Heterocycle Compounds with Antimicrobial Activity

2020 ◽  
Vol 26 (8) ◽  
pp. 867-904 ◽  
Author(s):  
Maria Fesatidou ◽  
Anthi Petrou ◽  
Geronikaki Athina

Background: Bacterial infections are a growing problem worldwide causing morbidity and mortality mainly in developing countries. Moreover, the increased number of microorganisms, developing multiple resistances to known drugs, due to abuse of antibiotics, is another serious problem. This problem becomes more serious for immunocompromised patients and those who are often disposed to opportunistic fungal infections. Objective: The objective of this manuscript is to give an overview of new findings in the field of antimicrobial agents among five-membered heterocyclic compounds. These heterocyclic compounds especially five-membered attracted the interest of the scientific community not only for their occurrence in nature but also due to their wide range of biological activities. Method: To reach our goal, a literature survey that covers the last decade was performed. Results: As a result, recent data on the biological activity of thiazole, thiazolidinone, benzothiazole and thiadiazole derivatives are mentioned. Conclusion: It should be mentioned that despite the progress in the development of new antimicrobial agents, there is still room for new findings. Thus, research still continues.

2019 ◽  
Vol 9 (1-s) ◽  
pp. 505-509 ◽  
Author(s):  
Shaheen Sulthana ◽  
P. Pandian

In recent years heterocyclic compounds analogues and derivatives have attracted wide attention due to their useful biological and pharmacological properties. Indole, Benzothiazole and its analogs are versatile substrates, which can be used for the synthesis of numerous heterocyclic compounds. Indole, Benzothiazole and its derivatives are used in organic synthesis and they are used in evaluating new product that possesses different biological activities. Hence, their extensive structural modification has result in different analogues of Indole and Benzothiazole derivatives depicting wide range of biological and pharmacological activities such as antiviral, anticonvulsant, anti-inflammatory, analgesic, antimicrobial and anticancer. This review article literature survey summarizes the synthesis and pharmacological activities of Indole, Benzothiazole and its derivatives. Keywords: Indole, Benzothiazole, antiviral, anticonvulsant, anti-inflammatory, analgesic, antimicrobial and anticancer


2020 ◽  
Vol 20 (5) ◽  
pp. 418-429 ◽  
Author(s):  
Asmaa F. Kassem ◽  
Fatimah Alshehrei ◽  
Eman M.H. Abbas ◽  
Thoraya A. Farghaly

Background & Objective:Quinazolines and their fused systems are noteworthy in pharmaceutical chemistry due to their wide range of biological activities.Methods:A direct and efficient approach for the synthesis of new series of fused quinazolines with triazole, thiazole, benzimidazole and tetrazole has been preceded via the reaction of quinazoline thione derivative with halogenated compounds or cyclocondensation of arylidene of quinazoline derivative with heterocyclic amines. Also, dibenzo[b,e][1,4]thiazepine derivatives was synthesized through the reaction of 2,6-bis-(2-chloro-benzylidene)-cyclohexanone with o-aminothiophenol.Results:The structures of all new synthesized heterocyclic compounds were confirmed and discussed on the bases of spectral data. The utility of the preparation and design of the above mentioned compounds has been shown to be clear in the results of their antimicrobial activity which revealed that some derivatives have potent activity exceeding or similar to the activity of the reference drugs.Conclusion:The insertion of triazole or thiazole moieties to be fused with quinazoline ring helps to enhance its antimicrobial activity.


2020 ◽  
Vol 24 (5) ◽  
pp. 473-486 ◽  
Author(s):  
Ligia S. da Silveira Pinto ◽  
Thatyana R. Alves Vasconcelos ◽  
Claudia Regina B. Gomes ◽  
Marcus Vinícius N. de Souza

Azetidin-2-ones (β-lactams) and its derivatives are an important group of heterocyclic compounds that exhibit a wide range of pharmacological properties such as antibacterial, anticancer, anti-diabetic, anti-inflammatory and anticonvulsant. Efforts have been made over the years to develop novel congeners with superior biological activities and minimal potential for undesirable side effects. The present review aimed to highlight some recent discoveries (2013-2019) on the development of novel azetidin-2-one-based compounds as potential anticancer agents.


