Lala Lajpat Rai Memorial Medical College

Meerut, India

Lala Lajpat Rai Memorial Medical College

Meerut, India
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Masand N.,Lala Lajpat Rai Memorial Medical College | Gupta S.P.,National Institute Of Technical Teachers Training And Research | Khosa R.L.,Bharat Institute of Technology | Patil V.M.,Bharat Institute of Technology
Central Nervous System Agents in Medicinal Chemistry | Year: 2017

Alzheimer’s disease (AD), the most common neurodegenerative disorder and demands to find a way for prevention and delayed onset. The development of therapeutics for AD is based on the amyloid cascade hypothesis (vaccines, β- and γ-Secretase inhibitors), or targeting tau and neurofibrillary tangle formation, neuroinflammation, etc. Cholinesterase, BACE-1, amyloid-β 1-42, γ and β-Secretase, Phosphodiesterase type IV (PDE4) inhibitors are the reported treatment strategies. Among these, the γ- and β-Secretase inhibitors can be clustered in several heterocyclic classes (imidazoles, thiazoles, indoles, benzaldehydes, pyrimidine, etc), with subsequent description of the structure-activity relationships, and extended to the pharmacological profile in order to evaluate their drug-likeness, with special attention to toxicity and bioavailability. This article discusses the approaches proposed by several research groups working on the synthesis of enzyme inhibitors, based on modelling studies and the way these findings were used to obtain new drugs for the treatment of AD. © 2017 Bentham Science Publishers.

Patil V.M.,Bharat Institute of Technology | Gurukumar K.R.,UMDNJ New Jersey Medical School | Chudayeu M.,UMDNJ New Jersey Medical School | Gupta S.P.,Meerut Institute of Engineering and Technology | And 3 more authors.
Medicinal Chemistry | Year: 2012

Hepatitis C virus (HCV) NS5B polymerase is the key replicating protein of the virus and thus an attractive target for drug development. Here we report on the synthesis and biological evaluation of a new series of benzimidazole derivatives as HCV NS5B inhibitors. This yielded compound 6b and 6d bearing 2-(2-benzyloxy)phenyl and 2-(4-methylbenzyloxy)phenyl moieties, respectively, as promising leads. Binding mode of compound 6d in allosteric pocket (AP)-1 of NS5B will form the basis for future structure-activity relationship optimization. © 2012 Bentham Science Publishers.

Sharma S.,ITM University | Saxena K.,Lala Lajpat Rai Memorial Medical College
Indian Journal of Pharmaceutical Sciences | Year: 2014

In an effort to search for more active antiinflammatory agent, a series of pyrazolinylbenzidines and isoxazolylbenzidines was designed, synthesized, and screened for their potential as novel orally inflammation inhibitors. Compounds 4,4'-bis-(1"-acetyl-5"-substitutedaryl-2"-pyrazolin-3"-yl)benzidines (8-13) and 4,4'-bis-(2"-substitutedarylisoxazolin-4'-yl)benzidines (14-19) have been synthesized from 4,4'-bis-(substituted benzylidenyl-acetyl)benzidines (2-7). The structures of the products have been delineated by spectral and elemental analysis. Compounds 2-19 evaluated for antiinflammatory activity and acute toxicity and results are reported. The compound 4,4'-bis-[1"-acetyl-5"-(p-methoxyphenyl)-2"-pyrazolin-3'-yl)benzidine (9) showed more potent and dose-dependent antiinflammatory activity in comparison to reference drug.

Patil V.M.,Subharti University | Masand N.,Lala Lajpat Rai Memorial Medical College | Gupta S.P.,National Institute of Technical Teachers Training and Research
Current Drug Discovery Technologies | Year: 2016

The various reported in silico screening protocols such as molecular docking are associated with various drawbacks as well as benefits. In molecular docking, on interaction with ligand, the protein or receptor molecule gets activated by adopting conformational changes. These conformational changes cannot be utilized to predict the 3D structure of a protein-ligand complex from unbound protein conformations rigid docking, which necessitates the demand for understanding protein flexibility. Therefore, efficiency and accuracy of docking should be achieved and various available/developed protocols may be adopted. One such protocol is GENIUS induced-fit docking and it is used effectively for the development of anti-HCV NS3-4A serine protease inhibitors. The present review elaborates the GENIUS docking protocol along with its benefits and drawbacks. © 2016 Bentham Science Publishers.

