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Proceedings on 21st World Conference on Pharmaceutical Chemistry and Drug Design
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Journal of Pharmacognosy & Natural Products

ISSN: 2472-0992

Open Access

Proceedings on 21st World Conference on Pharmaceutical Chemistry and Drug Design

Special Issue

Pages: 1 - 1

Editorial note of Proceedings on 21st World Conference on Pharmaceutical Chemistry and Drug Design, December 16, 2020, Webinar

Purcareanu Bogdan

We had a huge success with the completion of 21st World Conference on Pharmaceutical Chemistry and Drug Design on December 16, 2020. The significance of the meeting was achieved due to the accumulation of all the related group of spectators of research scientists to share their Knowledge, Research work, Technologies, and furthermore trade of worldwide Information towards the correct crowd at ideal time. Congress has received a generous response from all over the world. This has been organized with the aim of endorsing the development of new perceptions and ideas for investigating the high level of knowledge reached by scientific community in the field of Pharmaceutical Sciences.

The conference was organized around the theme “Recent Advancements in Drug Design”. The congress entrenched a firm relation of future strategies in the field of Drug Design.

We would like to thank accepted abstracts:

  • Bogdan Purcareanu, University Politehnica of Bucharest, Romania
  • Nadia Youssef Megally Abdo, Alexandria University, Egypt
  • Neelam Sherwani, Sultan Qaboos University, Oman
  • Mark R. Willis, Global Health Authority Agencies
  • Saleh Mohammed Alamri, De Montfort University, UK

We would like to thank each and every participant of Drug Chemistry 2020 webinar to make this a huge success. And special thanks to media partners for the promotion of our event.

The Conference Series Pharmaceutical Conferences aim to bring together the prominent researchers academic scientists, and research scholars to exchange and share their experiences on all aspects of Pharmaceutics. It is conjointly a knowledge domain platform for researchers, practitioners and educators to gift and discuss the foremost recent advances, trends, and issues in addition as sensible challenges and solutions adopted in the fields of Drug Chemistry.

We are also glad to announce our upcoming conference “22nd World Conference on Pharmaceutical Chemistry and Drug Design, September 16-17, 2021, Singapore

The topics to be discussed are Drug Designing, Anti-Cancer Medicinal Chemistry, Pharma Medicinal Chemistry, Chemoinformatic Drug Discovery, Clinical Trials and Regulatory Affairs in Pharmacy and Computer Aided Drug Design-CADD

Special Issue

Pages: 2 - 2

Innovative designs for loaded mesoporous structures and their evaluation in the desorption profiles for chestnut extract

Purcareanu Bogdan

Mesoporous materials attracted great interest in the last decade, for their applications in new drug design fields, especially for drug delivery. Morphology features and the capacity of obtaining tunable structures based on adjustment of the synthesis conditions, besides the lack of toxicity and the biodegradability properties, recommend this type of materials for loading with a great diversity of active molecules. The real challenges represent the obtaining of new materials with various properties and structures and loading with a complex mixture of bioactive compounds from plant extracts. The mesoporous-suport material synthesized is a sophisticated delivery system with significantly improved results on bioavailability and modulation of release kinetics. The obtained mesoporous materials were characterize using B.E.T. method and FT-IR analysis. To investigate the effect of pore size (3,16 nm; 6,54 nm; 5,84 nm) and specific surface area- SSA (897,4 m2/g; 528,4 m2/g; 504,2 m2/g) value on release profile, three types of mesoporous materials with different structural properties were loaded with standardized chestnut extract (Castanea sativa) using concentration gradient method.