Molecules ◽  
2021 ◽  
Vol 26 (11) ◽  
pp. 3166
Author(s):  
Anthi Petrou ◽  
Maria Fesatidou ◽  
Athina Geronikaki

Background: Thiazole is a good pharmacophore nucleus due to its various pharmaceutical applications. Its derivatives have a wide range of biological activities such as antioxidant, analgesic, and antimicrobial including antibacterial, antifungal, antimalarial, anticancer, antiallergic, antihypertensive, anti-inflammatory, and antipsychotic. Indeed, the thiazole scaffold is contained in more than 18 FDA-approved drugs as well as in numerous experimental drugs. Objective: To summarize recent literature on the biological activities of thiazole ring-containing compounds Methods: A literature survey regarding the topics from the year 2015 up to now was carried out. Older publications were not included, since they were previously analyzed in available peer reviews. Results: Nearly 124 research articles were found, critically analyzed, and arranged regarding the synthesis and biological activities of thiazoles derivatives in the last 5 years.


2021 ◽  
Vol 18 ◽  
Author(s):  
Nitishkumar S. Kaminwar ◽  
Sunil U. Tekale ◽  
Srinivas L. Nakkalwar ◽  
Rajendra P. Pawar

: Synthesis of isoxazole structural heterocyclic compounds is important due to their wide range of biological activities. In the present article, we report a convenient and easy method for the synthesis of 4-arylmethylidene-3-substituted-isoxazol-5(4H)-ones by the one-pot three-component reaction of aldehydes, β-keto ester, and hydroxylamine hydrochloride cat-alyzed by sulfated tin oxide as a heterogeneous catalyst.


Author(s):  
Rukhsana Tabassum ◽  
Muhammad Ashfaq ◽  
Hiroyuki Oku

Abstract:: Quinoline derivatives are considered as broad spectrum pharmacological compounds that exhibit wide range of biological activities. Integration of quinoline moiety can improve its physical and chemical properties and also pharmacological behavior. Due to its wide range of pharmaceutical applications it is very popular compound to design new drugs for treatment of multiple diseases like cancer, dengue fever, malaria, tuberculosis, fungal infections, AIDS, Alzheimer’s disease and diabetes . In this review our major focus is to pay attention on biological activities of quinoline compounds in treatment of these diseases such as, anti-viral, anti-cancer, anti-malarial, anti-bacterial, anti-fungal, anti-tubercular and anti-diabetic.


Author(s):  
Reyaz Hassan ◽  
Roohi Mohi-ud-din ◽  
Mohammad Ovais Dar ◽  
Abdul Jalil Shah ◽  
Prince Ahad Mir ◽  
...  

: Cancer is one of the most alarming diseases, with an estimation of 9.6 million deaths in 2018. Glioma occurs in glial cells surrounding nerve cells. The majority of the patients with gliomas have a terminal prognosis, and the ailment has significant sway on patients and their families, be it physical, psychological, or economic wellbeing. As Glioma exhibits, both intra and inter tumour heterogeneity with multidrug resistance and current therapies are ineffective. So the development of safer anti gliomas agents is the need of hour. Bioactive heterocyclic compounds, eithernatural or synthetic,are of potential interest since they have been active against different targets with a wide range of biological activities, including anticancer activities. In addition, they can cross the biological barriers and thus interfere with various signalling pathways to induce cancer cell death. All these advantages make bioactive natural compounds prospective candidates in the management of glioma. In this review, we assessed various bioactive heterocyclic compounds, such as jaceosidin, hispudlin, luteolin, silibinin, cannabidiol, tetrahydrocannabinol, didemnin B, thymoquinone, paclitaxel, doxorubicin, and cucurbitacins for their potential anti-glioma activity. Also, different kinds of chemical reactions to obtain various heterocyclic derivatives, e.g. indole, indazole, benzimidazole, benzoquinone, quinoline, quinazoline, pyrimidine, and triazine, are listed.


