Indian Journal of Chemistry

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Sect. B: Organic Chemistry including Medicinal Chemistry

VOL. 50B

NUMBER 7

July 2011

CONTENTS

Papers

 

 

 

901

Synthesis and biological evaluation of novel oxalamido derivatives as caspase-3 inhibitors

 

Several N-(substituted-phenyl)-oxalamide derivatives have been synthesized and screened for caspase-3 activity. Compound 7c exhibits low micromolar caspase-3 activity.

 

 

 

 

 

 

Saumitra Sengupta*, G Venkateshwar Rao & P K Dubey

 

Medicinal Chemistry Division, Aurigene Discovery Technologies Ltd, Bangalore 560 100, India

 

 

 

 

 

 

 

906

Synthesis and antimicrobial activities of nitro substituted indolo[3,2-c]acridines

 

The efficient synthesis of biologically active 9-nitro-7-phenyl-5,6-dihydro-indolo[3,2-c]acridines 2a-e is described from the  reaction of 2,3,4,9-tetrahydro-1H-carbazol-1-one with 2-amino-5-nitro-benzophenone in acetic acid and a few drops of H2SO4 at refluxing temperature. The obtained compound 1-methyl-9-nitro-7-phenyl-5,6-dihydro-indolo[3,2-c]acridine 2a on further treatment with Pd/C in diphenyl ether affords 1-methyl-9-nitro-7-phenyl-indolo[3,2-c]acridine 3a. The anti-microbial properties of the synthesized nitro substituted indolo[3,2-c]acridines have been investigated.

 

 

 

 

 

 

K Prabakaran, E Yamuna & K J Rajendra Prasad*

 

Department of Chemistry, Bharathiar University, Coimbatore 641 046, India

 

 

 

 

 

 

 

 

 

 

 

 

 

910

Synthesis and antibacterial evaluation of novel heterocycles from 5-chloro-3-methyl-1-phenyl­pyrazole-4-carbaldehyde

 

Novel 3,5-heteroaryl-2-pyrazolines 5a-d have been synthesized by refluxing heteroarylchalcones 4a,b and hydrazines in ethanol. Heterochalcones have been explored for addition reaction with Br2/MeOH in the presence of Pb(NO3)2 or AgNO3 to afford addition products 6a,b. The newly synthesized compounds are identified on the basis of spectral data. Heterochalcones and heteroaryl-2-pyrazolines have been evaluated for their antibacterial activity.

 

 

 

 

 

 

 

 

 

Zeba N Siddiqui*, Shagufta Praveen & Mohammed Musthafa T N

 

Department of Chemistry, Aligarh Muslim University, Aligarh 202 002, India

 

 

 

 

 

 

 

918

Kinetics and mechanism of the oxidation of diols by butyltriphenylphosphonium dichromate

 

The oxidation of diols by butyltriphenyl- phosphonium dichromate in DMSO, in the  presence of acid, involves a diprotonated chromate ester in a preiequilibria which in  slow step disproportionates via. hydride- ion transfer through cyclic transition state to give a final product, hydroxyaldehyde.

 

 

 

 

 

 

Dinesh Panday & Seema Kothari*

 

Department of Chemistry, J N V University, Jodhpur 342 001, India

 

 

 

 

 

 

 

 

 

 

Notes

 

 

 

926

A mild and efficient four component one-pot synthesis of 2,4,5-triphenyl-(1H-1-imidazolyl)­iso­xa­zoles catalyzed by ceric ammonium nitrate

 

Ceric ammonium nitrate (CAN) acts as an efficient catalyst for the synthesis of 2,4,5-triphenyl-1H-1-imidazolyl isoxazoles in a four component one-pot condensation of benzil or benzoin, aromatic aldehyde, isoxazole amine and ammonium acetate. This one-pot procedure is very simple, affording excellent yields in shorter reaction time at ambient temperature. Isoxazole amines are employed as one of the synthon in this multi-component condensation for the first time.

