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Pyrazole is a multipurpose lead compound developed by chemical architecture for effective
molecules which are biologically active. The sugar hydrazones, their acetylated derivatives as well as
their derived acyclic C-nucleoside analogs, and the thioglycosides of the 1, 2, 4-traizole derivatives
were also prepared. Recently, a thiazole moiety was attached to the pyrazole ring and assayed against
different cancer cell lines ( Masaret, 2021 ). They are an important class of compounds for drug
development; thus, they have attracted much attention. Download Free PDF View PDF Inorganica
Chimica Acta A new di-?-alkoxo-bridged dinuclear copper(II) complex of 1-(2-hydroxyethyl)-
pyrazole. These Pyrazole skeletons comprise various ranges of pharmacological activities such as
analgesic, antipyretic, anticancer, antiviral, anti-inflammatory, antioxidants, antimicrobial, anti-
diabetic, anticonvulsant, ant arrhythmic activities. The structures of the new compounds were
elucidated using IR, 1H-NMR, 13C-NMR and mass spectroscopy. The use, distribution or
reproduction in other forums is permitted, provided the original author(s) and the copyright owner(s)
are credited and that the original publication in this journal is cited, in accordance with accepted
academic practice. Novel pyrazole ligands History The term pyrazole was given to this class of
compounds by German Chemist in 1883. Antinociceptive and Anti-inflammatory Activities As pain
is a hallmark of tissue damage and inflammatory processes ( Baral et al., 2019 ), pyrazole analogs
with antinociceptive and anti-inflammatory activities are important to analgesic drug development.
In respect of first-line analgesic drugs, the fusion of pyrimidine moiety to the pyrazole backbone ( 32
) similarly increased thermal latency (160%) and reduced abdominal writhing (83%) as compared
with tramadol (175%) and aspirin (78%), respectively ( Khalifa et al., 2019 ). The addition of the
adamantyl residue to 1,5-diaryl pyrazole ( 33 ) elicited a higher anti-inflammatory activity over the
antinociceptive effect. Some of these analogs inhibit COX enzymes and suppress the synthesis of
prostaglandin. Article types Author guidelines Editor guidelines Publishing fees Submission
checklist Contact editorial office Frontiers in Pharmacology. Pyrazole moieties are listed among the
highly used ring systems for small molecule drugs by the USFDASee also., an analog of pyrazole
with two non-adjacent nitrogen atoms., another analog, the nitrogen atom in position 1 replaced by
oxygen.References. Natural) (Chandi Charan Kandar and Dilipkumar Pal, Department of
Pharmaceutical Chemistry, Institute of Pharmacy, Jalpaiguri, Government of West Bengal, West
Bengal, India, and others). The methoxy moiety (the electron-donating group) of these analogs
confers additional hydrogen bonding and interaction with COX-2 active sites (Lys68, Tyr108,
Tyr341, Arg106, and Arg499). The antitumor activity of some of the synthesized compounds were
studied, and a number of the tested compounds showed significant activities 12. To browse
Academia.edu and the wider internet faster and more securely, please take a few seconds to upgrade
your browser. You can download the paper by clicking the button above. In fact, such a heterocyclic
moiety represents the core structure for number of drugsLITERATURE: Eman M. Flefel et.al have
reported the new substituted pyrazole, thiazole, and 1, 2, 4-triazole derivatives were synthesized. All
the a-bromoenones 2 and bipyrazoles 3 are new compounds and their identity was established by
m.p., spectral and analytical data. Insulin resistance, oxidative products, and atherogenic
dyslipidemia are among metabolic abnormalities underlying diabetes. Most of the synthesized
compounds did not exhibit significant inhibitory activity against the tested strains 15. Conflict of
Interest The authors declare that the research was conducted in the absence of any commercial or
financial relationships that could be construed as a potential conflict of interest. The presence of new
chemical entities could lead to additional or loss of molecular interactions. The aforementioned target
interactions revealed how structural modification could enrich mechanistic studies. Download Free
PDF View PDF A REVIEW ON RECENT DEVELOPMENT OF PYRAZOLINE AS A
PHARMOCOLOGICALLY ACTIVE MOLECULE Ravi Kant Pyrazoline, among the various 5-
membered heterocyclic compound derivatives has drawn attention towards it because of its various
pharmacologically activities associated with it. A pyrazole derivative used as an analgesicIn 1959, the
first natural pyrazole, was isolated from seeds of.In medicine, derivatives of pyrazole are widely
usedThe pyrazole ring is found within a variety of pesticides as fungicides, insecticides and
herbicides, including, and. With the data showing the cleavage of caspase-8 and caspase-9 through
caspase-3 and caspase-7 activation in the cascade of caspases ( Toton et al., 2013 ), compound 4 is
unlikely to elicit a specific effect. Numerous pyrazole derivatives have been found to possess a broad
spectrum of biological activities, which stimulated the research activity in this field.
