- Synthesis, Molecular Properties Prediction and Antimicrobial Activity of Imidazolyl Schiff Bases, Triazoles and Azetidinones
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Benzylidenehydrazinyl imidazoles (3) are prepared from 2-hydrazinyl imidazoles (2) on treatment with hydrazine. The imine functionality in 3 is utilized to develop 5′-aryl-N-(4-aryl-1H-imidazol-2-yl)-1H-1,2,3-triazol-1-amines (5) by 1,3-dipolar cycloaddition of diazomethane followed by aromatization with I2 in DMSO. Compounds 3 are also explored to prepare 4′-aryl-1-(4-aryl-1H-imidazol-2-ylamino)-3-chloroazetidin-2-ones (6) on treatment with chloroacetyl chloride. The Molinspiration calculations predicted that 3, 5 and 6 have molecular hydrophobicity, conformational flexibility, good intestinal absorption and bioactivity scores. The chloro, bromo and nitro substituted imidazolyl azetidinones (6c, 6d, 6f) and nitro substituted imidazolyl triazole (5f) exhibited excellent antibacterial activity on B. subtilis, whereas chloro and nitro substituted imidazolyl triazoles (5c, 5f) showed prominent antifungal activity on A. niger.
- Rekha, Tamatam,Nagarjuna, Ummadi,Padmaja, Adivireddy,Padmavathi, Venkatapuram
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- Fragment-Based Approach to Targeting Inosine-5′-monophosphate Dehydrogenase (IMPDH) from Mycobacterium tuberculosis
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Tuberculosis (TB) remains a major cause of mortality worldwide, and improved treatments are needed to combat emergence of drug resistance. Inosine 5′-monophosphate dehydrogenase (IMPDH), a crucial enzyme required for de novo synthesis of guanine nucleotid
- Trapero, Ana,Pacitto, Angela,Singh, Vinayak,Sabbah, Mohamad,Coyne, Anthony G.,Mizrahi, Valerie,Blundell, Tom L.,Ascher, David B.,Abell, Chris
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p. 2806 - 2822
(2018/04/23)
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- Synthesis, Characterization, and Antioxidant Activity of a New Class of Amido linked Azolyl Thiophenes
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A new class of amido linked azolyl thiophenes was prepared from the synthetic intermediates azolyl amines and 5-chlorothiophene-2-carbonyl chloride adopting conventional and ultrasonication methodologies. It was observed that the reaction took place in shorter reaction times with higher yields under ultrasonication. The structures of the synthesized compounds were characterized by spectral parameters and also tested for antioxidant activity. Among all the tested compounds, methoxy substituted oxazolyl thiophene carboxamide (8c) displayed promising antioxidant activity. Besides, the electron donating groups on the phenyl ring enhanced the antioxidant activity when compared with the electron withdrawing groups.
- Thatha, Sreenivasulu,Ummadi, Nagarjuna,Venkatapuram, Padmavathi,Adivireddy, Padmaja
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p. 1410 - 1418
(2018/06/20)
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- Synthesis and Antimicrobial Activity of Azolyl Pyrimidines
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A new class of azolyl pyrimidines linked by diamino sulfone moiety was prepared and studied their antimicrobial activity. Chloro-substituted and nitro-substituted thiazolyl pyrimidines (9c and 9e) showed excellent antibacterial activity against Bacillus subtilis, while imidazolyl pyrimidines (10c and 10e) exhibited promising antifungal activity against Aspergillus niger.
- Butta, Ragavendra,Donthamsetty V, Sowmya,Adivireddy, Padmaja,Venkatapuram, Padmavathi
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p. 524 - 530
(2017/02/03)
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- Structure-activity relationship of 4(5)-aryl-2-amino-1 H -imidazoles, N 1-substituted 2-aminoimidazoles and imidazo[1,2- a ]pyrimidinium salts as inhibitors of biofilm formation by salmonella typhimurium and pseudomonas aeruginosa
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A library of 112 4(5)-aryl-2-amino-1H-imidazoles, 4,5-diphenyl-2-amino-1H- imidazoles, and N1-substituted 4(5)-phenyl-2-aminoimidazoles was synthesized and tested for the antagonistic effect against biofilm formation by Salmonella Typhimurium and Pseudomo
- Steenackers, Hans P. L.,Ermolatev, Denis S.,Savaliya, Bharat,De Weerdt, Ami,De Coster, David,Shah, Anamik,Van Der Eycken, Erik V.,De Vos, Dirk E.,Vanderleyden, Jozef,De Keersmaecker, Sigrid C. J.
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p. 472 - 484
(2011/04/15)
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- COMPOUNDS, COMPOSITIONS AND METHODS FOR CONTROLLING BIOFILMS
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This invention relates to substituted 2-aminoimidazoles and their imidazo[1,2- a]pyrimidinium salts precursors being active against biofilm formation. The present invention also relates to antimicrobial compositions comprising a microbial biofilm formatio
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Page/Page column 29
(2011/07/30)
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- Microwave-assisted synthesis of substituted 2-amino-1H-imidazoles from imidazo[1,2-a]pyrimidines
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An efficient method for the synthesis of mono- and disubstituted 2-amino-1H-imidazoles via microwave-assisted hydrazinolysis of substituted imidazo[1,2-a]pyrimidines is reported. This protocol avoids strong acidic conditions and is superior to the classic
- Ermolat'ev,Svidritsky,Babaev,Van der Eycken
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supporting information; experimental part
p. 5218 - 5220
(2009/12/06)
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