Ashish Patel | Parul university (original) (raw)

Papers by Ashish Patel

Diabetes is a group of metabolic diseases which characterized by increased blood glucose level al... more Diabetes is a group of metabolic diseases which characterized by increased blood glucose level along with polyuria, polydipsia and polyphagia. Protein tyrosine phosphatases (PTPs) are responsible for selective dephosphorylation of tyrosine residues and regulate a wide variety of cellular processes. Protein tyrosine phosphatase 1B (PTP1B) is implicated as a key negative regulator of the insulin and leptin signal-transduction pathways. PTP1B inhibitors have emerged as attractive and potent pharmaceutical agents for the treatment of type-2 diabetes, obesity as well as in cancer therapy. As per literature survey and referred patients, the various derivatives of 4-carboxy benzamide were prepared and confirmed by Mass, NMR, IR and by their physiochemical data. The anti diabetic activity of the synthesized compounds was tested against streptozotocin induce diabetic model. Among them 4-(3-(4-methyl phenyl)-2-(piperazine-1-yl) acrylamido) benzoic acid and 4-(3-(4-methyl phenyl)-2-(piperidine-1-yl) acrylamido) benzoic acid was more active due to presence of methyl group presence in para position and increase compound stability by lipophilic binding with enzyme while other methoxy derivatives of 4-carboxy benzamide shows moderate active due to less liphophilic binding with PTP 1B enzymes.

The global epidemic of obesity and type-2 diabetes mellitus (T2DM) has highlighted the need for n... more The global epidemic of obesity and type-2 diabetes mellitus (T2DM) has highlighted the need for new therapeutic approaches. The association of insulin resistance with these disorders and the knowledge that insulin receptor signaling is mediated by tyrosine (Tyr) phosphorylation has generated great interest in the regulation of the balance between Tyr phosphorylation and dephosphorylation. Several proteins Tyr phosphatases (PTPs) have been implicated in the regulation of insulin action, with the most convincing data for PTP1B. Protein tyrosine phosphatases (PTPs) constitute a large family of enzymes which are crucial modulators of cellular phosphorylation events. Recent studies have demonstrated that loss of protein tyrosine phosphatase-1B (PTP1B) activity resulted in enhancement of insulin sensitivity in addition to decrease in susceptibility to diet-induced obesity, specific PTP1B inhibitors have been developed as therapeutic
agents in type-2 diabetes and obesity and cancer also. A conformational change that is restricted to the movement of a flexible loop occurs during the catalytic cycle of the PTPases. However, the relationship between loop dynamics and enzyme catalysis remains to be established. The nature and identity of the rate-limiting step in the PTPases catalyzed reaction requires further investigation and may be dependent on the specific experimental conditions such as temperature, pH, buffer, and substrate used.

The objective of research work was to evaluate and perform stability study of prepared and develo... more The objective of research work was to evaluate and perform stability study of prepared and developed Sennoside A
and B capsule. The Sennoside A and B capsule was successfully develop by adding optimum necessary active
ingredient and all the prepared formulations were evaluated by different methods such as HPLC and dissolution
study Moreover, stability study was performed as per ICH guidelines. All five formulations were identified by
chromatogram of HPLC as well as performing dissolution and disintegration study. In addition to, organoleptic
qualitative and quantitative evaluation of calcium sennoside was carried by consideration of its pH, loss on drying,
tapped density, ash value and its assay. The results obtained in this research work clearly indicated that out of all
five formulation, formulation IV significantly increased the frequency and wet weight of stools to 31.5 ± 4.25 and
8.29 ± 1.21 g, and showed tendency to increase the frequency and wet weight of stools. The frequency and the wet
weight of stools following gum arabic for 14 days were 16.3±3.98 and 4.79±1.14 g respectively.
Key words: Sennoside capsule, Formulation, ICH, Stability study
_____________________________________________________________________

Diabetes is a metabolic disorder wherein blood glucose level is increased along with some other a... more Diabetes is a metabolic disorder wherein blood glucose level is increased along with some other abnormal
conditions like polyuria, polydipsia and polyphagia. As per WHO estimation, 380 million people will become
diabetic by 2025. Tyrosine residues are selectively dephosphorylated by Protein tyrosine phosphatases (PTPs) and
thus a wide variety of cellular processes are regulated by their action. Protein tyrosine phosphatase 1B (PTP1 B)
has shown to be a negative regulator in the insulin signaling pathways. Recent gene knockout studies carried out on
mice portrays PTP1B as an effective target for drug discovery process related to anti-diabetic and anti-obese
agents. PTPs are also involved in several other disorders like cancer. The structure of compounds synthesized by
the present method were confirmed by TLC, IR, NMR and Mass spectroscopy. The anti-diabetic activity of the
synthesized compounds were tested against PTP1B enzyme by using Calbiochem® PTP1B colorimetric assay kit.
Among all synthesized compounds 4c, 4d, 4e, 4f had shown promising anti-diabetic activity, while other compounds
have shown lesser potency as anti-diabetic agent.