Protonation of pyrazoles leads to pyrazolium cations that are less likely to undergo electrophilic
attack at C4, but attack at C3 is facilitated. Other Activities The modulation of central and peripheral
targets by the pyrazole ring and aforementioned moieties may induce diverse autonomic
manifestations. The purpose of this review was to collate literature work reported by researchers on
pyrazole for their various pharmacological activities and also reported recent efforts made on this
moiety. Rao Jyothi et al., have synthesized a novel series of 1, 3, 5-trisubstituted pyrazoles by the
cyclo condensation reaction of chalcones and substituted hydrazides by irradiation under microwave
energy and also by conventional method. These Pyrazole skeletons comprise various ranges of
pharmacological activities such as analgesic, antipyretic, anticancer, antiviral, anti-inflammatory,
antioxidants, antimicrobial, anti-diabetic, anticonvulsant, ant arrhythmic activities. You can
download the paper by clicking the button above. In the docking assay, the contribution of the 1,3-
diphenyl-1 H -pyrazole to hydrophobic interactions (Val 82, Ala 95, Val 127, Met 143, Met 143, and
Leu 197 of the ATP-binding pocket) and MEK inhibition ( Lv et al., 2016 ) was considered
significant. Download Free PDF View PDF See Full PDF Download PDF Loading Preview Sorry,
preview is currently unavailable. Cellular proliferation and metabolic enzymes provide important
cytotoxic, cytoprotective, antinociceptive, anti-inflammatory, and antidepressant targets. The
replacement of a polar 4-hydroxyphenyl substituent in pyrazoline nucleus ( 47 ) for a bulky
hydrophobic 1-naphthyl substituent ( 48 ) significantly reduced the antidepressant effect. They are
an important class of compounds for drug development; thus, they have attracted much attention.
The major activities exhibited by the pyrrole derivatives are insecticidal, antibacterial, antiviral,
sedative, hypnotic, anticonvulsant and antiinflammatory activity. Alteration in the activity of the
autonomic nervous system could impact cardiac, vascular, and respiratory functions. Patel, Vinod
Kumar Gurjar and Dilipkumar Pal, Ramanbhai Patel College of Pharmacy, Charotar University of
Science and Technology, Changa, Gujarat, India, and others). As the present review is limited to
selected biological activities, the author’s considerations, and future perspectives on some
representative analogs (see Supplementary Table S1 ), additional references are listed for the aspects
that are out of the present scope. Download Free PDF View PDF Biomedicines A Review of the
Recent Development in the Synthesis and Biological Evaluations of Pyrazole Derivatives Jack A
Tuszynski Pyrazoles are five-membered heterocyclic compounds that contain nitrogen. However, the
replacement of the pyrazole ring of mepirizole considerably attenuated this effect (7% inhibition of
ulcer formation) ( Ikeda et al., 1996 ). These data indicate that appropriate substitutions on the
pyrazole ring could reinforce gastroprotection. However, the specificity of the cytotoxic potential
and emerging resistance still need to be extensively evaluated. The existing collection of exertions on
research to provide information about the synthesis and innumerable biological activities of pyrazole
and their outcomes during the past year. The 4,5-dihydro-1 H -pyrazoles ( 47 and 48 ) showed a
considerable affinity with MAO-A amino acid residues (Ala68, Tyr69, Phe208, Tyr407, and Tyr444).
