Rupesh Dudhe

Thiazoles: having diverse biological activities

In the last few decades, a lot of work has been done on thiazole ring to find new compounds related to this scaffold to act as antioxidant, analgesic, anti-inflammatory, antimicrobial, antifungal, antiviral, diuretic, anticonvulsant, neuroprotective, and antitumor or cytotoxic drug molecules with lesser side effects. This review presents the up to date development on the design and development of different thiazole derivatives.

Free radical scavenging properties of pyrimidine derivatives

Free radicals are well known for playing a dual role in our body- deleterious as well as beneficial. It includes a metabolic pathway for its generation. Oxidative stress in our body occurs due to excessive generation of free radicals and reduced level of antioxidants, but at low concentrations, these radicals help to perform normal physiological functions of the body. Scientific evidence suggests that antioxidants reduce the risk for chronic diseases including cancer and heart disease. This review shows current tendency in the pyrimidine synthesis and reveals the pyrimidine core to be a very potent moiety which can be a rich source for the synthesis of new compounds having desirable antioxidant activity.

Insignificant anticancer activity of novel substituted pyrimidine derivatives

Background: Pyrimidine and fused pyrimidine derivatives play an important role in therapeutic strategies. It is known to be most prominent structures found in nucleic acid, including uracil, thymine, cytosine, adenine, and guanine, which are fundamental building blocks for deoxyribonucleic acid (DNA) and ribonucleic acid (RNA). Materials and Methods: A series of 3-[2-amino-6-(substituted)-pyrimidin-4-yl]-6-(substituted)-2H-chromen-2-one derivatives were prepared by reacting salicylaldehyde with ethylacetoacetate in the presence of piperidine by Knoevenagel reaction as a starting material. The chemical structures were confirmed by means of FTIR (Fourier Transform InfraRed Spectrophotometer-8400S), 1H NMR, and elemental analysis. The data of these synthesized compounds were submitted to National Institute of Health, USA, under the drug discovery program of NCI (National Cancer Institute) and screened for anticancer activity at a single high dose (10−5 M) in full NCI 60 cell lines. Results: Unfortunately, the selected compounds have not shown any potent significant anticancer activity in the NCI 60 cell line screening. Conclusion: The compound (T2) found to be most efficient anticancer activity with selective influence on breast cancer cell lines, especially on MCF7 cell line with a growth percentage of 33.63.

Pyrimidine containing furanose derivative having antifungal, antioxidant, and anticancer activity

Background A series of 6-(substituted aldehyde)-3,4-dihydro-1-(tetrahydro-3,4-dihydroxy-5-(hydroxymethyl) furan-2-yl)-4-phenylpyrimidine-2(1H)-one derivative (6A-6P) was synthesized from the 6-(substituted aldehyde)-4-phenylpyrimidine-2(1H)-one derivative (5A-5P) through following reaction mechanisms Claisen-Schmidt, Cyclization, and Satos fusion. The structures of the synthesized compounds were elucidated by I.R.,1H-NMR, elemental analysis, and mass spectroscopic techniques. Result The synthesized compounds were screened for in vitro antifungal activity at 25, 50, 100, and 200 μg/ml concentrations. Among them, compounds 6P, 6D, and 6M exhibited significant antifungal activity that was carried out by cup plate method against fungal strain which was collected from IMTECH Chandigarh, India, against standard drug fluconazole. Compounds have been further evaluated by measuring zone of inhibition and percent inhibition. The synthesized compounds were screened for in vitro antioxidant activity using the DPPH assay, based on the AAI and antioxidant activity unit (AAU), using a combination relation between DPPH concentration and absorbance. The antioxidant strength of compounds was compared against ascorbic acid. Among them, compounds 6K, 6F, 6E, 6G, 6H, and 6M exhibited significant antioxidant activity and 6J have less active compound. The data of these synthesized compounds were submitted to the National Institute of Health, USA, under the drug discovery program of National Cancer Institute (NCI) and screened for anticancer activity at a single high dose (10−5 M) in full NCI 60 cell lines. The selected compounds have shown potent significant anticancer activity in the NCI 60 cell line screening. Conclusion A new series of pyrimidine analogues that contain furanose moiety were synthesized by Satos fusion and characterized. The synthesized compounds screened for their in vitro antioxidant, antifungal activity, as well as anticancer activity given by the derivative which has chloro, methoxy, nitro, and chloro substitution having furanose contain pyrimidine derivative that showed the most potent activity. Electronic supplementary material The online version of this article (doi:10.1186/s13588-014-0003-0) contains supplementary material, which is available to authorized users.

Absence of antidiabetic activity in some novel thiazolidinone derivatives

Aim: It was aimed to synthesise some novel thiazolidinone derivatives and assess them for antidiabetic activity. Material and Methods: A series of substituted 5-ethylidene-2-(phenylimino) thiazolidin-4-ones were prepared by using phenylthiourea (I) as a starting material. Phenylthiourea on reaction with ethylchloroacetate, in the presence of ethanol and fused sodium acetate, gave 2-(phenylimino) thiazolidin-4-one (II), and 2-(phenylimino) thiazolidin-4-one on further reaction with substituted benzaldehyde gave substituted 5-ethylidene-2- (phenylimino) thiazolidin-4-one (III - XVIII). The synthesized compounds were authenticated on the basis of elemental analysis, IR, 1H NMR, and Mass spectral analysis and some of the compounds were selected on the basis of a literature review, to evaluate them for their antidiabetic activity. Results and Conclusion: All The tested compounds 5-(4-fluorobenzylidene)-2-(phenylimino) thiazolidin-4-on (VII) and 5-(4-Methylbenzylidene)-2-(phenylimino)thiazolidin-4-one (X), 5-(2, 4-dinitrobenzylidene)-2-(phenylamino) thiazolidin-4-one (XVII) were found to be ineffective in lowering the blood glucose level.

Discovery of Substituted Hydroxylphenyl Pyrimidine-2(1H) Thione as a New Series of Antioxidant using AAU and AAI Method

A series of substituted pyrimidine has been discovered as a new class of potent antioxidant. 6-(Substituted aldehyde)- 3,4-dihydro-1-(tetrahydro-3,4-dihydroxy-5-hydroxymethyl)furan-2-yl)-4-(4-hydroxyphenyl)pyrimidine-2(1H)-thione derivative (XVII-XXIV) was synthesized from the 6-(Substituted aldehyde) -4-phenylpyrimidine-2(1H)-thione derivative (IX-XVI) through the reaction mechanisms of Claisen-Schmidt, Cyclization and Satos fusion. The structures of the synthesized compounds were elucidated by I.R., 1 H-NMR, elemental analysis and mass spectroscopic techniques. The synthesized compounds were screened for in vitro antioxidant activity using the DPPH assay, based on the AAI and AAU, using a combination relation between DPPH concentration and absorbance. The antioxidant strength of compounds was compared against ascorbic acid. Among them, compounds XVII, XX, XIX and XXIV exhibited significant antioxidant activity, as seen by using the free radical scavenging (DPPH) method. doi: 10.14456/WJST.2015.83