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Asymmetric Reductive Amination of Carbonyl Compounds by Using<i>N,N,N</i>-Tributylpropanaminium Based Novel Chiral Ionic Liquid

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International Journal of Organic Chemistry 2013年第3期3卷 190-193页

作者： Boyina Rupini Sharda Pasricha brijesh rathi Department of Chemistry Sri Venkateswara College University of Delhi New Delhi India School of Agriculture Environmental Studies Indira Gandhi National Open University New Delhi India

Asymmetric reductive amination of carbonyl compounds was carried out using a novel class of aliphatic quarternary ammonium based chiral ionic liquid. S-(+)-2,3-dihydroxy-N,N,N-tributylpropanaminum bromide chiral ionic liquid has been synthesized, characterized and used for asymmetric reductive amination of carbonyl compounds in the presence of sodium borohydride. These preliminary results are encouraging and advocate dual role of novel ionic liquid as a medium and reducing agent for proficient conversion of ketones to amines, however, reductive amination reaction needs to be established for other substituents.

关键词： Ionic Liquid Asymmetric Reductive Amination Chiral Carbonyl Compounds

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Boronic acid-containing diarylpyrimidine derivatives as novel HIV-1NNRTIs: Design, synthesis and biological evaluation

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Chinese Chemical Letters 2021年第12期32卷 4053-4057页

作者： Da Feng Fenju Wei Yanying Sun Prem Prakash Sharma Tao Zhang Hao Lin brijesh rathi Erik De Clercq Christophe Pannecouque Dongwei Kang Peng Zhan Xinyong Liu Department of Medicinal Chemistry Key Laboratory of Chemical Biology(Ministry of Education)School of Pharmaceutical SciencesCheeloo College of MedicineShandong UniversityJi'nan 250012China Laboratory for Translational Chemistry and Drug Discovery Department of ChemistryHansraj CollegeUniversity of DelhiDelhi 110007India Rega Institute for Medical Research Laboratory of Virology and ChemotherapyK.U.LeuvenLeuven B-3000Belgium China-Belgium Collaborative Research Center for Innovative Antiviral Drugs of Shandong Province Ji'nan 250012China Suzhou Research Institute Shandong UniversitySuzhou 215123China

Drug resistance remains to be a serious problem with type Ⅰ human immunodeficiency virus(HIV-1) nonnucleoside reverse transcriptase inhibitors(NNRTIs). A series of novel boronic acid-containing diarylpyrimidine(DAPY) derivatives were designed via bioisosterism and scaffold-hopping strategies,taking advantage of the ability of a boronic acid group to form multiple hydrogen bonds. The target compounds were synthesized and evaluated for their anti-HIV activities and cytotoxicity in MT-4 *** 10 j yielded the most potent activity and turned out to be a single-digit nanomolar inhibitor towards the HIV-1 ⅢB [wild-type(WT) strain], L100 I and K103 N strains, with 50% effective concentration(EC_(50)) values of 7.19–9.85 nmol/L. Moreover, 10 j inhibited the double-mutant strain RES056 with an EC_(50) value of 77.9 nmol/L, which was 3.3-more potent than that of EFV(EC_(50)= 260 nmol/L) and comparable to that of ETR(EC_(50)= 32.2 nmol/L). 10j acted like classical NNRTIs with high affinity for WT HIV-1 reverse transcriptase(RT) with 50% inhibition concentration(IC_(50)) value of 0.1837 μmol/L. Furthermore,molecular dynamics simulation indicated that 10 j was proposed as a promising molecule for fighting against HIV-1 infection through inhibiting RT activity. Overall, the results demonstrated that 10 j could serve as a lead molecule for further modification to address virus-drug resistance.