Patil V.M.,Bharat Institute of Technology | Masand N.,Lala Lajpat Rai Memorial Medical College | Gupta S.P.,National Institute Of Technical Teachers Training And Research
Current Topics in Medicinal Chemistry | Year: 2016

The developing number of hepatitis C virus infected cases worldwide has threatened people’s health. The available therapeutic options have low specificity, side effects and high rate of drug resistance and thus potentiate the need for novel effective anti-HCV drugs. Agents obtained from natural sources offer an enormous scope of structural diversity and broad therapeutic range of coverage. This review summarizes the research and development of anti-HCV agents (plant extracts/ isolated components) obtained from various natural sources along with the associated mechanism of HCV inhibition. Some of the reported examples include triterpenes, naringenin, Proanthocyanidin, curcumin, Epigallocatechin-3-gallate, quercetin and abrogates having diverse anti-HCV properties. The compiled knowledge regarding anti-HCV agents from natural sources will provide considerable information for developing novel safe and effective anti-HCV drugs. © 2016 Bentham Science Publishers.

Patil V.M.,Subharti University | Gupta S.P.,National Institute Of Technical Teachers Training And Research | Masand N.,Lala Lajpat Rai Memorial Medical College
Current Enzyme Inhibition | Year: 2017

Objective: To investigate the various physicochemical descriptors employed towards biological activity of tyrosine kinase inhibitors. Background: In oncology, kinase domain has emerged as an important pharmacological target. The receptor tyrosine kinases on deregulation (i.e. over expression, chromosomal translocation, gene amplication, mutation) contribute towards development of cancer and thus it has been emerged as potential target in oncology. Method: The available 2D/3D-QSAR methodologies like Hansch analysis, CoMFA, CoMSIA provide the models to correlate biological activity with their 2D/3D descriptors. The identified electrostatic, steric, H-bond, hydrophobic interaction energies involved in ligand-receptor interactions were analyzed. Results: The QSAR models derived for some of the well reported and evaluated tyrosine kinase inhibitors like benzimidazole, pyrido[2,3-d]pyrimidine, quniazolines, quinolines, pyrrolo-pyrimidines, biphenyl amide-based, phenylaminopyrimidine-based, indolinones, and 1,4-dihydroindeno[1,2-c]pyrazole derivatives have found to be useful to investigate the mechanism of tyrosine kinase inhibition. Conclusion: The validated and tested QSAR and 3D-QSAR models for different chemical classes of tyrosine kinase inhibitors have acceptable predictive power. Application: The compiled data on some of the available derived 2D/3D-QSAR models as well as contributing descriptors has utility in understanding structure-activity relationship studies in respect to various endpoints within the chemical series. © 2017 Bentham Science Publishers.

Gupta S.P.,Crossing tech | Samanta S.,Birla Institute of Technology | Masand N.,Lala Lajpat Rai Memorial Medical College | Patil V.M.,Bharat Institute of Technology
Medicinal Chemistry Research | Year: 2013

The k nearest neighbor-molecular field analysis (kNN-MFA) is used to study the correlation between the molecular properties and biological activities of the recently reported 2,5-disubstituted imidazo[4,5-c]pyridines as anti-HCV agents. The most predictive kNN-MFA model derived from the superposition of docked conformations, has good cross-validated q 2 (0.96) and satisfied predictive ability $$ r-{\text{pred}}^{2} $$ (0.88). It could rationalize the HCV inhibitory activity profile of many compounds used in the present study as well as the important structural features responsible for activity. Furthermore, the effects of various structural modifications on biological activity are investigated, and biological activities of novel structures are estimated using the developed 3D QSAR model. © 2012 Springer Science+Business Media, LLC.

