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Synthesis and biological study of novel 5-{(4-(6,7-dihydrothieno-[3,2-c]pyridin-5(4H)-ylsulfonyl)phenylamino)-methyl)-quinolin-8-ol and its metal complexes

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Chinese Chemical Letters 2011年第11期22卷 1297-1300页

作者： Paresh n.patel Khyati D.patel Hasmukh S.patel Department of Chemistry Sardar patel University Vallabh VidyanagarGujarat 388120India

A novel 5-（（4-（6,7-dihydrothieno[3,2-c]pyridin-5（4H）-ylsulfonyl）phenylamino）methyl）quinolin-8-ol（HTPSMQol） was synthesized by optimized reaction of 4-（6,7-dihydrothieno[3,2-c]pyridin-5（4H）-ylsulfonyl）aniline with 5-chloromethyl-8-hydroxy-quinoline hydrochloride（CMHQ）.Also complexes of HTPSMQol were prepared by using various M（Ⅱ） metal *** compounds were analyzed by spectroscopic techniques and screened against various strains of *** results showed higher antimicrobial activity of HTPSMQol compared to its metal complexes and comparable with Ciprofloxacin.

关键词： 4 5 6 7-Tetrahydrothieno[3 2-c]pyridine(THTPs) 8-Hydroxyquinoline(8HQs) Sulfonamide Antimicrobial activity

Synthesis of some novel divalent transition metal complexes as antimicrobials

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Chinese Chemical Letters 2011年第8期22卷 935-938页

作者： Kaushal K.Oza Paresh n.patel Hasmukh S.patel Department of Chemistry.Sardar patel University.Vallabh Vidyanagar 388120 GujaratIndia

A novel series of transition metal complexes have been synthesized from the reaction of 5-（（3-（methylthio）-5-（pyridin-4-yl）-4H- 1,2,4-triazol-4-ylamino）melhyl）quinolm-8-ol with transition metal *** structures of these compounds have been elucidated by elemental and spectral ***,compounds were screened for in vitro antimicrobial activity against the representative panel of two Gram-positive and two Gram-negative bacteria and two strains of *** various compounds show potent inhibitory action against test organisms.

关键词： 4-Amino-5-mercapto-1 2 4-tria/oles 8-Hydroxyquinoline Spectroscopic studies Antimicrobial activity

Determination of asenapine in presence of its inactive metabolites in human plasma by LC-MS/MS

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Journal of Pharmaceutical Analysis 2018年第5期8卷 341-347页

作者： nirav R patel Mallika Sanyal naveen Sharma Dinesh S.patel Pranav S.Shrivastav Bhavin n.patel Bioanalytical Laboratory Uiantha Research India Ltd.BodakdevAhmedabad 380054GujaratIndia Kadi Sarva Viswavidyalaya Sector-15Ghandhinagar 382715GujaratIndia Department of Chemistry St.Xavier's CollegeNavrangpuraAhmedabad 380009GujaratIndia Department of Chemistry School of SciencesGujarat UniversityNavrangpuraAhmedabad 380009GujaratIndia

A highly selective and sensitive liquid chromatography-tandem mass spectrometry （LC-MS/MS） assay has been described for the determination of asenapine （ASE） in presence of its inactive metabolites n-desmethyl asenapine （DMA） and asenapine-n-glucuronide （ASG）. ASE, and ASE 13C-d3, used as internal standard （IS）, were extracted from 300 μL human plasma by a simple and precise liquid-liquid extraction procedure using methyl tert-butyl ether. Baseline separation of ASE from its inactive metabolites was achieved on Chromolith Performance RPse （100 mm ×4.6 mm） column using acetonitrile- 5.0 mM ammonium acetate-10% formic acid （90：10：0.1, v/v/v） within 4.5 min. Quantitation of ASE was done on a triple quadrupole mass spectrometer equipped with electrospray ionization in the positive mode. The protonated precursor to product ion transitions monitored for ASE and ASE 13C-d3 were m/z 286.1 → 166.0 and m/z 290.0 → 166.1, respectively. The limit of detection （LOD） and limit of quantitation （LOQ） of the method were 0.0025 ng/mL and 0.050 ng/mL respectively in a linear concentration range of 0.050-20.0 ng/mL for ASE. The intra-batch and inter-batch precision （% CV） and mean relative recovery across quality control levels were 〈 5.8% and 87.3%, respectively. Matrix effect, evaluated as IS-normalized matrix factor, ranged from 1.03 to 1.05. The stability of ASE under different storage conditions was ascertained in presence of the metabolites. The developed method is much simpler, matrix free, rapid and economical compared to the existing methods. The method was suc- cessfully used for a bioequivalence study of asenapine in healthy Indian subjects for the first time.

