- Synthesis and biological evaluation of novel aryloxyacetic acid hydrazide derivatives as anticancer agents
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In our continuing search for new anticancer agents, herein we report the synthesis of 2-(4-chloro-3-methylphenoxy)-N'-[(aryl)methylidene]acetohydrazides 3a–j and the evaluation of their anticancer activities on cell viability, morphological changes and ca
- ?enkarde?, Sevil,Erdo?an, ?mer,?evik, ?zge,Kü?ükgüzel, ?. Güniz
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p. 2634 - 2643
(2021/07/16)
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- Synthesis and xanthine oxidase inhibitory activity of 7-methyl-2- (phenoxymethyl)-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one derivatives
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An elevated level of blood uric acid (hyperuricemia) is the underlying cause of gout. Xanthine oxidase is the key enzyme that catalyzes the oxidation of hypoxanthine to xanthine and then to uric acid. Allopurinol, a widely used xanthine oxidase inhibitor is the most commonly used drug to treat gout. However, a small but significant portion of the population suffers from adverse effects of allopurinol that includes gastrointestinal upset, skin rashes and hypersensitivity reactions. Moreover, an elevated level of uric acid is considered as an independent risk factor for cardiovascular diseases. Therefore use of allopurinol-like drugs with minimum side effects is the ideal drug of choice against gout. In this study, we report the synthesis of a series of pyrimidin-5-one analogues as effective and a new class of xanthine oxidase inhibitors. All the synthesized pyrimidin-5-one analogues are characterized by spectroscopic techniques and elemental analysis. Four (6a, 6b, 6d and 6f) out of 20 synthesized molecules in this class showed good inhibition against three different sources of xanthine oxidase, which were more potent than allopurinol based on their respective IC50 values. Molecular modeling and docking studies revealed that the molecule 6a has very good interactions with the Molybdenum-Oxygen-Sulfur (MOS) complex a key component in xanthine oxidase. These results highlight the identification of a new class of xanthine oxidase inhibitors that have potential to be more efficacious, than allopurinol, to treat gout and possibly against cardiovascular diseases.
- Sathisha,Khanum, Shaukath A.,Chandra, J.N. Narendra Sharath,Ayisha,Balaji,Marathe, Gopal K.,Gopal, Shubha,Rangappa
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p. 211 - 220
(2011/03/17)
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- Synthesis, characterization and antimicrobial evaluation of novel imines and thiazolidinones
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2-(4-Chloro-3-methylphenoxy)acetohydrazide (2) derived from ethyl 2-(4-chloro-3-methylphenoxy) acetate (1) was reacted with different aromatic aldehydes to yield N-(substituted benzylidiene)-2-(4-chloro-3- methylphenoxy)acetamide (3a-e). Cyclization of compound (3a-e) with thioglycolic acid yielded 2-(4-chloro- 3-methylphenoxy)-N-(4-oxo-2-arylthiazolidin-3-yl) acetamide (4a-e). The newly synthesized compounds were characterized on the basis of spectral studies and evaluated for antibacterial and antifungal activities.
- Fuloria, Neeraj Kumar,Singh, Vijender,Yar, Mohammad Shahar,Ali, Mohammed
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experimental part
p. 141 - 146
(2009/06/28)
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- Synthesis, Characterization, Spectral and Antifungal Properties of Some 5-Substituted-1,3,4-oxadiazole-2-thiones and Their Mannich Bases
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A series of 5-substituted aryloxymethyl-1,3,4-oxadiazole-2-thione (3a-e) and their Mannich bases 4-8 are synthesized and subjected to fungitoxic screening.The structures of these compounds are established on the basis of elemental analysis 1H-n.m.r. and mass spectral data.The mass spectral fragmentation pathways of these compounds are discussed.
- Holla, B. Shivarama,Kalluraya, Balakrishna,Nath, S. C.
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p. 549 - 557
(2007/10/02)
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- Synthesis and Biological Activity of 3-Pentadecylaryloxyacetic Acids, Their Hydrazides and Cyclic Derivatives: Oxadiazoles and Pyrroles
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Several 3-pentadecylaryloxyacetic acids (III), their hydrazides (IV), 2-amino-5-(3'-pentadecylaryloxymethyl)-1,3,4-oxadiazoles (V) and 1-(3'-pentadecylaryloxyacetamido)-2,5-dimethylpyrroles (VI) have been synthesised and evaluated for their biological activity.Some of the compounds exhibit strong antiinflammatory action in experimental animals.Presence of a long alkyl chain (C13H31) renders the compounds to be less toxic.
- Ramalingam, T.,Sattur, P. B.
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p. 1204 - 1207
(2007/10/02)
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