Tautomeric forms of unsubstituted pyrazole.Now a day’s vast number of compounds with pyrazole
nucleus have been reported to show a broad spectrum of biological activity including. Natural)
(Chandi Charan Kandar and Dilipkumar Pal, Department of Pharmaceutical Chemistry, Institute of
Pharmacy, Jalpaiguri, Government of West Bengal, West Bengal, India, and others). In the
meantime, pyrazole derivatives have been synthesized as target structures and have demonstrated
numerous biological activities such as antituberculosis, antimicrobial, antifungal, and anti-
inflammatory. A pyrazole derivative used as an analgesicIn 1959, the first natural pyrazole, was
isolated from seeds of.In medicine, derivatives of pyrazole are widely usedThe pyrazole ring is
found within a variety of pesticides as fungicides, insecticides and herbicides, including, and. Article
types Author guidelines Editor guidelines Publishing fees Submission checklist Contact editorial
office Frontiers in Pharmacology. Sahu SK et al., have synthesized a series of novel 4-(5-substituted
aryl-4, 5-dihydropyrazole-3-yl-amino) phenols by treating substituted aryl-N-chalconyl amino
phenols with hydrazine hydrate. The health promoting properties of these pyrazoles are discussed in
this book with different therapeutic applications of pyrazole scaffold. This mini-review explores
selected activities and structural modifications of some pyrazole analogs. The N1-benzenesulfonyl
ring at the pyrazoline nucleus seems to mediate additional interactions with the side chain and
backbone residues of amino acids at the binding pocket of MAO-A ( Tripathi et al., 2018 ). The
analogs with halogen groups in the phenyl ring could also promote hydrophobic interactions with
MAO-A. Pyrazole chemically known as 1, 2-diazole has become a popular topic due to its manifold
uses.
Patel, School of Pharmacy, Parul University, P. O. Limda, Vadodara, Gujarat, India, and others).
Topics related to pyrazole and its analogues as potential anticancer, anti-angiogenesis, antiviral,
antioxidative, anti-convulsive, anthelmintic, anti-inflammatory, antidiabetic agents are described in
this book in detail. A pyrazole derivative used as an analgesicIn 1959, the first natural pyrazole, was
isolated from seeds of.In medicine, derivatives of pyrazole are widely usedThe pyrazole ring is
found within a variety of pesticides as fungicides, insecticides and herbicides, including, and. As the
present review is limited to selected biological activities, the author’s considerations, and future
perspectives on some representative analogs (see Supplementary Table S1 ), additional references are
listed for the aspects that are out of the present scope. Lambat, Sami H. Mahmood and Subhash
Banerjee, Department of Chemistry, Guru Ghasidas University, Koni, Bilaspur, Chhattisgarh, India,
and others). Protonation of pyrazoles leads to pyrazolium cations that are less likely to undergo
electrophilic attack at C4, but attack at C3 is facilitated. It provides extended ideas on pyrazole and
its derivatives including their synthesis, chemistry, structure activity relationship (SAR) and
therapeutic applications. Compound 3b showed highest anti-bacterial and antifungal activity than all
other compounds 16. Tempat pkl smk di salatiga tempat pkl jurusan perkantoran di jogja cara mencari
tempat pkl untuk smk tempat pkl jurusan rpl di jogja. The a-bromo compounds 2 were utilized as
efficient precursors for the synthesis of several bipyrazolyl derivatives, 4-(3-methyl-1- phenyl-1H-
pyrazol-5-yl)-1, 3-diaryl-1H-pyrazoles (3). In the present review our main interest is to emphasize the
various synthetic molecules developed to promote the pyrazole molecule in the modern era of
anticancer agent. In respect of first-line analgesic drugs, the fusion of pyrimidine moiety to the
pyrazole backbone ( 32 ) similarly increased thermal latency (160%) and reduced abdominal writhing
(83%) as compared with tramadol (175%) and aspirin (78%), respectively ( Khalifa et al., 2019 ).