 

 

 

 

 

 

 

 

E Rajanarendar*, K Rama Murthy & M Nagi Reddy

 

Department of Chemistry, Kakatiya University, Warangal 506 009, India

 

 

 

 

 

 

 

931

Synthesis and antibacterial activity of benz­amides and sulfonamide derived from 2-amino-5-bromo/nitropyridine against bacterial strains isolated from clinical patients

 

Different benzamide and sulfonamide derivatives of 2-amino-5-bromo/nitropyridine with potent antibacterial activity have been discussed.

 

 

 

 

 

 

 

 

Diwakar Rai & Ramendra K Singh*

 

Nucleic Acids Research Laboratory, Department of Chemistry, University of Allahabad, Allahabad 211 002, India

 

 

 

 

 

 

 

 

 

 

 

 

 

937

Synthesis of some new derivatives of 3,5-dimethyl azopyrazole as antifungal agents

 

Substituted 2-aminobenzothiazole 1 has been reacted with acetyl acetone and different hydrazines to give various (3,5-dimethyl-1-phenyl-1H-pyrazol-4-yl)-(substituted-benzothiazol-2-yl)-diazenes. IR, 1H NMR, mass spectral studies and elemental analysis have confirmed the structures of all these compounds. These compounds are evaluated for their antifungal activity.

 

 

 

 

2a

R’ =6-F

2b

R’ =4-Cl

3a

R’=6-F, R”= -C6H5

3b

R’=6-F, R”= -2,4di-NO2-C6H3

3c

R’=6-F, R”= -CS-NH2

3d

R’=6-F, R”= -CO-C6H5

3e

R’= 4-Cl, R”= -C6H5

3f

R’=4-Cl, R”= -2,4di-NO2-C6H3

3g

R’= 4-Cl, R”= -CS-NH2

3h
R’= 4-Cl, R”= -CO-C6H5

 

 

 

 

 

 

 

V Sareen*, V Khatri, D Shinde & S Sareen

 

Department of Chemistry, University of Rajasthan, Jaipur 302 004, India

 

 

 

 

 

 

 

941

Synthesis, characterization and antimicrobial activity of some 3-(2-(1H-benzo[d]imidazol-2-yl)­phenyl)-2-arylthiazolidin-4-ones

 

Several 3-(2-(1H-benzo[d]imidazol-2-yl)phenyl)-2-arylthiazolidin-4-ones have been prepared and tested for their antibacterial and antifungal activities.

 

 

 

 

 

 

N C Desai*, Nayan Bhatt, Mukesh Kumar & Atul Makwana

 

Medicinal Chemistry Division, University Department of Chemistry, Bhavnagar University, Bhavnagar 364 002, India

 

 

 

 

 

 

 

 

 

 

 

 

 

946

A one-step synthesis of 5,7-diaryl-1,5-dihydro (or 1,2,3,5-tetrahydro)-pyrano [2,3-d]pyrimidin-2,4-diones (or 2-thioxo-4-ones)

 

Reactions of 1,3-diaryl-2-propene-1-ones with barbituric acid or thiobarbituric acid give the corresponding 5,7-diaryl-1,5-dihydro (or 1,2,3,5-tetrahydro)pyrano[2,3-d]pyrimidin-2,4-diones (or 2-thioxo-4-ones) in glacial acetic acid in the presence of phosphorous pentoxide.

 

 

 

 

 

M Giasuddin Ahmed*, U K R Romman, Kawsari Akhter,

Md Ershad Halim, Md Mahbubur Rahman  & S Mosaddeq Ahmed

 

Department of Chemistry, University of Dhaka, Dhaka 1000, Bangladesh

 

 

 

 

 

 

 

949

Antibacterial evaluation of some novel 5-imida­zolones

 

The title compounds are prepared by the reaction between different azlactones 1a-j and thiophene-2-ethylamine 2. The constitution of all the synthesized compounds has been established by their physical properties, elemental analysis and spectral analysis. All the synthesized compounds have been screened for their in vitro antibacterial activity by using Gram - positive and Gram - negative bacteria.

 

 

 

 

 

 

Anjani Solankee*, Ghanshyam Patel & Kirti Patel

 

Department of Chemistry, B. K. M. Science College,  Valsad 396 001, India

 

 

 

 

 

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