- Development of Highly Potent Carbazole Amphiphiles as Membrane-Targeting Antimicrobials for Treating Gram-Positive Bacterial Infections
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The development of new antimicrobial agents capable of curing drug-resistant bacteria-induced infections is becoming a major challenge to the global healthcare system. To develop antimicrobials with new molecular entities, a series of novel carbazole-based compounds were designed and synthesized by biomimicking the structural properties and biological function of antimicrobial peptides. Compound 29 was selected as a lead compound from the structure-activity relationship analyses and biological activity evaluation. Compound 29 showed excellent antimicrobial activity against Gram-positive bacteria (MICs = 0.78-1.56 μg/mL), poor hemolytic activity (HC50 > 200 μg/mL), and low cytotoxicity to mammalian cells. Compound 29 had fast bactericidal properties and effectively prevented bacterial resistance in laboratory simulations. Antibacterial mechanism studies revealed that compound 29 directly destroyed bacterial cell membranes, leading to bacterial deaths. Importantly, compound 29 displayed an excellent efficacy in a murine bacterial keratitis model caused by Staphylococcus aureus ATCC29213.
- Lin, Shuimu,Liu, Jiayong,Li, Hongxia,Liu, Ying,Chen, Yongzhi,Luo, Jiachun,Liu, Shouping
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- An efficient improved synthesis of carvedilol, via 2-(2-methoxyphenoxy)ethyl 4-methylbenzenesulfonate intermediate
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A facile synthesis of Carvedilol via a key 2-(2-methoxyphenoxy) ethyl 4-methylbenzenesulfonate intermediate is described and this approach avoids the formation of bis side product (impurity-B) due to weak basic conditions and also operationally suitable for industrial application.
- Tatendra Reddy,Suneel Kumar,Omprakash,Dubey
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p. 1615 - 1618
(2015/02/02)
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- A facile synthesis of carvedilol via β-amino alcohol intermediate
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A facile synthesis of Carvedilol via a key β-amino alcohol intermediate is described and this approach avoids the formation of bis side product (impurity B).
- Tatendra Reddy,Suneel Kumar,Omprakash,Dubey
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p. 251 - 254
(2013/09/24)
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- Lewis acid mediated nucleophilic ring-opening of 1-Benzhydryl Azetidine-3-ol with aryl alcohols: A formal synthesis of carvedilol
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Lewis acid mediated nucleophilic azetidine ring opening of 1-benzhydrylazetidine-3-ol with phenolic oxygen as nucleophile is reported. This approach was also utilized successfully to synthesize, carvedilol a β-adrenergic blocking agent.
- Krishna Reddy,Ramamohan,Ganesh,Srinivas,Mukkanti,Madhusudhan
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p. 3468 - 3472
(2012/07/30)
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- A facile synthesis of carvedilol, β-adrenergic blocking agent, via a key 5-substituted-.-oxazolidinone intermediate
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A facile synthesis of Carvedilol via a key 5-substituted-.-oxazolidinone intermediate is described and this approach avoids the formation of bis side product (impurity B). This approach could be useful for the preparation of many β-amino alcohols without formation of bis impurity.
- Madhusudhan,Kumar, B. Anand,Chintamani,Rao, M. Narasimha,Udaykiran,Suresh,Kumar, V. Kiran,Mukkanti
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experimental part
p. 606 - 610
(2010/12/25)
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- Carbazolyl-substituted ethanolamines as selective beta -3 agonists
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PCT No. PCT/US97/15230 Sec. 371 Date May 4, 1998 Sec. 102(e) Date May 4, 1998 PCT Filed Aug. 28, 1997 PCT Pub. No. WO98/09625 PCT Pub. Date Mar. 12, 1998Disclosed herein are selective beta 3 adrenergic agonists represented by the following structural formula: The variables in the structural formula shown above are defined in the specification. Also disclosed are methods of using these compounds for agonizing the beta 3 adrenergic receptor in patients in need of such treatment, for example, patients in need of treatment for obesity or Type II diabetes.
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