Special Issue

Pages: 3 - 3

Uses of Cyclohexane-1,4-Dione in the synthesis of heterocyclic compounds incorporating Tetrahydrobenzo[b]Thiophene: Synthesis, characterization and cytotoxicity

Nadia Y. Megally Abdo

Tetrahydrobenzo[b]Thiophene derivatives are well known  as  pharmaceutically  active  compounds and many of them are used as anti-cancer drugs. The aim of this work is to synthesize Tetrahydrobenzo[b]Thiophene derivative as a key starting material, use it for further  heterocyclization through reaction with different reagents and then study thier cytotoxicity and kinase inhibition.  2-Amino-6-oxo-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carbonitrile (3) was prepared  from the reaction of cyclohexan-1,4-dione  with elemental sulfur and malononitrile in1,4-dioxane containing a catalytic amount of  triethylamine. The latter compound reacted with triethylorthoformate and either malononitrile or ethyl cyanoacetate in 1,4-dioxane in presence of triethylamine afforded 4H-thieno[2,3-f]chromene 10a,b. Also, the reaction of compound (3) with phenylisothiocyanate in dimethylformamide in presence of potassium hydroxide followed by addition of either α-chloroacetate or ethyl chloroacetate afforded fused thiophene and thiazole derivatives, respectively

Special Issue

Pages: 4 - 4

Design and virtual screening of potential CD14inhibitors with focus and chlorogenic acid as Lead

Poyi Olanike Catherine

Pharmacovigilance (PV) is defined according to WHO, as the science and activities relating to the detection, assessment, understanding and prevention of adverse effects or any other drug-related problem. The aims of PV are to enhance patient care and safety in relation to the use of medicines; and to support public health programmes by providing reliable, balanced information for the effective assessment of the risk- benefit profile of medicines. In silico methods are primarily used alongside the generation of in vitro data both to create the model and to test it. Such models have seen frequent use in the discovery and optimization of novel molecules with affinity to a target, the clarification of absorption, distribution, metabolism, excretion and toxicity properties as well as physicochemical characterization. Cheminformatics plays a key role to maintain and access enormous amount of chemical data, produced by chemist by using a proper database.

Special Issue

Pages: 5 - 5

Computer-aided drug design and analysis of some isonicotinic hydrazide-derived analogues against Mycobacterium Tuberculosis targets (3igo.pdb and 4duh.pdb)

Naruka. S.Y

Isonicotinic acid hydrazide (INH) is the most important drug in the therapy of tuberculosis but not without some serious side effects. Therefore, with the use of computer aided drug design, the free amino group (-NH2) present in INH was condensed with various carbonyl compounds to form hydrazones-Schiff bases. These hydrazones were further converted into thiazolidinones by the addition of thiaglycolic acid. As shown in Fig. 1 and 2, molecular docking studies of the designed compounds reveal that all the analogues possess better binding affinity (INH-140: -6.4Kcal/mol, INH-360: -6.5Kcal/mol,) compared to parent compound-INH (INH-78: -5.1Kcal/mol) at the target proteins (3igo.pdb and 4duh.pdb). INH exhibited a better PA (prediction activity) score compared to the designed analogues but all the analogues show less toxicity potential relatively.

Special Issue

Pages: 6 - 6

Aloe dhufarensis - Anitoxidant and Anti-inflammatory properties

Neelam Sherwani

Aloe dhufarensis Lavranos a threatened species, is a near endemic to Southern Dhofar province of Oman and neighbouring eastern Yemen. Aloe dhufarensis is the most xerophytic of all the Aloe species found in Oman, this evergreen succulent stemless perennial, locally called Subr or Sakkal is known for centuries in Oman for its medicinal values, but the pharmacological effects of this important species have not been fully explored. This research was undertaken to validate the traditional use of Aloe dhufarensis in wound healing, to treat diabetes, fever and headache. The phyto-constituents, total phenoilcs, total flavonoid content, antioxidant, anti-inflammatory and anti-microbial activity of Aloe dhufarensis was evaluated.  In the present findings considerable antioxidant potential was depicted by the methanolic extracts of  Aloe dhufarensis, the leaf extracts exhibited considerable  DPPH scavenging activity ( IC50 value of 83.46 μg/ml), a strong hydrogen peroxide scavenging activity (IC50 value of  289.786 μg/ml) and a high total antioxidant capacity (256 ± 1.4 mg AAE/ g). The total phenolic content and the total flavonoid content was observed to be 452±3.2 mg GAE/ g and 44.16 ± 0.9 mg of QE/g of dry extract.  Leaf extract displayed significant protein denaturation inhibition and a marked anti-proteinase activity.

