- Pyrazole-Thiazole Core-Containing Analogs Exhibit Adjunctive Activity with Meropenem against Carbapenem-Resistant Enterobacteriaceae (CRE)
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Pyrazole-thiazole core-containing compound KP-40 and 20 novel derivatives were designed and synthesized through traditional SAR analysis. These molecules displayed adjunctive activity with meropenem against Gram-negative bacteria evidenced by a range of fractional inhibitory concentration (FIC=0.5–0.25) and minimum adjunctive concentration (MAC=128–32 μM) values. Of this series of molecules, four compounds displayed notable adjunctive potential, with FIC and MAC values of 0.25 and 32 μM, respectively. Moreover, the solubility of these compounds was improved to an acceptable range. Further analysis using our “in house” permeation and efflux multi parameter optimization (PEMPO) algorithm revealed key physicochemical properties that may be critical for the development of active Gram-negative antibacterials. Taking PEMPO scores into consideration prior to executing synthesis of analogs may be a simple, yet rapid and effective strategy that can be used in conjunction with traditional SAR approaches to aid in the design of potent Gram-negative antibacterials.
- Kim, Chungsik,Kassu, Mintesinot,Smith, Kenneth P.,Kirby, James E.,Manetsch, Roman
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p. 2775 - 2780
(2021/07/02)
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- METHODS OF TREATMENT WITH AMINOLEVULINIC ACID SYNTHASE 2 (ALAS2) MODULATORS
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Described herein is a compound of Formula I or a pharmaceutically acceptable salt thereof: wherein Ring A R1, R2, a, b, and n are as defined herein. Also described is a method of treating a subject having a disorder in need of treatment, comprising inhibiting aminolevulinic acid synthase 2 (ALAS2) in the subject by administering a compound of Formula (I) or a pharmaceutically acceptable salt thereof. Disorders that are of particular interest are blood disorders, such as porphyria and anemia.
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Paragraph 00144
(2020/12/29)
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- Green synthesis approaches of 2-bromo-4-methyl thiazole-5-carboxamide derivatives as potent microbial agents
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As a part of our ongoing research in the development of new, selective and environmental friendly methodologies, herein we report a new series of 2-bromo-4-methylthiazole-5-carboxamide derivatives using polyethylene glycol-400 (PEG-400) as a solvent. All
- Miryala, Jeevanreddy,Morthad, Mahesh,Battu, Satyanarayana
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p. 297 - 302
(2019/01/19)
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- Facile synthesis of novel (1-Aryl/alkyl-1H-1,2,3-triazol- 4-yl)methyl-2-bromo-4-methylthiazole-5-carboxylates by Cu(I) catalyzed click reaction
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A number of novel thiazole-triazole heterocycles bearing (1-aryl/alkyl-1H-1,2,3-triazol-4-yl)methyl- 2-bromo-4-methylthiazole-5-carboxylates was synthesized through the click reaction. The structure of all new synthesized compounds was established by sup
- Sudhakar,Thirupathi,Balakishan,Narsima chary,Ravi
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p. 1722 - 1729
(2016/08/26)
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- Process for the preparation of thiazole derivatives
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This document discloses a process for the preparation of a synthetic intermediate in the synthesis of molecules having the following formula (I):
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Paragraph 0150-0151
(2015/11/09)
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- QUINOLONES USEFUL AS INDUCIBLE NITRIC OXIDE SYNTHASE INHIBITORS
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The present invention relates to novel quinolones of Formula I that inhibit inducible NOS synthase together with methods of synthesizing and using the compounds including methods for inhibiting or modulating nitric oxide synthesis and/or lowering nitric oxide levels in a patient by administering the compounds for the treatment of disease.
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Page/Page column 51
(2008/12/06)
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- THIAZOLE DERIVATIVES AS KINASE INHIBITORS
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A series of thiazole derivatives which are substituted in the 2-position by a substituted morpholin-4-yl moiety, being selective inhibitors of P13 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.
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Page/Page column 38-39
(2008/12/05)
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- The Preparation of Thiazole-4- and -5-carboxylates, and an Infrared Study of their Rotational Isomers
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Convenient general procedures have been developed for preparing series of thiazole-4- and -5-carboxylates containing alkyl and halogeno substituents.While both series of esters show i.r. carbonyl doublets caused by rotational isomerism, the more intense absorptions of the 4-carboxylates are the lower wavenumber components, whereas those of the 5-carboxylates are the higher wavenumber components.In both series the stronger bands arise from the thermochemically more stable forms; identification of these forms as the carbonyl O,S-syn-s-trans rotamers is more certain with the 4-carboxylates than with the 5-carboxylates.
- Barton, Anne,Breukelman, Stephen P.,Kaye, Perry T.,Meakins, G. Denis,Morgan, David J.
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p. 159 - 164
(2007/10/02)
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