Indian Journal of Chemistry

Sect. B: Organic Chemistry including Medicinal Chemistry

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Special Issue on Interplay of Chemical and Biological Sciences: Impact on Health and Environment

VOL. 48B

NUMBER 12

December 2009

CONTENTS

Papers

 

 

 

1699

Adventures in heterocycle chemistry: The oxa-Michael cascade for the synthesis of complex natural products and highly functionalized bioactive compounds

 

 

 

 

 

N Volz, M C Bröhmer, J Toräng, M Nieger & S Bräse*

 

Institut für Organische Chemie, Karlsruhe Institute of Technology, Fritz-Haber-Weg 6, 76131 Karlsruhe, Germany

 

 

 

 

 

 

 

1704

Polymerization of 1,6-diynes — Scope, structure, and optical properties

A minireview is provided on recent advances in the field of 1,6-diyne polymerizations by olefin metathesis catalysts as well as the synthesis and characterization of related short-length oligoenes.

 

 

 

 

 

 

 

 

 

 

 

 

 

Constantin Czekelius*

 

Institut für Chemie und Biochemie, Freie Universität Berlin, Germany

 

 

 

 

 

 

 

 

 

 

 

 

 

1709

Expanding the applications of locked nucleic acids

 

LNA nucleoside 5-triphosphates have been investigated as substrates for various DNA and RNA polymerases by performing primer extension reactions, PCR amplification and in vitro transcription reactions.

 

 

 

 

 

 

 

 

 

 

 

 

Rakesh N Veedu* & Jesper Wengel

 

Nucleic Acid Center, Department of Physics and Chemistry, University of Southern Denmark, Campusvej 55,

Odense M, 5230, Denmark

 

 

 

 

 

 

 

 

1712

Synthesis and regioselective deacylation studies on peracylated 2′-azido arabino- and ribo-thymine nucleosides: Towards 5′-O,2′-N-linked oligo­nucleotides

Peracylated 1-(2′-azido-α-l-arabino-/β-d-ribofuranosyl)­thy­mine has been chemoenzymatically synthesized and subjected to deacylation studies in the presence of CAL-B (Candida antarctica lipase-B immobilized on polyacrylate) in aceto­nitrile.

 

 

 

 

 

 

 

Deepti Sharma, Anuj Khandelwal, Raman K Sharma, Sumati Bhatia, L Chandrashekar Reddy,
Carl E Olsen, Jesper Wengel, Virinder S Parmar & Ashok K Prasad*

 

Bioorganic Laboratory, Department of Chemistry, University of Delhi, Delhi 110 007, India

 

 

 

 

 

 

 

 

 

 

 

 

 

1721

Novel oligonucleotide analogues based on morpho­lino nucleoside subunits–Antisense technologies: New chemical possibilities

 

 

 

 

 

 

 

 

 

 

 

Tatyana V Abramova*, Marat F Kassakin & Vladimir N Silnikov

 

Instit′ute of Chemical Biology and Fundamental Medicine, Lavrent’ev Ave, 8, 630090, Novosibirsk, Russia

 

 

 

 

 

 

 

1727

Lipase-catalyzed regio- and stereoselective de­acylation: Separation of anomers of peracylated a,b-d-ribofuranosides

 

Lipozyme® TL IM catalyzed regio- and stereoselective deacylation of the acyloxy function involving C-5-OH of the a-anomer over the other acyloxy function  in the anomeric mixture of peracylated a,b-d-ribofuranosides has been achieved. The enzymatic methodology finds application for the easy and efficient separation of acylates of anomers of a,b-d-ribofuranosides.

 

 

 

 

 

 

 

 

 

 

 

 

 

 

Raman K Sharma, Neha Aggarwal, Anu Arya, Carl E Olsen, Virinder S Parmar & Ashok K Prasad*

 

Bioorganic Laboratory, Department of Chemistry, University of Delhi, Delhi 110 007, India

 

 

 

 

 

 

 

 

 

 

 

 

 

1732

Synthesis and antimicrobial activity of 5-(2-aminothiazol-4-yl)-3, 4-dihydro-4-phenyl pyrimi­din-2(1H)-one

 

An efficient cyclocondensation of appropriately substituted of 2 with thiourea in ethanol proceeds in high yield to furnish the corresponding substituted 5-(2-aminothiazol-4-yl)-3, 4-dihydro-4-phenyl pyrimidin-2(1H)-one.

 

 

 

 

Kushal R Lanjewar, Anjali M Rahatgaonkar, Mukund S Chorghade* & Binda D Saraf

 

Chemistry Department, Institute of Science, R T M Nagpur University, Nagpur 440 001, India

 

 

 

 

 

 

 

1738

Synthesis and lipase-catalysed enantioselective acylation studies on ethyl 4-aryl-3,4-dihydropyri­midin-2(1H)-ones

 

A series of different analogs of 4-aryl-3,4-dihydropyrimidin-2(1H)-one have been synthesized and their biocatalytic resolution has been carried out using immobilized lipase CAL-L(A) (immobilized on accurel).