关键词： HIV-1 NNRTIs NNIBP DAPY Boronic acid Molecular dynamics simulation

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Depletion of the Ozone Layer and Its Consequences: A Review

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American Journal of Plant Sciences 2013年第10期4卷 1990-1997页

作者： Anjali Aggarwal Reeta Kumari Neeti Mehla Deepali Rishi Pal Singh Sonal Bhatnagar Kameshwar Sharma Kuldeep Sharma Vashishtha Amit brijesh rathi Department of Biochemistry Sri Venkateswara College University of Delhi New Delhi India Department of Botany Deshbandhu College University of Delhi New Delhi India Department of Botany Sri Venkateswara College University of Delhi New Delhi India Department of Botany Uni- versity of Delhi New Delhi India. Department of Chemistry Sri Venkates- wara College University of Delhi New Delhi India

Ozone (O3) is a stratospheric layer that plays important role in providing support to humans for their survival. It is an essential factor for many global, biological and environmental phenomena. The ultra-violet (UV) rays emitted from sun are captured by ozone and thereby provide a stable ontological structure in the biosphere. Various anthropogenic activities such as emissions of CFCs, HCFCs and other organo-halogens lead to the depletion of ozone. The ozone depletion resulted in secondary production of an ozone layer near the ground (terrestrial ozone layer), which is responsible for adverse effects on plants, humans and environment with increased number of bronchial diseases in humans. The mutations caused by UV rays result in variation in morphogenic traits of plants which ultimately decreases crop productivity. However, UV radiation is required in optimum intensity for both plants and animals. This review takes into an account the wide ranging effects of ozone depletion with a majority of them being detrimental to the plant system.

关键词： Ozone Depletion Ultra-Violet Radiation Chlorofluorocarbons Plants Ecosystem

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Posterior segment nucleotomy for dislocated sclerotic cataractous lens using chandelier endoilluminator and sharp tipped chopper

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International Journal of Ophthalmology(English edition) 2015年第4期8卷 833-834页

作者： brijesh Takkar Rajvardhan Azad Shorya Azad Anubha rathi Dr.Rajendra Prasad Centre for Ophthalmic Sciences All India Institute of Medical Sciences

· AIM: To describe a new surgical technique for managing dislocated sclerotic cataractous lens.· METHODS: Six patients with advanced posteriorly dislocated cataracts were operated at a tertiary care centre and analyzed retrospectively. After standard 3 port23 G pars plana vitrectomy and perfluorocarbon liquid(PFCL) injection, the dislocated white cataract was held with occlusion using phaco fragmatome and then chopped into smaller pieces with a sharp tipped chopper using 25 G chandelier endoilluminator. Each piece was emulsified individually. Following aspiration of PFCL,Fluid Air Exchange was done in all the cases and surgery completed uneventfully.·RESULTS: Best corrected visual acuity(BCVA) in all the patients was better than 6/12 after one month of follow up. No serious complications were noted till minimum 6mo of follow up.·CONCLUSION: Four port posterior segment nucleotomy with a chandelier endoilluminator, fragmatome and a chopper appears to be a safe, easy and effective procedure for managing dislocated sclerotic cataractous nuclei. Ultrasonic energy used and adverse thermal effects of the fragmatome on the sclera may be lesser.

关键词： posterior segment nucleotomy intravitreal nucleotomy dislocated sclerotic lens dislocated hard lens dislocated lens complications of phacoemulsification

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Bilateral lens subluxation in a case of Behcet's disease related uveitis

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Eye Science 2016年第3期31卷 197-198页

作者： Anubha rathi brijesh Takkar Shorya Vardhan Azad Pradeep Venkatesh Rohan Chawla Retina and Uvea Services Dr R P Centre for Ophthalmic SciencesAll India Institute of Medical Sciences

Ocular inflammation accompanying the pediatric Behcet's disease(BD)is characterized by a relapsing and complicated course,often resulting in blindness due to severe bilateral affection(1).Ectopia lentis(EL)is an important association of multiple ocular and systemic syndromes,with favorable visual outcomes if managed ideally(2).We discuss a unique case presenting with a combination of these entities。

关键词： BD case

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