关键词： Asenapine Asenapine 13C-d3 Metabolites LC-MS/MS Bioequivalence study Human plasma

Highly sensitive LC–MS/MS method to estimate doxepin and its metabolite nordoxepin in human plasma for a bioequivalence study

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Journal of Pharmaceutical Analysis 2018年第6期8卷 378-385页

作者： nirav P.patel Mallika Sanyal naveen Sharma Dinesh S.patel Pranav S.Shrivastav Bhavin n.patel Bio-Analytical Laboratory Cliantha Research India Ltd.BodakdevAhmedabad 380054GujaratIndia Kadi Sarva Viswavidyalaya Sector-15Ghandhinagar 382715GujaratIndia Department of Chemistry St.Xavier's CollegeNavrangpuraAhmedabad 380009GujaratIndia Department of Chemistry School of SciencesGujarat UniversityNavrangpuraAhmedabad 380009GujaratIndia

A selective, sensitive and rugged liquid chromatography–tandem mass spectrometry(LC–MS/MS) assay has been developed for the simultaneous determination of doxepin(Dox) and its pharmacologically active metabolite, nordoxepin(nDox) in human plasma. The analytes and their internal standards(IS)were extracted from 500 m L of human plasma by liquid-liquid extraction using methyl tert-butyl *** separation was achieved on Hypurity C8 column(100 mm ? 4.6 mm, 5 mm) using a mixture of acetonitrile-methanol(95:5, v/v) and 2.0 mM ammonium formate in 93:7(v/v) ratio. Detection was accomplished by tandem mass spectrometry in the positive ionization and multiple reaction monitoring acquisition mode. The protonated precursor to product ion transitions studied for Dox, nDox,and their corresponding ISs, propranolol and desipramine, were m/z 280.1-107.0, 266.0-107.0,260.1-116.1 and 267.1-72.1, respectively. A linear dynamic range of 15.0–3900 pg/mL for Dox and 5.00–1300 pg/mL for nDox was established with mean correlation coefficient(r2) of 0.9991 and 0.9993, respectively. The extraction recovery ranged from 86.6%–90.4% and 88.0%–99.1% for Dox and nDox, respectively. The intra-batch and inter-batch precision(% CV) across quality control levels was r 8.3% for both the analytes. Stability evaluated under different storage conditions showed no evidence of degradation and the % change in stability samples compared to nominal concentration ranged from 4.7% to12.3%. The method was successfully applied to a bioequivalence study of 6 mg doxepin hydrochloride orally disintegrating tablet in 41 healthy Indian subjects under fasting and fed conditions.

关键词： Doxepin nordoxepin LC–MS/MS Liquid-liquid extraction Human plasma Bioequivalence study

Role of aberrant Sonic hedgehog signaling pathway in cancers and developmental anomalies

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The Journal of Biomedical Research 2022年第1期36卷 11-19页

作者： Trupti n.patel Pavan Kumar Dhanyamraju School of Biosciences and Technology Vellore Institute of TechnologyVellore CampusVelloreTamil Nadu 632014India Department of Pharmacology Penn State University College of MedicineHersheyPA 17033USA Penn State Cancer Institute HersheyPA 17033USA.

