Y. Rajendra Prasad

Synthesis and pharmacological evaluation of clubbed isopropylthiazole derived triazolothiadiazoles, triazolothiadiazines and mannich bases as potential antimicrobial and antitubercular agents.

A series of novel clubbed Isopropylthiazole derivatives triazolothiadiazines 2a-g, dihydro triazolothiadiazoles 3a-g, thioxotriazoles 4a-d, triazolothiadiazole 5, arylideneamino triazolethiones 7a-h and oxadiazolethiones 11a-b were synthesized and characterized by IR, (1)H NMR, (13)C NMR, elemental and mass spectral analysis. These compounds were evaluated for their preliminary in vitro antibacterial, antifungal and antitubercular activity against Mycobacterium tuberculosis H(37)Rv strain by broth dilution assay method. All the compounds exhibited moderate to significant antibacterial and antifungal activities. Results of the antitubercular screening against M. tuberculosis H(37)Rv showed compounds 7c and 7d exhibited good antitubercular activity (MIC 4 and 8 μg/mL) respectively, when compared with first line drug such as isoniazid (0.25 μg/mL).

Synthesis and Antimicrobial Activity of Some Chalcone Derivatives

In an effort to develop antimicrobial agents, a series of chalcones were prepared by Claisen-Schmidt condensation of appropriate acetophenones with appropriate aromatic aldehydes in the presence of aqueous solution of potassium hydroxide and ethanol at room temperature. The synthesized compounds were characterized by means of their IR, 1H-NMR spectral data and elemental analysis. All the compounds were tested for their antibacterial and antifungal activities by the cup plate method.

Synthesis and Antimicrobial Activity of Some New Chalcones of 2-Acetyl Pyridine

Six new chalcones were synthesised by condensing 2-acetyl pyridine with aldehyde derivatives in dilute ethanolic potassium hydroxide solution at room temperature according to Claisen-Schmidt condensation. All these compounds were characterised by means of their IR, 1 H NMR spectroscopic data and microanalyses. The antimicrobial activity of these compounds was evaluated by the cup plate method.

Synthesis and evaluation of some novel isochroman carboxylic acid derivatives as potential anti-diabetic agents

A series of novel isochroman mono-carboxylic acid derivatives were synthesized, characterized and evaluated for their ability to inhibit protein tyrosine phosphatase 1B (PTP1B) in vitro in order to use them as potential anti-diabetic agents. Analysis of structure-activity relationships led to the identification of potent compound 4n which inhibited PTP1B with IC(50) value of 51.63+/-0.91 nM. In general, high potency was associated with a dithiolane ring with a spacer of five carbons to the isochroman ring. Compound 4n has been selected for in vivo evaluation as drug candidate for anti-diabetic activity.

Synthesis and evaluation of some novel dibenzo[b,d]furan carboxylic acids as potential anti-diabetic agents

A series of novel dibenzo[b,d]furan mono-carboxylic acid derivatives were synthesized, characterized and evaluated for their ability to inhibit Protein Tyrosine Phosphatase 1B (PTP1B) in vitro in order to use them as potential anti-diabetic agents. Structure-activity relationship study led to the identification of potent compound 5 E which inhibited PTP1B with IC(50) value of 82+/-0.43 nM. Compound 5 E was screened in vivo as drug candidate for anti-diabetic activity using rosiglitazone maleate as the standard. Compound 5 E showed significant reduction in body weight, fed-state whole blood glucose (WBG), fasting WBG, plasma glucose and plasma cholesterol levels and non-significant reduction in fasting plasma triglyceride levels in ob/ob mice.

A prenylated flavanone from Tephrosia maxima

Abstract A new flavanone, maxima flavanone A, was isolated from the chloroform extract of the roots of Tephrosia maxima along with maxima isoflavone J and t

Prenylated flavonoids from Tephrosia spinosa

Abstract The isolation and characterization of a new chalcone, spinochalcone C, and two new flavanones, spinoflavanones A and B, from various parts of Tephrosia spinosa are reported in addition to the known flavanone, fulvinervin A.

Two chalcones from Tephrosia spinosa

Abstract Chemical examination of the petroleum and chloroform extracts of the roots of Tephrosia spinosa has yielded two new chalcones, spinochalcones A and B, in addition to the known chalcone flemistrictin A.

Two prenylated flavanones from Mundulea suberosa

Abstract Two new prenylated flavanones, mundulea flavanones A and B, were isolated from the chloroform extract of stembark of Mundulea suberosa along with the previously reported compounds munetone, mundulone and mundulea lactone. Their structures were established by spectral data as 4′-hydroxyisoderricin and 7-methyl-4′-hydroxyglabranin

Synthesis and biological evaluation of novel 4,5-dihydropyrazole derivatives as potent anticancer and antimicrobial agents

A focused library of 4,5-dihydropyrazole dervivatives (4, 5, 6, 7a–h, 8, 9a–g, and 10a–g) were synthesized from novel 5-(2,6-difluorophenyl)-3-phenyl-4,5-dihydropyrazole-1-carbothioamide 4. The synthesized compounds were characterized using elemental analysis and spectral data (IR, mass spectra, 1H and 13C NMR) and evaluated for antimicrobial activity by broth dilution method and in vitro anticancer activity. Among the synthesized compounds 7a, 9c, 9g, and 10d exhibit broad spectrum antimicrobial activity against tested microbial strains. The in vitro cancer results ascertain 7a, 9c, and 10d are most potent molecules in comparison to reference standard cisplatin.