Indian Journal of Chemistry

 

Sect. B: Organic Chemistry including Medicinal Chemistry

http://www.niscair.res.in; http://nopr.niscair.res.in

Total visitors: 6239 since 06-08-2012

 

VOL. 51B

NUMBER 8

August 2012

 

CONTENTS

 

Papers

 

 

 

 

1105

Design, microwave-assisted synthesis and in silico docking studies of new 4H-pyrimido[2,1-b]benzo­thiazole-2-arylamino-3-cyano-4-ones as possible ade­no­sine A2B receptor antagonists

 

A series of new 4H-pyrimido[2,1-b]benzothiazole-2-arylamino-3-cyano-4-ones 6a-g have been designed and synthesized by MAOS technique and evaluated in silico (docking studies) using a homology model of A2B adenosine receptor employing GOLD (CCDC, 4.0.1 version) software.

 

 

 

 

C Balakumar, D Pran Kishore, K Venkat Rao, B Lakshmi Narayana, K Rajwinder,  V Rajkumar &

A Raghuram Rao*

Centre with Potential for Excellence in Biomedical Sciences (CPEBS), Panjab University, Chandigarh 160 014, India

 

 

 

 

 

 

 

1114

Synthesis and biological evaluation of some new bipyrazolylbenzenesulfonamides as possible anti­microbial and chemotherapeutic agents

 

A series of functionalized bipyrazoles, fused bipyrazoles and other related heterocyclic systems have been synthesized. The key intermediate bipyrazoles have been prepared by cyclocondensation of the appropriate chalcone with 4-hydrazinobenzenesulfonamide hydrochloride. All the synthesized compounds show weak anticancer activity and weak antimicrobial and antifungal activity against some bacteria and fungi.

 

 

 

 

Hassan M Faidallah*, Khalid A Khan, Abdullah M Asiri & Mohie E M Zayed

 

Department of Chemistry, Faculty of Science, King Abdulaziz University, P.O. Box 80203  Jeddah 21589, Saudi Arabia

 

 

 

 

 

 

 

 

 

 

 

 

 

1123

Stereocontrolled oxidative additions upon N-alkyl-1,4-dihydropyridines: Synthesis of hexahydrofuro[2,3-b]pyridine derivatives

 

 

 

 

 

 

 

 

 

 

 

 

Rakesh Kumar*, Dhiraj Kumar & Ashok K Prasad

 

Department of Chemistry, Kirori Mal College, University of Delhi, Delhi 110 007, India

 

 

 

 

 

 

 

1131

Protective role of native bovine serum albumin and alpha-unsaturated fatty acids on catechin oxidation

Catechin, a common ingredient of tea and coffee undergoes spontaneous oxidation by aerial O2, heat and UV exposure or ammonium persulfate treatment. Several α–unsaturated fatty acids, β–Mercapto ethanol and native bovine serum albumin block the oxidation process. The present studies indicate that ammonium persulfate, UV illumination and aerial oxygenation produce the same yellow poly-phenolic species.

 

 

 

 

 

 

 

 

 

 

Sankar P Mitra

 

Acotrix Inc.,100 Berber Avenue, Worcester, MA 01606, U.S.A.

 

 

 

 

 

 

 

 

 

 

 

 

 

1145

Synthetic potentiality of novel N-methyl isoxazolidines in the synthesis of 1,3-amino alcohols under microwave irradiation

 

Microwave assisted N-O bond cleavage of novel N-methyl isoxazolidines under mild conditions have been studied and found to afford 1,3-amino alcohols readily with high yield in a short reaction time.

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

Bhaskar Chakraborty* & Prawin Kumar Sharma

 

Organic Chemistry laboratory, Sikkim Government College, Gangtok 737 102, India

 

 

 

 

 

 

 

 

 

 

 

 

 

1151

Effect of A1,3-strain on the stereochemistry of N-acetyl and N,O-diacetyl-r-2,c-6-diphenylpiperidin-4-one oximes

 

The N-acetyl and N,O-diacetyl –r-2,c-6-diphenyl-piperidin-4-one oximes has been found to adopt twist-boat conformations on the basis of results from NMR spevral studies, X-ray crystallography and semiempirical MO calculations

 

 

 

 

 

 

 

 

 

R Vijayalakshmi, M Muthukumar, S Ponnuswamy* & R Jeyaraman

 

Department of Chemistry, Bharathidasan University, Tiruchirappalli 620 024, India

 

 

 

 

 

Notes

 

 

 

1163

Iodine catalysed aza-Michael addition of carbamates to chalcones

 

 

 

 

 

 

 

 

 

 

 

 

 

Sanjib Deuri, Dolly Kataki & Prodeep Phukan*

 

Department of Chemistry, Gauhati University, Guwahati 781 014, India

 

 

 

 

 

 

 

 

 

 

 

 

 

1168

Zinc chloride promoted efficient and facile BOC protection of amines

 

Amines are efficiently protected as their BOC derivatives under mild reaction condition when reacted with BOC2O in presence of ZnCl2. The present method is applicable to a variety of amines including aliphatic, aromatic as well as hetero aromatic amines.

 

 

 

 

 

 

 

 

M Arifuddin*, N Lakshmikant, N Rajasekar & D B Shinde

 

National Institute of Pharmaceutical Education and Research (NIPER Hyderabad), Balanagar, Hyderabad 500 037, India

 

 

 

 

 

 

 

1173

Ultrasound and microwave assisted rapid and sustainable route to synthesis of benzothiazine derivatives

 

Ultrasound and microwave assisted synthesis of 2-Meldrum-2H,4H-2-carbonyl methyl-3-oxo-1,4-benzothiazine 10, 2-dimidone-2H,4H-2-carbonyl methyl-3-oxo-1,4-benzothiazine 11, 2H,4H-2-amino-[3-methyl pyrazol-5-one-1-yl]-carbonyl methyl-3-oxo-1,4-benzothiazine 12, 2H,4H-2-amino-[3,5-dmethyl pyrazol-1-yl]-carbonyl methyl-3-oxo-1,4-benzothiazine 13 and 2H,4H-2-amino-[3-phenyl, 5-methyl pyrazol-1-yl]-carbonyl methyl-3-oxo-1,4-benzothiazine 14 from 2-aminobenzenethiol and 1,3 diketo compounds containing active methylene group have been carried out. All the synthesized compounds have been investigated for their antibacterial activities.

 

 

 

 

 

 

 

 

Vijay V Dabholkar* & Rahul P Gavande

 

Organic Research Laboratory, Department of Chemistry, K C College, Churchgate, Mumbai 400 020, India

 

 

 

 

 

 

 

 

 

 

 

 

 

1180

Green synthesis of novel isoxazoline derivatives using N-methyl-α-chloro nitrone and their antibacterial activities

 

Microwave assisted 1,3-Dipolar cycloaddition reaction of N-methyl-α-chloro nitrone with various alkynes as dipolarophile have been studied and found to afford diastereomeric novel isoxazoline derivatives with high selectivity. All the synthesized compounds have been screened for their antibacterial activity and are found to exihibit significant activity.

 

 

 

Bhaskar Chakraborty*, Prawin Kumar Sharma  & Amalesh Samanta

 

Organic Chemistry Laboratory, Sikkim Government College, Gangtok 737 102, India

 

 

 

 

 

Authors for correspondence are indicated by (*)