Development is a sophisticated process maintained by various signal transduction pathways,including the Hedgehog(Hh)*** important functions are executed by the Hh signaling cascade such as organogenesis,tissue regeneration,and tissue homeostasis,among various *** the multiple functions carried out by this pathway,any mutation causing aberrant Hh signaling may lead to myriad developmental abnormalities besides *** the present review article,we explored a wide range of diseases caused by aberrant Hh signaling,including developmental defects and ***,we concluded this mini-review with various treatment strategies for Hh-induced diseases.

关键词： cancer developmental anomaly hedgehog signal transduction drug treatment

Melanoma therapeutics: a literature review

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The Journal of Biomedical Research 2022年第2期36卷 77-97页

作者： Pavan Kumar Dhanyamraju Trupti n.patel Department of Pediatrics and Pharmacology Pennsylvania State University College of MedicineHersheyPA 17033USA School of Biosciences and Technology Vellore Institute of TechnologyVellore CampusVelloreTamil Nadu 632014India

Melanoma is a relentless type of skin cancer which involves myriad signaling pathways which regulate many cellular *** makes melanoma difficult to treat,especially when identified *** present,therapeutics include chemotherapy,surgical resection,biochemotherapy,immunotherapy,photodynamic and targeted *** interventions are usually administered as either a single-drug or in combination,based on tumor location,stage,and patients'overall health ***,treatment efficacy generally decreases as patients develop treatment *** profiling of melanocytes and the discovery of novel molecular factors involved in the pathogenesis of melanoma have helped to identify new therapeutic *** this literature review,we examine several newly approved therapies,and briefly describe several therapies being assessed for *** goal is to provide a comprehensive overview of recent developments and to consider future directions in the field of melanoma.

关键词： cancer melanoma intervention target resistance

Management of pancreaticobiliary disease using a new intra-ductal endoscope:The Texas experience

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World Journal of Gastroenterology 2009年第11期15卷 1353-1358页

作者： Douglas S Fishman Paul R Tarnasky Sandeep n patel Isaac Raijman Texas Children’s Hospital Section of Pediatric Gastroenterology and NutritionBaylor College of Medicine6621 Fannin StreetHoustonTX 77030United States Digestive Health Associates Methodist Pavilion II 221 West Colorado Blvd.DallasTX 75208-2359United States Division of Gastroenterology and nutrition The University of Texas Health Science Center at San Antonio7703 Floyd Curl Drive San AntonioTX 78229-3900United States Digestive Associates of Houston 6620 Main Street.HoustonTX 77030United States

AIM:To evaluate a new single-operator mini-endoscope, Spyglass,for its performance,feasibility and safety in the management of pancreaticobiliary disease. METHODS:In a multicenter retrospective analysis of patients undergoing intraductal endoscopy,we evaluated 128 patients(71 men,mean age 57.6 years).Indications were therapeutic(TX)in 72(56%) and diagnostic(DX)in 56(44%). RESULTS:Peroral endoscopy was performed in 121 and percutaneous in *** indications included CBD stones in 41,PD stones in six,and biliary strictures in *** indications included abnormal LFT’s in 15, abnormal imaging in 38 and cholangiocarcinoma staging in *** of the stone(s)was considered good in 31,fair in six,and poor in four. Advancement of the electrohydraulic lithotripsy probe was not possible in three patients and proper targeting of the lesion was partial in four patients.A holmium laser was used successfully in three *** clearance was achieved in 37 patients after one procedure and in four patients after two *** of biliary strictures was modified in 20/29 and confirmed to be malignant in 10/*** the modified patients,no diagnosis was available in *** demonstrated malignancy in 8/17 and non-malignancy in *** pathology by imaging studies and abnormal LFT’s was modified in 43/63(66%).Staging of cholangiocarcinoma demonstrated multicentric cholangiocarcinoma in 2/*** was no morbidity associated with the use of Spyglass. COnCLUSIOn:Spyglass Spyscopeis a first generation, single operator miniature endoscope that can evaluate and treat various biliary and pancreatic tract diseases.