Sebastian M.P.,Population Council | Khan M.E.,Population Council | Kumari K.,Lala Lajpat Rai Memorial Medical College | Idnani R.,Lala Lajpat Rai Memorial Medical College
International Perspectives on Sexual and Reproductive Health | Year: 2012

CONTEXT: The Indian family planning program, though successful in increasing contraceptive use among couples who have achieved their desired family size, has not been equally successful in educating couples about the use of contraceptive methods for birth spacing. METHODS: An evaluation was conducted of a behavior change communication intervention integrated into the existing government program to increase knowledge and use of the lactational amenorrhea method and postpartum contraception through counseling by community workers. The intervention, which ran between September 2006 and January 2007, was conducted among 959 pregnant women aged 15-24 who lived in Uttar Pradesh, India. The evaluation used logistic regression analyses to measure differences in knowledge and contraceptive use between baseline and the four- and nine-month postpartum follow-up surveys within and between the intervention and comparison groups. RESULTS: The follow-up data show increases in knowledge of the lactational amenorrhea method and spacing methods and in use of spacing methods. At four months postpartum, women in the intervention group were more likely to know the healthy spacing messages than those in the comparison group (odds ratio, 2.1). At nine months postpartum, women in the intervention group, those with higher knowledge of healthy spacing practices and those with correct knowledge of two or more spacing methods were more likely than others to be using a contraceptive method (1.5-3.5). Use of modern contraceptives for spacing at nine months postpartum was 57% in the intervention group versus 30% in the comparison group. CONCLUSIONS: Targeted behavior change communication using community workers is an effective and feasible strategy for promoting postpartum contraception.

Mithal C.,Lala Lajpat Rai Memorial Medical College
Nepalese journal of ophthalmology : a biannual peer-reviewed academic journal of the Nepal Ophthalmic Society : NEPJOPH | Year: 2011

To evaluate the efficacy of lignocaine 2 % jelly as topical anesthesia in pterygium surgery with conjunctival limbal autograft using fibrin glue. A non-randomized interventional study was carried out including twenty-one patients who presented with primary pterygium. Under 2% lignocaine jelly, surgical dissection of the pterygium, scraping of corneal bed with crescent blade, excision of Tenons capsule, harvesting conjunctival limbal autograft superiorly, and securing it with respect to limbus and stromal orientation with fibrin glue were done. Postoperatively, the patients discomfort and pain were evaluated by Wongs pain scoring system. The mean pain score was 0.70 ± 0.97. Only one patient (4.76%) out of the whole series experienced pain who rated more than three on the visual analog scale of 5. Thirteen patients (61.9%) had pain score of zero, that is, no pain. The surgeons evaluation of the technique in terms of surgical ease and complications was favorable. There were no dislodged grafts and no cases required suturing. There were no cases of infection, significant inflammation, epithelial problems and reduction in visual acuity. There was a single case of recurrence (4.76%) five months postoperatively which was managed conservatively. Conclusions: Topical anesthesia with lignocaine 2% jelly using fibrin sealant is safe and effective in pterygium surgery allowing for short operative times. It results in low pain and good aesthetic and functional outcomes. © NEPjOPH.

Malhotra M.,Lala Lajpat Rai Memorial Medical College
Journal of Laryngology and Otology | Year: 2010

Objectives: Tympanoplasty continues to pose a challenge in developing countries, where treatment cost and lack of compliance with second stage surgery are often important factors in determining the surgical strategy. This study aimed to determine the effectiveness of the newly developed, umbrella autograft. Materials and methods: In 22 patients suffering chronic suppurative otitis media, in whom the incus and stapes suprastructure were found to be absent during surgery, reconstruction was achieved using cartilage-malleus umbrella graft assembly. Six-month post-operative results were evaluated on the basis of average hearing gain, measured at 0.5, 1, 2 and 3kHz.Results: At six months post-operatively, 77.3 per cent of patients showed hearing improvement. Audiography at this time indicated significant improvement (p<0.001), suggesting that this hearing gain may stand the test of time. Conclusion: Umbrella graft tympanoplasty appears to be a promising technique in terms of cost-effectiveness and the autologous nature of implant materials. © JLO (1984) Limited 2010.

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