The addition of the adamantyl residue to 1,5-diaryl pyrazole ( 33 ) elicited a higher anti-
inflammatory activity over the antinociceptive effect. To browse Academia.edu and the wider
internet faster and more securely, please take a few seconds to upgrade your browser. The N-atom at
position 1 is unreactive, but loses its proton in the presence of base. The use, distribution or
reproduction in other forums is permitted, provided the original author(s) and the copyright owner(s)
are credited and that the original publication in this journal is cited, in accordance with accepted
academic practice. Numerous pyrazole derivatives have been found to possess a broad spectrum of
biological activities, which stimulated the research activity in this field. The restoration of redox
homeostasis or prevention of oxidative stress, inflammation, glycation, and vascular injury is key to
neuroprotection ( Hrelia et al., 2020 ). Chemically diverse pyrazole analogs have shown promising
cellular or neuronal protections. Therefore, many important properties of these molecules were
analyzed by comparing with the properties of benzene derivatives 3. In a summary, this book is a
valuable resource for research scholars, academics, students, industrialists and subject experts
working in the multidisciplinary fields like medicinal chemistry, synthetic chemistry, biochemistry,
pharmacology, natural product chemistry and other related areas in the field of pyrazole derivatives
drug discovery and research. Due to its wide range of biological activity, pyrazoles ring constitutes a
relevant synthetic route in pharmaceutical industry. Other Activities The modulation of central and
peripheral targets by the pyrazole ring and aforementioned moieties may induce diverse autonomic
manifestations. The N1-benzenesulfonyl ring at the pyrazoline nucleus seems to mediate additional
interactions with the side chain and backbone residues of amino acids at the binding pocket of
MAO-A ( Tripathi et al., 2018 ). The analogs with halogen groups in the phenyl ring could also
promote hydrophobic interactions with MAO-A. Meanwhile, different group substitutions on other
positions of pyrazole rings could offer additional data on potency and efficacy. The analogs that
suppress pro-inflammatory mediators could also modulate insulin sensitivity and protect against
metabolic syndrome. We hope that the bioactivity of pyrazole derivatives will be beneficial for the
rational design of new generation of small molecule drugs. Alteration in the activity of the autonomic
nervous system could impact cardiac, vascular, and respiratory functions. Altogether, the inhibitory
effects of these analogs on specific regulators of cellular processes could alter ATP production,
functions of organelles, redox reactions, and proliferative, vascular, and inflammatory responses.
Numerous interactions of these derivatives at their targets could impact future research
considerations and prospects while offering opportunities for optimizing therapeutic activity with
fewer adverse effects. In a classical method developed by German chemist in 1898, pyrazole was
synthesized from. RC, KC, IRJ, LR, HN, PC, MN, and JM contributed to the writing, revision, and
discussion.
Antinociceptive and Anti-inflammatory Activities As pain is a hallmark of tissue damage and
inflammatory processes ( Baral et al., 2019 ), pyrazole analogs with antinociceptive and anti-
inflammatory activities are important to analgesic drug development. However, a detailed
investigation of the level of analog-induced changes in redox reactions, oxidative stress,
inflammation, glycation, and other metabolic processes could facilitate the repositioning of cytotoxic
analogs for cytoprotection, and vice versa. To browse Academia.edu and the wider internet faster
and more securely, please take a few seconds to upgrade your browser. As a privileged structure
present in different classes of drugs, the pyrazole moiety has inspired new classes of drug
development ( Faria et al., 2017; Patil, 2020; Yet, 2018 ). In a classical method developed by German
chemist in 1898, pyrazole was synthesized from. In fact, such a heterocyclic moiety represents the
core structure for number of drugsLITERATURE: Eman M. Flefel et.al have reported the new
substituted pyrazole, thiazole, and 1, 2, 4-triazole derivatives were synthesized. Insulin resistance,
oxidative products, and atherogenic dyslipidemia are among metabolic abnormalities underlying
diabetes. The N1-benzenesulfonyl ring at the pyrazoline nucleus seems to mediate additional
interactions with the side chain and backbone residues of amino acids at the binding pocket of
MAO-A ( Tripathi et al., 2018 ). The analogs with halogen groups in the phenyl ring could also