关键词： Intra-ductal endoscopy Choledochoscopy Cholangiopancreatoscopy Endoscopic retrogradecholangiopancreatography Biliary disease Sclerosingcholangitis Cholangiocarcinoma Lithotripsy Pancreaticdisease Spyglass

Exploring nationally and regionally defined models for large area population mapping

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International Journal of Digital Earth 2015年第12期8卷 989-1006页

作者： A.E.Gaughan F.R.Stevens C.Linard n.n.patel A.J.Tatem Department of Geography and Geosciences University of LouisvilleLouisvilleKYUSA Biological Control and Spatial Ecology UniversitéLibre de BruxellesBrusselsBelgium Department of Geography and Geoinformation Science George Mason UniversityFairfaxVAUSA Department of Geography and Environment University of SouthamptonSouthamptonUK Fogarty International Center National Institutes of HealthBethesdaMDUSA Flowminder Foundation StockholmSweden

Interactions between humans,diseases,and the environment take place across a range of temporal and spatial scales,making accurate,contemporary data on human population distributions critical for a variety of *** for disaggregating census data to finer-scale,gridded population density estimates continue to be refined as computational power increases and more detailed census,input,and validation datasets become ***,the availability of spatially detailed census data still varies widely by *** this study,we develop quantitative guidelines for choosing regionally-parameterized census count disaggregation models over country-specific *** examine underlying methodological considerations for improving gridded population datasets for countries with coarser scale census data by investigating regional versus country-specific models used to estimate density surfaces for redistributing census *** is given to the spatial resolution of input census data using examples from East Africa and Southeast *** suggest that for many countries more accurate population maps can be produced by using regionally-parameterized models where more spatially refined data exists than that which is available for the focal *** study highlights the advancement of statistical toolsets and considerations for underlying data used in generating widely used gridded population data.

关键词： human population modeling random forest regression dasymetric mapping gridded population datasets

Synthesis and Microbial Studies of new Pyridine Derivatives-Ill

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Chinese Journal of Chemistry 2007年第9期25卷 1363-1369页

作者： patel, n. B. AGRAVAT, S. n. Department of Chemistry Veer Narmad South Gujarat University Surat-395 007 Gujarat India

2-Amino substituted benzothiazole 4a--4I and p-acetamidobenzenesulfonyl chloride 2 were used to prepare 2-（p-aminophenylsulfonamido） substituted benzothiazole 6a--6I using mixture of pyridine and acetic anhydride which formed an electrophilic complex （n-acetyl pyridinium） to facilitate condensation to give desired product by removal of HC1. 2-{p-[（3-Carboxypyrid-2-y1）amino]phenylsulfonamido}benzothiazoles 8a--81 were synthesized from 2-chloropyridine-3-carboxylic acid 7 and 6a--6I in 2-ethoxy ethanol using Cu-powder and K2CO3. Acid chlorides 9a--91 were condensed with 2-hydroxyethyl piperazine 10 and 2,3-dichloropiperazine 11 for amide deriva- tives 2-（p-（（3-（4-（2-hydroxyethy1）piperazin-1-ylcarbonyl）pyrid-2-y1）amino）phenylsulfonamido）benzothiazoes 12a -121 and 2-{p-[3-（2,3-dichloropiperazin-l-ylcarbonyl）pyrid-2-ylamino]phenylsulfonamido}benzothiazoles 13a- 131 respectively. The structures of the new compounds have been established on the basis of their chemical analysis and spectral data （IR, 1↑H nMR and mass）. All the compounds have been screened for their antibacterial and antifungal activities.

关键词： 2-amino substituted benzothiazole antimicrobial 2-chloropyridine-3-carboxylic acid electrophilic 2-ethoxyethanol