IJCB DEC 2009

Indian Journal of Chemistry
Sect. B: Organic Chemistry including Medicinal Chemistry http://www.niscair.res.in; http://nopr.niscair.res.in Total visitors: 951 since 11-12-09
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 ()**

CONTENTS

Papers