in Wiley Online Library (wileyonlinelibrary.com).Thiazole and related nucleus are one of the most important potential entities in the largely growing chemical world of heterocyclic compounds exhibiting remarkable pharmacological activities. The knowledge of various synthetic pathways and diverse physicochemical parameters of such compounds draw the especial attention of medicinal chemists to produce combinatorial library and carry out exhaustive efforts in the search of lead molecules. The similar compounds synthesized through different routes bear variable magnitudes of biological activities. The present review highlights a broad view on biological activities of compounds having thiazole nucleus.
Due to its appreciable diversity in biological actions, thiazole and its substituted components, a significant class of heterocyclic compounds has developed as an influential scaffold in the field of chemical sciences. The variability of thiazole core has been expressed through the effective instigation of its anticancer (Dasatinib, Tiazofurin), antiretroviral (Ritonavir, Brecanavir), antimicrobial (Sulfathiazole, Ravuconazole) and anti-inflammatory (Fenclozic acid, Meloxicam) derivatives. This reasonable diversity in the physiological reaction pattern led many scientists to refine and develop new structural alternatives with much more efficient pharmacological action. This review is crucial for previous studies and projects to survey the antimicrobial activity of thiazole and thiazole related compounds to the mid of 2019.
Thiophene has emerged as a potent scaffold that has pulled the keen interest of the researchers because of its considerable diversity in biological activities. The versatility of the thiophene nucleus is demonstrated by the successful introduction of its derivatives, which have anti‐inflammatory (Thenaldine), anticancer (Ralitrexed), antioxidant (Erdosteine), and antimicrobial (Cefoxitin and Temocillin) activities. This decent variety in the biological response profile has pulled in the consideration of numerous researchers to research this skeleton to its distinctive potential against several activities. This review is integral to prior reviews and plans to review the work regarding antibacterial and antifungal activities of thiophene, substituted thiophene and thiophene‐like compounds, and also Schiff bases of thiophene and substituted thiophenes from year 1995 to the beginning of 2018.
: Cancer is the world's second-largest cause of mortality and one of the biggest global health concerns. The prevalence and mortality rates of cancer remain high despite significant progress in cancer therapy. The search for more effective as well as less toxic treatment methods for cancer is at the focus of current studies. Thiophene and its derivatives have surged as an influential scaffold which, because of their appreciable diversity in biological activities, has pulled the concerned interest of the researchers in the field of medicinal chemistry. By the affluent introduction of its derivatives, which have antioxidant, anti-inflammatory, antimicrobial, and anticancer activities, the adaptability of the thiophene moiety has been displayed. The nature and positioning of the substitutions significantly impacted thiophene moiety activity. This decent array in the living response account about this moiety has picked plentiful researcher’s consideration to inquire about it to its peculiar potential across certain activities. In the field of cancer therapy against different cancer cells, the structureactivity relationship for each of the derivatives showed an excellent understanding of thiophene moiety. Information from the various articles revealed the key role of thiophene moiety and its derivatives to develop the vital lead compound. The essential anticancer mechanisms identified include inhibition of the topoisomerase, inhibition of tyrosine kinase, tubulin interaction and apoptosis induction through activation of reactive oxygen species. This review is an endeavor to promote the anticancer potential of the derivatives whether having thiophene or condensed thiophene as a core moiety or as a substituent that can lead in the future to synthesize varieties of chemotherapeutic entities in the field of cancer treatment.
Unicelled conidia of Colletotrichum gloeosporioides germinated 3 h after inoculation producing single germ tubes. The orientation of the germ tubes and their lateral branches as they grew was towards the open stomata and away from closed stomata. By 24 h post-inoculation, the lateral branches had developed specialized infection vesicles either over the stomata or within the stomatal cavities. The infection vesicles produced primary infection hyphae which entered the leaves through stomatal openings. The disease symptoms became apparent by 6 days post-inoculation when clusters of abundant conidiophores emerged by rupturing the leaf epidermal layer, forming acervuli mostly near the base of idioblasts. The pressure exerted by the emerging conidiophores caused stretching of epidermal layer leading to the widening of the acervuli. The conidia are borne on the tips of the erect conidiophores. U. S. Copyright Clearance Center Code Statement: 0931±1785/2001/4912±0629 $ 15.00/0 www.blackwell.de/synergy 630 KUMAR UMAR et al.
The cardio protective action of cilostazol, milrinone and their combination effect on myocardial infarction induced by isoproterenol subjected to Wistar rats was done by studying various parameters-heart rate, % infarct size change, LDH level, CPKMB level, ECG pattern. In the following research work effect of synthetic drugs cilostazol, milrinone and their combined effect were studied over various biochemical and cardiac parameters. Isoproterenol was used in inducing myocardial infarction to Wistar rats. Isoproterenol (15 mg/100g) administration, causes an increased levels of biochemical markers-lactate dehydrogenase (2546.25±1.38), creatine phosphokinase (1485.5±.80) in serum of rats indicating potential action of isoproterenol on myocardium. Due to necrosis of myocardium a marked increase of these enzymes was seen in blood. A significant decrease in heart rate (262±.96) in isoproterenol treated rats was observed. Infarct size in ISO group rats (41%±.008) increased to certain extent with promiscuous yellow colored non-viable cells visible indicating infarction. Statistical analysis done by one-way ANOVA followed by the Dunnett's multiple comparison test where ISO control group compared with other groups, p value < 0.001 indicating extremely significant results. The present study demonstrated pharmacological benefits of combination dose of cilostazol, milrinone as evidenced by improvement in heart rate, Lactate dehydrogenase level, Creatine phosphokinase MB level, Electrocardiogram pattern, % infarct size.
abstract:The brachial plexus innervates the upper extremities. While variations in the formation of the brachial plexus and its terminal branches are quite common, it is uncommon for the median nerve to innervate the muscles of the arm. During the dissection of an elderly male cadaver at the Department of Anatomy, All India Institute of Medical Sciences, New Delhi, India, in 2016, the coracobrachialis muscle was found to be supplied by a direct branch from the lateral root of the median nerve and the musculocutaneous nerve was absent. The branches of the median nerve supplied the biceps brachii and brachialis muscles and the last branch continued as the lateral cutaneous nerve of the forearm. These variations may present atypically in cases of arm flexor paralysis or sensory loss on the lateral forearm. Knowledge of these variations is important in surgeries and during the administration of regional anaesthesia near the shoulder joint and upper arm.
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