Design, Synthesis, and in Vivo SAR of a Novel Series of Pyrazolines as Potent Selective Androgen Receptor Modulators

Zhang, Xuqing; Li, Xiaojie; Allan, Grant; Sbriscia, Tifanie; Linton, Olivia; Lundeen, Scott G.; Sui, Zhihua

doi:10.1021/jm0613976

Cited by 85 publications

(38 citation statements)

References 32 publications

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“…In addition, androgen receptor agonists have shown activities as protective, as well as regenerative, and have been considered as therapeutic options in cases of muscle insult (e.g., toxin insult, freeze insult, disuse atrophy) [35][36][37][38]. A component of skeletal muscle in such injury situations, whether direct or indirect, often involves nerve denervation.…”

Section: Discussionmentioning

confidence: 99%

Molecular Changes at the Post-Synapse and Improved Motor Function Suggest Accelerated Recovery with SARM Treatment in an Androgen-Depleted Animal Model of Nerve Injury

Bryant¹

2017

J Musculoskelet Disord Treat

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Section: Discussionmentioning

confidence: 99%

Molecular Changes at the Post-Synapse and Improved Motor Function Suggest Accelerated Recovery with SARM Treatment in an Androgen-Depleted Animal Model of Nerve Injury

Bryant¹

2017

J Musculoskelet Disord Treat

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“…These types of heterocyclic compounds are useful intermediates in the preparation of biologically interesting compounds [24] (Scheme 4).…”

Section: Epoxidation Of -Unsaturated Trifluoromethyl Ketonesmentioning

confidence: 99%

Asymmetric epoxidation of α,β-unsaturated ketones using α,α-diarylprolinols as catalysts

Zheng

Zhao

2010

Chin. Sci. Bull.

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Asymmetric epoxidation of , -unsaturated ketones has been extensively studied and several important procedures have been developed in the last decade. This review addresses the most significant advances in asymmetric epoxidation of , -unsaturated ketones using proline-derived , -diarylprolinols as catalysts. Special attention has been paid to the enantioselective epoxidation of chalcones, , -unsaturated trifluoromethyl, trichloromethyl ketones and , -unsaturated -keto esters based on the reseach of our group. epoxidation, electron-deficient olefins, organocatalysis, ketone, prolinol Citation:Zheng C W, Zhao G. Asymmetric epoxidation of , -unsaturated ketones using , -diarylprolinols as catalysts.Optically active epoxides are highly useful intermediates and building blocks for the synthesis of biologically active compounds. Various effective systems have been developed over the years for the preparation of chiral epoxides [1]. Among the many powerful methods for the enantioselective epoxidation of olefins, metal-catalyzed epoxidation of allylic alcohols with chiral titanium catalysts [2], epoxidation of allylic [3] and homoallylic [4] alcohols using chiral vanadium catalysts and epoxidation of unfunctionalized olefins using chiral manganese [5] or iron [6] catalysts have proven to be powerful approaches. In recent years, significant progress has been made by Shi [7] on asymmetric epoxidation of various types of olefins catalyzed by chiral ketonesand iminium salts [8], and Shibasaki has developed the epoxidation of electron-deficient olefins catalyzed by La-BINOL-Ph 3 As=O complex which gave a better result [9]. Development of new methodologies, characterized by operational simplicity and use of easily available catalysts, is the main target of modern organic synthesis. Asymmetric organocatalysis offers most of these advantages, since *Corresponding author (email: zhaog@mail.sioc.ac.cn)metal-free and environmentally friendly conditions have been accomplished for many transformations using small organic molecules as chiral promoters. Since the epoxidation of electron-deficient carbonyl compounds [10] using alkaline H 2 O 2 was reported by Weitz-Scheffer, much progress has been made towards the development of an asymmetric variant. Phase-transfer catalysts investigated by Wynberg et al. [11] and polyamino acids developed by Juliá and coworkers [12] for the asymmetric epoxidation of , -unsaturated ketones meant a breakthrough for this type of reactions. Recently, the use of chiral prolinols as organocatalysts has been reported as a new methodology for asymmetric epoxidation of electron-deficient olefins [13,14]. This review describes the progress in this area.

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“…In addition to having antiproliferative [11], Antiparasitic [12] and herbicidal properties [13]. Several pyrazoles have also been reported to have anti-inflammatory [14] and antiprotozoal effects [15,16].…”

Section: Introductionmentioning

confidence: 99%

Synthesis of New Heterocyclic Compounds with Biological Activity against Pathogenic Microbes in the Albaha Area

Mahmoud¹

2018

BJSTR

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Several new heterocyclic derivatives containing fused pyrazoloxazine moieties were synthesized via cycloaddition reactions of binucleophilic dentates, including hydrazine hydrate and its derivatives as well as active methylene compounds and aniline derivatives, resulting in novel five-, six-and seven-membered heterocyclic compounds. Due to increased microbial resistance to currently available drugs accentuate a real problem, so novel antimicrobial drugs are needed. Pyrazoles are good candidate as antimicrobial agents, where they have low-molecularweight compounds, nonvolatile and chemically stable. The novel synthesized five-, six-and seven-membered heterocyclic compounds were tested for their antimicrobial activity against different pathogenic microorganisms inside Albaha area. Bacterial species included Staphylococcus aureus, Staphylococcus epidermidis, Salmonella enteritidis, Streptococcus faecalis, Streptococcus agalactiae, Klebsiella pneumonia, Proteus mirabilis, Pseudomonas aeruginosa, Acinetobacter baumannii, and Enterobacter aerogenes. However, the following fungi were tested: Aspergillus niger, Aspergillus fumigates, Penicillium chrysogenium, Trichophyton rubrum and Candida albicans 157 and Candida albicans causes candidiasis. Staphylococcus aureus 119 was largely inhibited were observed after contact with synthesized pyrazoloxazine derivatives 1, 5, 8, 10, 13 and 24. Of the susceptible bacteria, Klebsiella pneumonia and Enterobacter aerogens 157 were the least affected, with inhibition zones between 10 and 12 mm. The pyrazoloxazine derivatives 3, 4, 25, 2Y, Ox1 and Ox2 inhibited all the fungi tested, including Aspergillus niger, Aspergillus fumigatus, Penicillium chrysogenium and Trichophyton rubrum. The zones of inhibition ranged from 40 to 14 mm/disc for these organisms. The current study demonstrates that the newly synthesized pyrazoloxazine derivatives have a good inhibition capacity against most tested pathogenic bacterial and fungal species.

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Design, Synthesis, and in Vivo SAR of a Novel Series of Pyrazolines as Potent Selective Androgen Receptor Modulators

Cited by 85 publications

References 32 publications

Molecular Changes at the Post-Synapse and Improved Motor Function Suggest Accelerated Recovery with SARM Treatment in an Androgen-Depleted Animal Model of Nerve Injury

Molecular Changes at the Post-Synapse and Improved Motor Function Suggest Accelerated Recovery with SARM Treatment in an Androgen-Depleted Animal Model of Nerve Injury

Asymmetric epoxidation of α,β-unsaturated ketones using α,α-diarylprolinols as catalysts

Synthesis of New Heterocyclic Compounds with Biological Activity against Pathogenic Microbes in the Albaha Area

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