Special Issue

Pages: 7 - 7

Anti-microbial peptides Vs cancer cells ?? An academic review

Saleh Mohammed Alamri

Although there have been a large number of positive developments in the treatment of cancer in recent years, it has been noted that some cancer cells have developed a resistance to drugs. As a result, there is increasing attention being paid to the development of anti-cancer agents with an alternative mode of action.  Cationic Anti-Microbial Peptides (AMPs) are harmless to normal mammalian cells but have toxic effects on bacteria, and numerous studies have shown they can also have similar cytotoxic reactions to cancer cells. These studies have led to an increased interest in further understanding the immune system, focusing particularly on the potential for natural and synthetic AMPs to be used as clinical antibiotics. It is believed that AMPs strong binding to, and selective disruption of, cancer and bacterial cells can be partly attributed to the electrostatic attraction between these negatively charged cells and the positively charged AMPs.  At the moment, it is not clear why only some host defense peptides have the ability to eliminate cancer cells, nor whether the underlying molecular mechanisms relating to the anti-cancer and anti-bacterial properties of AMPs have any similarities.  This article reviews several studies documenting the various AMPs which have demonstrated cytotoxic activity towards cancer cells, as well as discussing whether these AMPs are suitable to be used as cancer therapy. 

Special Issue

Pages: 8 - 8

Controlled release of pyrimidine compound using polymeric coated zif-8 metal-organic framework as glucagon-like peptide-1 receptor agonist carrier

Ruba Fouad Al-Ajeil

This work demonstrates synthetic strategies for the incorporation of a synthesized pyrimidine glucagon-like peptide-1 (GLP-1) agonist into alginate-coated ZIF-8. The prepared pyrimidine GLP-1 agonist used for the treatment of diabetes type II, was trapped inside polymer coated ZIF-8. The encapsulation of the GLP-1 agonist was confirmed by UV-visible and FT-IR spectroscopies. Furthermore, the release kinetics of GLP-1 agonist drug from alginate-coated ZIF-8 were investigated in phosphate-buffered saline at 37 Ô?ŽC at pH 8 and 1.5. The alginate-coated ZIF-8 exhibited much faster drug release at basic pH than at pH 1.5, indicating the potential of the alginate-coated ZIF-8 system to overcome the fast degradation at acidic pH of the stomach and improve the drug’s activity. This study may open the way for the synthesis of new metal organic frameworks (MOFs) to enhance drug delivery systems.

Special Issue

Pages: 9 - 9

A simple and inexpensive simultaneous UV spectrophotometric method to determine Metformin and Glimepiride in fixed dose combinations tablet

Zilhadia

Type 2 diabetes mellitus is one of the most common metabolic diseases, with an increasing prevalence worldwide and a global pandemic. Metformin is the first agent used to lower blood glucose in type 2 diabetic patients. However, using the combination with the sulfonyl urea group, especially glimepiride has recently increased with the benefits of improving patient compliance and cost effectiveness. The purpose of this study was to validate the method of determining metformin/glimepiride fixed dose combinations taken at Pramuka market (the largest drug market in Jakarta) using an inexpensive and easy method, namely UV-Vis spectrophotometry. The maximum wavelength of metformin HCl was 237 and glimepiride was 228 nm. The maximum wavelengths of the two compounds were so close that a simultaneous method was carried out. As per ICH guidelines, the validation indicators measured are linearity, Limit of Detection (LOD), Limit of Quantification (LOQ), accuracy and precision.

Special Issue

Pages: 10 - 10

Direct reporting of adverse drug reactions by healthcare consumers in Africa; a narrative review

Halimat Adedeji- Adenola

Background: Direct reporting by health care consumers has been adopted in some developed and developing countries with a positive impact in improving pharmacovigilance through increased reporting rate. There are limited reports on direct reporting and its outcome in Africa.