promote hydrophobic interactions with MAO-A. The newly synthesized compounds were screened
for anti-inflammatory activity. It provides extended ideas on pyrazole and its derivatives including
their synthesis, chemistry, structure activity relationship (SAR) and therapeutic applications. Natural)
(Chandi Charan Kandar and Dilipkumar Pal, Department of Pharmaceutical Chemistry, Institute of
Pharmacy, Jalpaiguri, Government of West Bengal, West Bengal, India, and others). Like other
nitrogen involving heterocycles, different tautomeric structures can be written for pyrazoles. We hope
that the bioactivity of pyrazole derivatives will be beneficial for the rational design of new
generation of small molecule drugs. The substitutions, additions, or removal of functional groups are
effective strategies for designing biologically important analogs. Conversion to scorpionates
Pyrazoles react with to form a class of ligands known as. Tautomeric forms of unsubstituted
pyrazole.Now a day’s vast number of compounds with pyrazole nucleus have been reported to show
a broad spectrum of biological activity including. The presence of new chemical entities could lead to
additional or loss of molecular interactions. The antiedematogenic activity of these analogs (46 and
44%) appears similar to the analog of celecoxib (42%). Molecular docking data portraying compound
42 as the most active analog ( Hassan et al., 2019 ) provide clues to the role of the morpholine
(heterocyclic nucleus) with electron-withdrawing substituents on the phenyl ring. You can download
the paper by clicking the button above. All the a-bromoenones 2 and bipyrazoles 3 are new
compounds and their identity was established by m.p., spectral and analytical data. LT contributed to
the writing, revision, discussion, and drafting of the final work. Tempat pkl smk di salatiga tempat
pkl jurusan perkantoran di jogja cara mencari tempat pkl untuk smk tempat pkl jurusan rpl di jogja.
However, the specificity of the cytotoxic potential and emerging resistance still need to be
extensively evaluated. Additional interactions of these analogs with COX-2 (Arg106 and Ser339)
and 5-LOX (Leu368, Leu414, Ile415, and Phe421) could inspire additional modification in the
subsequent series of pyrazole analogs with the anti-inflammatory potential. This mini-review
explores cytotoxic, cytoprotective, antinociceptive, anti-inflammatory, and antidepressant activities
of some pyrazole analogs to advance structure-related pharmacological profiles and rational design
of new analogs. The published research works on pyrazole derivatives synthesis and biological
activities between January 2018 and December 2021 were retrieved from the Scopus database and
reviewed accordingly. The series of available pyrazole analogs could provide clues to structural
activity relationship (SAR) and predict potential therapeutic or adverse effects. FIGURE 1. These
Pyrazole skeletons comprise various ranges of pharmacological activities such as analgesic,
antipyretic, anticancer, antiviral, anti-inflammatory, antioxidants, antimicrobial, anti-diabetic,
anticonvulsant, ant arrhythmic activities. The pyrazole anion is much less reactive toward
nucleophiles, but the reactivity to electrophiles is increased 2Pyrazoles are aromatic molecules due to
their planar conjugated ring structures with six delocalized ?-electrons.
The growing number of synthesized analogs without data of biological activity, mechanism of action,
and comparative study with standard drugs containing the pyrazole ring ( Hill and Whelan, 1980;
Kameyama et al., 1981; Clemett and Goa, 2000; Samat et al., 2008; Straube, 2012; Dopp et al.,
2013; Mitou et al., 2015; Karrouchi et al., 2018 ) may yield promising results, if evaluated in the
future research. Deprotonation at C3can occur in the presence of strong base, leading to ring
opening. In this review, we report the structures of 1H-pyrazoles with their corresponding biological
activities for 21st (in 2000-2014 years) century. The new products 2 and 3 were tested for their in
vitro antibacterial activity against Staphylococcus aureus, Bacillus subtilis (Gram positive),
Escherichia coli, and Pseudomonas aeruginosa (Gram negative) and antifungal activity against
Aspergilus flavus and Aspergillus niger. Tautomeric forms of unsubstituted pyrazole.Now a day’s
vast number of compounds with pyrazole nucleus have been reported to show a broad spectrum of
biological activity including. Recently, a thiazole moiety was attached to the pyrazole ring and
assayed against different cancer cell lines ( Masaret, 2021 ). However, the number of phenyl
substituents on the pyrazole ring seems to create a specific pattern of metabolic enzyme inhibition.
