- 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, antimicrobial, and anti-inflammatory activities of acetamido pyrrolyl azoles
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The acetamido pyrrolyl oxazoles/thiazoles/imidazoles were prepared and tested for their antimicrobial and anti-inflammatory activities. The nitro substituted acetamido pyrrolyl thiazole (11f) and pyrrolyl imidazole (12f) exhibited promising antibacterial activity against K. pneumoniae. The compound 12f showed good antifungal activity against P. chrysogenum. The methoxy acetamido pyrrolyl oxazole (10c) displayed potential anti-inflammatory activity.
- Sowmya, Donthamsetty V.,Basha, Shaik Sharafuddin,Devi, Palampalli Uma Maheswari,Lavanyalatha, Yerraguravagari,Padmaja, Adivireddy,Padmavathi, Venkatapuram
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p. 1010 - 1021
(2017/04/13)
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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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- 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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scheme or table
p. 472 - 484
(2011/04/15)
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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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- Method for inhibiting advanced glycosylation of proteins using aminosubstituted imidazoles
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The present invention relates to compositions and methods for inhibiting nonenzymatic cross-linking (protein aging), Accordingly, a composition is disclosed which comprises 2-aminoimidazoles capable of inhibiting the formation of advanced glycosylation endproducts of target proteins by reacting with the carbonyl moiety of the early glycosylation product of such target proteins formed by their initial glycosylation, The method comprises contacting the target protein with the composition, Both industrial and therapeutic applications for the invention are envisioned, as food spoilage and animal protein aging can be treated.
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- Synthesis and Halogenation of Some New 2-Amino-4-substituted Iminazoles and Their Possible Use as Pesticides
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2-Amino-4-substituted iminazoles (1a-k) have been synthesised by condensing various ketones with guanidine using bromine as condensing agent in dry methanol.These have been halogenated to yield the corresponding 5-halogeno derivatives (II, III).Both halogenated and nonhalogenated iminazoles exhibit antifungal activity against Piricularia oryzae (Cav.) and antibacterial activity against the common pathogenic bacteria, Staphy. aureus and Esch. coli.Structure-activity relationship has also been discussed.
- Nath, J. P.,Mahapatra, G. N.
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p. 526 - 528
(2007/10/02)
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