Author(s):  
Lucas F. E. Moor ◽  
Thatyana R. A. Vasconcelos ◽  
Raisa da R. Reis ◽  
Ligia S. S. Pinto ◽  
Thamires M. da Costa

: Quinoline and its derivatives comprise an important group of heterocyclic compounds that exhibits a wide range of pharmacological properties such as antibacterial, antiviral, anticancer, antiparasitic, anti-Alzheimer and anticholesterol. In fact, the quinoline nucleus is found in the structure of many drugs and in rational design in medicinal chemistry for the discovery of novel bioactive molecules. Persistent efforts have been made over the years to develop novel congeners with superior biological activities and minimal potential for undesirable side effects. This review highlights some discoveries on the development of quinoline-based compounds in recent years (2013-2019) focusing on their biological activities, including anticancer, antitubercular, antimalarial, anti-ZIKV, anti-DENV, anti-Leishmania and anti-Alzheimer’s disease.


Author(s):  
Praveen Kumar Sharma ◽  
Reena Makkar

ABSTRACTIn recent days, heterocycles and their derivatives have become strong reflection in medicinal research and pharmaceutical fields because of theirpractical pharmacological and biological activities. Organic compounds; mainly heterocyclic compounds are wealthy in natural world and containextra value because their structural subunits are established in many natural products such as enzymes, vitamins, antibiotics, acids, and hormones.Thiazine nucleuses found in compounds have variety of pharmacological activities such as antitumor, antimicrobial, antibacterial, antifungal, antiviral,and anti-inflammatory. This review spotlight on the substituted thiazines with possible antimicrobial activities that are at the present in development.Keywords: Antibacterial, Substituted thiazines, Antimicrobial agents.


2019 ◽  
Vol 25 (21) ◽  
pp. 2323-2337 ◽  
Author(s):  
Elisabetta Esposito ◽  
Claudio Nastruzzi ◽  
Maddalena Sguizzato ◽  
Rita Cortesi

The skin and mucous membranes are subjected to many disorders and pathological conditions. Nature offers a wide range of molecules with antioxidant activity able to neutralize, at least in part, the formation of free radicals and therefore to counteract the phenomena of cellular aging. Since synthetic drugs for the treatment of skin diseases can induce resistance, it is particularly interesting to use compounds of plant origin, transporting them in pharmaceutical forms capable of controlling their release and absorption. This review provides an overview of new findings about the use of lipid-based nanosystems for the delivery of natural molecules useful on the topical treatment of skin disorders. Several natural molecules encapsulated in lipid nanosystems have been considered in the treatment of some skin pathologies or diseases. Particularly, the use of rosemary and eucalyptus essential oil, saffron derivatives, curcumin, eugenol, capsaicin, thymol and lycopene has been reported. The molecules have been alternatively encapsulated in viscous systems, such as the organogels, or in liquid systems, such as ethosomes, transferosomes, solid lipid nanoparticles and monoolein based dispersions thickened by inclusion in carbomer gels. The nanostructured forms have been in vitro and in vivo investigated for the treatment of skin disorders due to dehydration, inflammation, melanoma, wound healing, fungal infections or psoriasis. The data reported in the different studies have suggested that the cutaneous application of lipid nanosystems allows a deep interaction between lipid matrix and skin strata, promoting a prolonged release and efficacy of the loaded natural molecules. This review suggests that the application of natural molecules onto the skin by lipid-based nanosystems can provide numerous clinician benefits in dermatology and cosmetics.


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