or NR8R9; R6 and R7are each independently selected from hydrogen, C I-4alkyl, C I-4alkyloxyC1-4alkyl, -Het5 or CI-4alkyl substituted with one or where possible more substituents being selected from hydroxy, or Het5; R8 and R9 are each independently selected from hydrogen, C,1-4alkyl, -Het7 or mono- or di(C 1-4alkyl)aminosulphonyl; Het3represents a heterocycle selected from piperidinyl, or piperazinyl wherein said monocyclic heterocycles each independently may optionally be substituted with one, or where possible two or three substituents each independently selected from hydroxy, aminosulfonyl, amino, mono-or di(C 1-4 alkyl)aminosulfonyl, hydroxyC 1-4alkyloxyC1-4alkyl or C1-4alkyloxy; Het4represents a heterocycle selected from morpholinyl, piperidinyl or piperazinyl wherein said monocyclic heterocycles each independently may optionally be substituted with one, or where possible two or three substituents each independently selected from C1-4alkyl, C1-4alkyloxycarbonyl or mono- or di(C1-4alkyl)aminosulfonyl; Het5 represents a heterocycle selected from pyridinyl or piperidinyl wherein said monocyclic heterocycles each independently may optionally be substituted with one, or where possible two or three substituents each independently selected from aminosulfonyl, or mono- or di(Cl-4alkyl)aminosulfonyl; Het7 represents piperidinyl.
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- Substituted acrylophenones and related mannich bases as possible spermicides and inhibitors of HIV envelope glycoprotein-CD4 interaction.
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Several appropriately substituted 4-(dialkylamino-alkyl)-substituted-styryl-alkyl ketones or acetophenones were prepared and subjected to the Mannich reaction to yield compounds that would incorporate both alpha,beta-unsaturated keto groups and a substituted aminomethyl function with or without another olefinic moiety at position 4. The spermicidal activity of the prepared compounds was evaluated. Several compounds 2d, 4a and 4e were found to possess spermicidal activity at 0.005% concentration, while compounds 2a, 2c, 2f, 3a and 4b were active at 0.01% concentration. Compounds 2a, 2c, 3a, 4a and 4e also inhibited the interaction between recombinant HIV Env and CD4. Out of these, compound 2c was found to be most active.
- Kumaria, Niharika,Dwivedi, Anil Kumar,Maikhuri, Jagdamba Prasad,Gupta, Gopal,Habib, Saman,Dhar, Janak Dulari,Singh, Satyawan
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p. 855 - 864
(2007/10/03)
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