Journal of Pharmaceutical Research

Yadav Mithlesh ¹, Maheshwari Monika ¹, Vaishali ², Arvind Kumar ², Pathak Devender ¹

Affiliations
1 Rajiv Academy for Pharmacy, Delhi-Mathura Highway, Chhattikara-281006, Mathura, IN
2 S. D. College of Pharmacy & Vocational Studies, Muzaffarnagar, (U.P.), IN

Abstract

Equimolar quantity of 2-aminothiophenol and ethylchloroacetate was condensed and the solid mass obtained was refluxed. The compound obtained was refluxed with 4-aminoacetophenone to produce 3(4'-acetylphenylamino) 1,4-benzothiazine. The 3(4'-acetylphenylamino)1,4-benzothiazine was reacted with corresponding aldehyde to give 3[4'-(3"-substituted-2"-propenone-1"-yl) phenylamino]1,4-benzothiazine. The above synthesized compounds and guanidine nitrate were refluxed to afford 3[4'(2"-amino-4"- substituted-phenyl)-pyrimidine-4"yl)phenylamino]1,4-benzothiazine. The structures of the newly synthesized compounds were elucidated on the basis of elemental analysis, FTIR and 1H-NMR and have been screened for antimicrobial activity.

Keywords

1, 4-Benzothiazine, Spectral Analysis, Antibacterial, Antifungal.

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Gupta Mohit ¹, Minu Manninder ², Pathak Devender ¹

Affiliations
1 Department of Pharmaceutical Chemistry, Rajiv Academy for pharmacy, Mathura, N.H. #2 Delhi-Mathura Bye-pass, Chhatikara, Mathura-281006, Uttar Pradesh, IN
2 Department of Chemistry, Faculty of Science, Dayal Bagh Educational Institute, Dayal Bagh, Agra - 282110 (U.P.), IN

Abstract

The reaction of l-Proline with hydrazine hydrate (99%) in the presence of conc. sulfuric acid gave pyrrolidine- 2-carbohydrazide (I). The reaction was carried out by both conventional and microwave method. Compound I on treatment with substituted aromatic aldehydes furnished the corresponding schiff's bases (1a-10a), which on further reaction with mercaptoacetic acid yielded N-(4'-Oxo-2'-substituted phenylthiazolidin-3'- yl)pyrrolidine-2-carboxamide (1b-10b). The structures of these compounds were confirmed by UV, FTIR, ¹H NMR, ESI-mass spectra and elemental analysis. All the synthesized compounds were screened for antimicrobial activity against variety of bacterial and fungal strains. The compounds 3b, 6b and 8b showed maximum antibacterial activity against B.subtilis and S.aureus, 2b and 10b against E.coli and P.aeruginosa and compounds 3b, 7b and 8b showed the maximum antifungal activity against C. albicans and A. niger.

Keywords

Hydrazide, Schiff's Bases, Thiazolidin-4-Ones, Antimicrobial.

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Pathak Devender ¹, Sharma Neha ¹

Affiliations
1 Department of Pharmaceutical Chemistry, Rajiv Academy for Pharmacy, Mathura - 281001 (U.P.), IN

Abstract

A number of substituted chalcones (1a-1o) were synthesized by the reaction of substituted benzaldehyde and substituted acetophenone in presence of ethanolic sodium hydroxide solution. On further treating these substituted chalcones (1a-1o ) with urea in alkaline medium, yielded a series of 4,6 disubstituted pyrimidine-2-one derivatives (2a-2o). The structures of the newly synthesized compounds have been established on the basis of IR, ¹H-NMR, MS (ESI) data and elemental analysis. All the compounds were screened for their analgesic activity by Acetic acid induced writhing method and anti-inflammatory activity by Carrageenan induced hind paw oedema assay.

Keywords

Pyrimidine, Chalcones, Analgesic Activity, Anti-Inflammatory Activity.

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Dabas Rohit ¹, K. S. Hareen ¹, Yadav Mithlesh ¹, Pathak Devender ¹

Affiliations
1 Department of Pharmaceutical Chemistry, Rajiv Academy for Pharmacy, Mathura, Delhi-Mathura Highway, Chhattikara-281006, (U.P.), IN

Abstract

Present work deals with the synthesis, characterization and cytotoxic screening of novel substituted pyrazole derivatives. Different acetophenones (I) with various substituted aromatic aldehydes (II) were condensed into corresponding chalcones (1_a-e), which upon bromination gave chalcone dibromides (2_a-e). The treatment of 2_a-e with hydrazine hydrate, phenylhydrazine and 2,4-dinitrophenylhydrazine in the presence of TEA (triethanolamine) afforded different di and tri-phenyl substituted novel pyrazoles (3_a-d and 4_a-h). All the newly synthesized compounds were characterized by UV, FTIR, ¹H NMR, mass spectral analysis and elemental analysis. All the compounds were screened for anticancer activity against A549 cell line by SRB assay. Compounds 3_d, 4_b, 4_d, 4_f and 4_h showed promising cytotoxic potential.

Keywords

Cytotoxicity, Chalcone Dibromides, Pyrazole, SRB, Anticancer, A549 Cell Line.

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