A Fourier transform infrared (FT-IR) spectrometric method was developed for the rapid and direct ... more A Fourier transform infrared (FT-IR) spectrometric method was developed for the rapid and direct measurement
of Cilnidipine in pharmaceutical drugs. Cilnidipine is newly discovered and very effective antihypertensive
drug. Cilnidipine can be determined by various methods and now we are adding a new one that uses a Fourier
transform infrared spectrophotometric technique. The method involves the measurement of absorbance of
carbonyl group (C=O) peak at 1697 cm-1. The proposed method was validated for pharmaceuticals in tablet form
and %RSD was found to be less than two with recovery levels 99.8-102.5 and 99.8- 101.4 as per absorbance and
peak area respectively.
Keywords: FT-IR, Cilnidipine, Carbonyl peak, Tablet formulation, FTIR

In the present study From the literature survey carried out it was planned to synthesize new Schi... more In the present study From the literature survey carried out it was planned to synthesize new Schiff base 2-Substituted-3-(pyridin-
4-ylmethyleneamino) quinazolin-4-(3H)-one (01, 02, 03). This series of compounds was synthesised using anthranilic acid,
different acetyl/benzoyl chloride, pyridine-4-aldehyde and absolute alcohol as a solvent under cooling condition (0-5 C), stirring o
and condensation. All the compounds synthesized were characterized by IR, NMR and MASS Spectra. The synthesized
compoundswere tested for their In vitro antibacterial activity against theGram-positive bacteria Staphylococcus aureus (ATCC-
29213) and Gram-negative bacteria Escherichia coli (ATCC-8739) and antifungal activity against Candida albicans (ATCC-
29213) compared to parent drugs Ampicillin and Fluconazole at same concentration. Compound 02 exhibited maximum
antibacterial activity and also exhibited optimum antifungal activity

Among medicinal plants, Moringa oleifera Lam. has been recommended for several disorders in folk ... more Among medicinal plants, Moringa oleifera Lam. has been recommended for several disorders in folk medicine.
Indian Materia Medica describes the use of roots of Moringa oleifera Lam in the treatment of a number of
ailments, including asthma, gout, lumbago, rheumatism, enlarged spleen or liver, etc. Nevertheless, no pharmacological
studies of Moringa oleifera Lam root have thus far evaluated for its anti diarrheal activity.
Thus the purpose of the present study is to evaluate scientifically the effect of hydroalcoholic (50:50) extract
of root of Moringa oleifera Lam against castor oil induced diarrhea models in rats. The parameters used for
the evaluations are the decrease in severity and frequency in diarrheas caused due to castor oil, futher to understand
the probable mechanism of its anti-diarrhoeal activity, its effect was evaluated on intestinal transit, castor
oil induced intestinal fluid accumulation (enteropooling) and electrolyte concentration in the small intestinal
fluid. The methanolic root extract of Moringa oleifera Lam 200 (p<0.01)and 400 mg/kg (p<0.001)produced a
significant reduction in the severity and frequency of diarrhea, intestinal fluid accumulation, the volume of intestinal
content and intestinal transit compared to normal saline control group, dose dependently more than atropine(
3mg/kg i.p). This signifies the usefulness of this model and the clinical effect of the extract.
Moringa oleifera Lam root extract may be useful in a wide range of diarrheal states due to both disorders of
transit e.g.functional diarrhoeas, radiation diarrhea or due to abnormal secretory mechanisms like in cholera or
E.coli entero-toxin induced diarrhea. Further studies are necessary for chemical characterization of the active
principles and more extensive biological evaluations.

Since long time, quinazoline and their derivatives are found to be active for the synthesis of va... more Since long time, quinazoline and their derivatives are found to be active for the synthesis of various categories of drugs. The 2, 3-di-substituted quinazolin-4-(3H)-ones (III) and its derivatives have been synthesized as a one pot procedure from the reaction of Anthranilic acid (I), acid chlorides and different primary amines with the intermediate 4-(3H)-benzoxazinone (II) at different microwave conditions. High yield, less by products, short reaction time (7 to10 min), mild conditions and easy workup are the advantages of this methodology. The pure compounds are separated through the preparative TLC method and using hydro-alcoholic solution. The final derivatives are characterized by UV, IR, Mass, NMR and screened for antimicrobial and antibacterial activity.