The substitutions, additions, removal, or fusion of different functional groups in the pyrazole ring are
key to the synthesis of lead compounds that are effective against emerging and complex diseases (
Faisal et al., 2019; Aziz et al., 2020; Ramsay et al., 2018; Benek et al., 2020; He et al., 2016 ).
Pharmacological characterization of these analogs will benefit from our comprehension of the
functional group modifications on the central pyrazole ring ( Figure 2 ). These results support the
elevation of antinociceptive efficacy through the addition of electron-withdrawing groups. As the
pyrazole moiety offers a central motif to different functional groups ( Basu et al., 2017; Noor et al.,
2017; Tripathi et al., 2018; Murahari et al., 2019; Kenchappa and Bodke, 2020 ), its simplified
synthetic routes and potential activities are expected to continue to inspire additional chemical
modifications ( Johnston and Strobel, 2020 ) toward clinical applications. As the present review is
limited to selected biological activities, the author’s considerations, and future perspectives on some
representative analogs (see Supplementary Table S1 ), additional references are listed for the aspects
that are out of the present scope. REFERENCE ID: PHARMATUTOR-ART-2073PharmaTutor
(ISSN: 2347 - 7881)Volume 2, Issue 1Received On:; Accepted On:; Published On: How to cite this
article: V Yerragunta, D Suman, K swamy, V Anusha, P Patil, M Naresh, Pyrazole and Its Biological
Activity, PharmaTutor, 2014, 2(1), 40-48INTRODUCTION:The chemistry of pyrazoles has been
extensively investigated in the past. Article types Author guidelines Editor guidelines Publishing fees
Submission checklist Contact editorial office Submit your research Search Download article.
Compound 33 induced a lower antiedematogenic effect than the reference drug celecoxib (39 and
82% of edema inhibition, respectively). Therefore, many important properties of these molecules
were analyzed by comparing with the properties of benzene derivatives 3. All the synthesized
compounds were characterized by physical, chemical, analytical and spectral data. Altogether, the
inhibitory effects of these analogs on specific regulators of cellular processes could alter ATP
production, functions of organelles, redox reactions, and proliferative, vascular, and inflammatory
responses. However, the specificity of the cytotoxic potential and emerging resistance still need to be
extensively evaluated. The N-atom at position 1 is unreactive, but loses its proton in the presence of
base. In the present review our main interest is to emphasize the various synthetic molecules
developed to promote the pyrazole molecule in the modern era of anticancer agent. Download Free
PDF View PDF See Full PDF Download PDF Loading Preview Sorry, preview is currently
unavailable. The antimicrobial activity of the tested compounds is compared with the commercially
available antibiotic, ciprofloxacin and antifungal agent, fluconazole. Chemistry Of Pyrazole Pdf
Online Chemistry Of Pyrazole Pdf List Naresh 2Department of Pharmaceutical Chemistry,1Malla
Reddy College of Pharmacy, Maisammaguda, Secunderabad-500014, A.P.2Bharath Institute of
Technology Pharmacy-Ibrahimpatnam, AP.ABSTRACT:The aim of this review is to provide an
overview of diverse pharmacological activities of pyrazole moiety. The pyrazole anion is much less
reactive toward nucleophiles, but the reactivity to electrophiles is increased 2Pyrazoles are aromatic
molecules due to their planar conjugated ring structures with six delocalized ?-electrons. Novel
pyrazole ligands History The term pyrazole was given to this class of compounds by German
Chemist in 1883. The presence of new chemical entities could lead to additional or loss of molecular
interactions. The methoxy moiety (the electron-donating group) of these analogs confers additional
hydrogen bonding and interaction with COX-2 active sites (Lys68, Tyr108, Tyr341, Arg106, and
Arg499). To browse Academia.edu and the wider internet faster and more securely, please take a few
seconds to upgrade your browser. The article presents a comphrehensive review on the antimicrobial
activities of some novel derivatives of pyrrole ring.