Purpose: To identify and present the available evidence on direct reporting of adverse drug reactions by healthcare consumers in Africa.

Methodology: A review guided by Cochrane handbook was conducted. Electronic scientific databases such as PubMed, Cumulative Index to Nursing and Allied Health Literature, Embase and Cochrane Library were searched. Google scholar, general Google search engine, the website fotr the regulatory resources for africa and World Health Organisation-Uppsala monitoring were also searched for available guidelines, documents and publications. The review period was January 1992 to October 2019

Special Issue

Pages: 11 - 11

Counterfeit pharmaceuticals & medical devices ?? A global regulatory overview and the impact on the industry

Mark R. Willis

The threat and proliferation of counterfeit pharmaceuticals has escalated over the last 15 years.  In 2016, the World Health Organization estimated that 10 to 30 percent of all pharmaceuticals globally are counterfeit, though this number can increase up to 50 to 70 percent in some underdeveloped and in-transit nations.  While WHO estimated that only 10 percent of the pharmaceuticals in the United States (U.S.) market are counterfeit, this was still a considerable amount.  According to the IQVIA Institute for Human Data Sciences, in 2016 the United States dispensed a total of 4.453 billion prescription drugs.  This quantity is estimated to grow to over five billion by 2021.  If 10 percent of those prescriptions dispensed were counterfeit according to WHO’s estimates, then nearly 500 million counterfeit prescriptions were consumed throughout the United States in 2016

Special Issue

Pages: 12 - 12

The role of alkaline phosphatase (alp) and ?-glutamyltransferase (ggt) enzymes activities in monitoring the effect of enzyme replacement therapy in children with gaucher disease

Yasir sj.Alrubaye

The threat and proliferation of counterfeit pharmaceuticals has escalated over the last 15 years.  In 2016, the World Health Organization estimated that 10 to 30 percent of all pharmaceuticals globally are counterfeit, though this number can increase up to 50 to 70 percent in some underdeveloped and in-transit nations.  While WHO estimated that only 10 percent of the pharmaceuticals in the United States (U.S.) market are counterfeit, this was still a considerable amount.  According to the IQVIA Institute for Human Data Sciences, in 2016 the United States dispensed a total of 4.453 billion prescription drugs.  This quantity is estimated to grow to over five billion by 2021.  If 10 percent of those prescriptions dispensed were counterfeit according to WHO’s estimates, then nearly 500 million counterfeit prescriptions were consumed throughout the United States in 2016. 

Special Issue

Pages: 13 - 13

Prevalence of XDR-Salmonella typhi in Patients with Enteric Fever in a pediatric emergency of a public sector Hospital in Sindh

Abeera Tabassum

Objective: To determine prevalence of XDR S.Typhi in patients diagnosed with Enteric fever in pediatric emergency of a public sector hospital in Sindh.

Methods: We have conducted a retrospective review of patients record over a period of 6 months (Jan 2019 to Jun 2019) in a pediatric emergency of a public sector hospital supported by Childlife foundation. All patient diagnosed as Enteric fever on clinical basis and their blood culture sent were enrolled in the study. We collected the data on MR#, age, presenting complaint, diagnosis and blood culture report. Percentages and frequencies were calculated for quantitative variables.

Results: 42772 patients visited the PED during the study period. 1157 (2.7%) patients diagnosed clinically as enteric fever. 246 (21%) patients had their blood culture done hence enrolled in the study. Mean age was 5 .5 years (4 years – 7 years). 70% were male. 42 (17%) blood culture showed growth of XDR S. Typhi while 149 (60%) showed no growth. 55 (22%) patient had growth of non-resistant S. Typhi and other organisms. The overall cost of treatment per patient per day is 15 USD.

Conclusion: Emerging outbreak of XDR S.Typhi is alarming in Sindh. Increasing number of patients are being diagnosed daily adding additional healthcare cost. There are insufficient facilities to care for these sick children leading to increase length of stay in pediatric emergencies

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