 

 

 

 

 

Ashok K Prasad, Pragya Arya, Sumati Bhatia, Raman K Sharma, Rishipal Singh, Brajendra K Singh,
Erik Van der Eycken, Rajpal Singh, Carl E Olsen & Virinder S Parmar

 

Bioorganic Laboratory, Department of Chemistry, University of Delhi, Delhi 110 007, India

 

 

 

 

 

 

 

1749

Weinreb amide based building blocks for convenient access to various synthetic targets

New building blocks based on Weinreb-amide functionality for the synthesis of various important targets are described.

 

 

 

 

 

 

 

B Sivaraman, B N Manjunath, A Senthilmurugan, K Harikrishna & Aidhen Indrapal Singh*

 

Department of Chemistry, Indian Institute of Technology, Madras, Chennai 600 036, India

 

 

 

 

 

 

 

 

 

 

1757

Synthesis of new succinate-dihydrotestosterone-dihydropyrimidine conjugate

 

 

 

 

L Figueroa-Valverde*, F Díaz-Cedillo & A Camacho-Luis

 

Facultad de Ciencias Químico-Biológicas, Lab de Farmaco-química, Universidad Autónoma de Campeche,

Av. Agustín Melgar s/n entre calle Juan de la Barrera y C-20, Col Buenavista C.P.24039 Campeche Cam, México

 

 

 

 

 

 

 

1761

Mammalian target of rapamycin (mTOR) inhibitors with therapeutic potential for colitis

 

 

 

 

 

Vijaykumar Deore, Mandar R Bhonde, Ram A Vishwakarma, Nilesh M Dagia, Sanjay Kumar &
Abhijit Roychowdhury

 

Department of Medicinal Chemistry & Department of Pharmacology, Piramal Life Sciences
1-Nirlon Complex, Off Western Express Highway, Goregaon (E), Mumbai 400 063, India

 

 

 

 

 

 

 

1766

Synthesis of nano-sized C3-symmetric 2,4,6-triphenyl-1,3,5-s-triazine and 1,3,5-triphenylben­zene derivatives via the trimerization followed by Suzuki-Miyaura cross-coupling or O-alkylation reactions and their biological evaluation

 

C3-symmetric biphenyl-based and triphenoxy derivatives of 1,3,5-s-traizine and 1,3,5-triphenyl benzene have been synthesized using a sequence of cyclotrimerization and Suzuki-Miyaura cross-coupling or O-alkylation reactions and the biological activity of O-alkylated triazines has been tested towards HeLa cell proliferation.

 

 

 

 

Sambasivarao Kotha*, Dhurke Kashinath, Manu Lopus & Dulal Panda

Department of Chemistry, Indian Institute of Technology-Bombay, Powai, Mumbai 400 076, India

 

 

 

 

 

 

 

 

 

 

1771

Green methodologies in synthesis and natural product chemistry of phenolic compounds

 

 

 

 

Arun K Sinha*, Naina Sharma, Amit Shard, Abhishek Sharma, Rakesh Kumar & Upendra K Sharma

 

Natural Plant Products Division, Institute of Himalayan Bioresource, Technology, Palampur 176 061, India

 

 

 

 

 

 

 

1780

Experimental and computational evaluation of new quinolinyl chalcones as potent antiplasmodial agents

In a search for new antiplasmodial agents against Plasmodium falciparum, a series of thirty five diversely substituted chalcones derived from a quinoline scaffold e.g. (E)-3-(2-chloroquinolin-3-yl)-1-(2-hydroxyphenyl)prop-2-en-1-one/(E)-(2-chloro-6-ethoxyquinolin-3-yl)(2-hydroxyphenyl) prop-2-en-1-one and (2Z)-3-(2-chloroquinolin-3-yl)-1-(2-hydroxy­henyl)-3-iodoprop-2-en-1-one are prepared and studied for their binding in the active sites of Plasmodium falciparum lactate dehydrogenase (pfLDH) enzyme.

 

 

2a-y

2a-j                                                                                             3a-j

 

 

 

Shikha S Dave, Ajay M Ghatole, Anjali M Rahatgaonkar, Mukund S Chorghade*,

P M S Chauhan & Kumkum Srivastava

 

Chemistry Department, Institute of Science, Civil Lines, Nagpur 440 001, India

 

 

 

 

 

 

 

 

 

 

 

 

1794

Synthesis and studies on antimicrobial, anti­inflammatory and antiproliferative activities of  heterocycles derived from 4-/5-/6-/7-nitro/5-fluoro/chloro/bromoindole-2-carbohydrazides

 

Synthesis and studies on antimicrobial, antiinflammatory and anti­proliferative activities of heterocycles derived from 4-/5-/6-/7-nitro/5-fluoro/chloro/bromoindole-2-carbohydrazides are reported.

 

 

 

B Narayana, B  V Ashalatha, K K Vijaya Raj & B K Sarojini

 

Department of  Studies and Research in Chemistry, Mangalore University, Mangalagangotri  574 199, India

 

 

 

 

 

 

 

1806

Annual Index

 

 

 

 

 

Authors for correspondence are indicated by (*)